2024-03-29T11:48:06Zhttps://minerva.usc.es/oai/requestoai:minerva.usc.es:10347/225482020-05-26T02:01:03Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Effect on nail structure and transungual permeability of the ethanol and poloxamer ratio from cyclodextrin-soluble polypseudorotaxanes based nail lacquer
Cutrín Gómez, Elena
Anguiano Igea, Soledad
Delgado Charro, M Begoña
Gómez Amoza, José Luis
Otero Espinar, Francisco Javier
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Transungual drug delivery
Nail
Medicated nail lacquers
Onychomycosis
Nail psoriasis ungueal
Polypseudorotaxanes
Methyl-β-cyclodextrin
Poloxamers;
Ciclopirox olamine
Clobetasol propionate
Aqueous-based nail lacquers have shown potential in promoting the diffusion of drugs into the nail. In our laboratory, we have recently developed a transungual delivery system based on an aqueous dispersion of cyclodextrin-poloxamer soluble polypseudorotaxanes, supramolecular host−guest assemblies that improves the drug permeation into the nail. However, the high-water content and the rheological and adhesive properties of this lacquer negatively affect properties that play a fundamental role in the patients’ acceptance such as stickiness, nail film formation or drying rate, properties. In this work, we have optimized the composition of these lacquers to improve these properties whilst maintaining good drug permeation profiles. Incorporating ethanol into the vehicle and reducing the proportion of Poloxamer 407 (PL), provided a good strategy. The use of hydro-ethanolic mixtures (>50% ethanol) and the reduction of the poloxamer concentration significantly improved the lacquer drying speed by reducing the stickiness and promoting film formation on the nail surface. Additionally, in a surprising way, the use of hydro-ethanolic vehicles further enhanced the permeation of ciclopirox olamine and clobetasol propionate, used for the treatment of onychomycosis and nail psoriasis respectively, into the nail and hooves
2020-05-25T15:01:00Z
2020-05-25T15:01:00Z
2018
journal article
Cutrín-Gómez, E.; Anguiano-Igea, S.; Delgado-Charro, M.B.; Gómez-Amoza, J.L.; Otero-Espinar, F.J. Effect on Nail Structure and Transungual Permeability of the Ethanol and Poloxamer Ratio from Cyclodextrin-Soluble Polypseudorotaxanes Based Nail Lacquer. Pharmaceutics 2018, 10, 156
http://hdl.handle.net/10347/22548
10.3390/pharmaceutics10030156
1999-4923
eng
https://doi.org/10.3390/pharmaceutics10030156
http://creativecommons.org/licenses/by/4.0/
open access
© 2018 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/)
MDPI
oai:minerva.usc.es:10347/158602023-07-10T06:16:39Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227com_10347_2924com_10347_2891col_10347_12265col_10347_12284
Determination of Gonyautoxin-4 in Echinoderms and Gastropod Matrices by Conversion to Neosaxitoxin Using 2-Mercaptoethanol and Post-Column Oxidation Liquid Chromatography with Fluorescence Detection
Silva, Marisa
Rey López, Verónica
Botana López, Ana María
Vasconcelos, Vitor
Botana López, Luis Miguel
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Universidade de Santiago de Compostela. Departamento de Química Analítica, Nutrición e Bromatoloxía
Paralytic shellfish poisoning
Toxins
Post-column oxidation fluorescence
Interfering matrix peaks
Thiol compounds
Paralytic Shellfish Toxin blooms are common worldwide, which makes their monitoring crucial in the prevention of poisoning incidents. These toxins can be monitored by a variety of techniques, including mouse bioassay, receptor binding assay, and liquid chromatography with either mass spectrometric or pre- or post-column fluorescence detection. The post-column oxidation liquid chromatography with fluorescence detection method, used routinely in our laboratory, has been shown to be a reliable method for monitoring paralytic shellfish toxins in mussel, scallop, oyster and clam species. However, due to its high sensitivity to naturally fluorescent matrix interferences, when working with unconventional matrices, there may be problems in identifying toxins because of naturally fluorescent interferences that co-elute with the toxin peaks. This can lead to erroneous identification. In this study, in order to overcome this challenge in echinoderm and gastropod matrices, we optimized the conversion of Gonyautoxins 1 and 4 to Neosaxitoxin with 2-mercaptoethanol. We present a new and less time-consuming method with a good recovery (82.2%, RSD 1.1%, n = 3), requiring only a single reaction step
2017-10-19T11:19:21Z
2017-10-19T11:19:21Z
2015-12-30
journal article
Silva, M.; Rey, V.; Botana, A.; Vasconcelos, V.; Botana, L. Determination of Gonyautoxin-4 in Echinoderms and Gastropod Matrices by Conversion to Neosaxitoxin Using 2-Mercaptoethanol and Post-Column Oxidation Liquid Chromatography with Fluorescence Detection. Toxins 2016, 8, 11.
2072-6651
http://hdl.handle.net/10347/15860
10.3390/toxins8010011
eng
http://doi.org.10.3390/toxins8010011
info:eu-repo/grantAgreement/EC/FP7/312184
info:eu-repo/grantAgreement/MINECO/Plan Estatal de Investigación Científica y Técnica y de Innovación 2013-2016/AGL2014-58210-R/ES/EVALUACION DE LA SEGURIDAD ALIMENTARIA DE PRODUCTOS PESQUEROS ASOCIADA A LA PRESENCIA DE TOXINAS MARINAS DE NUEVA APARICION EN AGUAS EUROPEAS
http://creativecommons.org/licenses/by/4.0/
open access
© 2015 by the authors; licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons by Attribution (CC-BY) license (http://creativecommons.org/licenses/by/4.0/)
MDPI
oai:minerva.usc.es:10347/244792021-02-17T03:01:02Zcom_10347_2989com_10347_2889com_10347_227com_10347_2904com_10347_2890com_10347_2888col_10347_9764col_10347_12265
Pharmacological Extracts and Molecules from Virola Species: Traditional Uses, Phytochemistry, and Biological Activity
González Rodríguez, María
Ruiz Fernández, Clara
Vera, Francisco
Ait Eldjoudi, Djedjiga
Ramadan Farrag Abdel Hafez, Yousof
Cordero Barreal, Alfonso
Pino Mínguez, Jesús
Lago Paz, María Francisca
Campos Toimil, Manuel
Carvalho, Glaucimeire Rocha
Pereira, Thiago Melo Costa
Gualillo, Oreste
Universidade de Santiago de Compostela. Centro de Investigación en Medicina Molecular e Enfermidades Crónicas
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Myristicaceae
Pharmacology
Phytotherapy
Virola surinamensis
Virola sebifera
Resin
Essential oil
Flavonoid
Lignan
Alkaloid
Virola is the largest genus of Myristicaceae in America, comprising about 60 species of medium-sized trees geographically spread from Mexico to southern Brazil. The plant species of this genus have been widely used in folk medicine for the treatment of several ailments, such as rheumatic pain, bronchial asthma, tumors in the joints, intestinal worms, halitosis, ulcers, and multiple infections, due to their pharmacological activity. This review presents an updated and comprehensive summary of Virola species, particularly their ethnomedicinal uses, phytochemistry, and biological activity, to support the safe medicinal use of plant extracts and provide guidance for future research. The Virola spp.’s ethnopharmacology, including in the treatment of stomach pain and gastric ulcers, as well as antimicrobial and tryponosomicidal activities, is attributable to the presence of a myriad of phytoconstituents, such as flavonoids, tannins, phenolic acids, lignans, arylalkanones, and sitosterol. Hence, such species yield potential leads or molecular scaffolds for the development of new pharmaceutical formulations, encouraging the elucidation of not-yet-understood action mechanisms and ascertaining their safety for humans
2021-02-16T12:16:01Z
2021-02-16T12:16:01Z
2021
journal article
Molecules 2021, 26(4), 792; https://doi.org/10.3390/molecules26040792
http://hdl.handle.net/10347/24479
10.3390/molecules26040792
1420-3049
eng
https://doi.org/10.3390/molecules26040792
http://creativecommons.org/licenses/by/4.0/
open access
© 2021 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/)
Atribución 4.0 Internacional
MDPI
oai:minerva.usc.es:10347/267212023-07-10T06:11:22Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Niosomes-based gene delivery systems for effective transfection of human mesenchymal stem cells
Carballo Pedrares, Natalia
Kattar, Axel
Concheiro Nine, Ángel Joaquín
Álvarez Lorenzo, Carmen Isabel
Rey Rico, Ana
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Niosomes
MSCs
DOTMA
Gene transfer
Sucrose
Stability
Gene transfer to mesenchymal stem cells (MSCs) has arisen as a powerful approach to increase the therapeutic potential of this effective cell population. Over recent years, niosomes have emerged as self-assembled carriers with promising performance for gene delivery. The aim of our work was to develop effective niosomes-based DNA delivery platforms for targeting MSCs. Niosomes based on 1,2-di-O-octadecenyl-3-trimethylammonium propane (DOTMA; 0, 7 or 15%) as cationic lipid, cholesterol as helper lipid, and polysorbate 60 as non-ionic surfactant, were prepared using a reverse phase evaporation technique. Niosomes dispersions (filtered or not) and their corresponding nioplexes with a lacZ plasmid were characterized in terms of size, charge, protection, and complexation abilities. DOTMA concentration had a large influence on the physicochemical properties of resulting nioplexes. Transfection efficiency and cytotoxic profiles were assessed in two immortalized cell lines of MSCs. Niosomes formulated with 15% DOTMA provided the highest values of β-galactosidase activity, being similar to those achieved with Lipofectamine®, but showed less cytotoxicity. Filtration of niosomes dispersions before adding to the cells resulted in a loss of their biological activities. Storage of niosomes formulations (for 30 days at room temperature) caused minor modification of their physicochemical properties but also attenuated the transfection capability of the nioplexes. Differently, addition of the lysosomotropic agent sucrose into the culture medium during transfection or to the formulation itself improved the transfection performance of non-filtered niosomes. Indeed, steam heat-sterilized niosomes prepared in sucrose medium demonstrated transfection capability
2021-08-09T11:42:14Z
2021-08-09T11:42:14Z
2021
journal article
Materials Science and Engineering: C 2021, 128: 112307. https://doi.org/10.1016/j.msec.2021.112307
0928-4931
http://hdl.handle.net/10347/26721
10.1016/j.msec.2021.112307
eng
https://doi.org/10.1016/j.msec.2021.112307
info:eu-repo/grantAgreement/AEI/Plan Estatal de Investigación Científica y Técnica y de Innovación 2017-2020/RTI2018-099389-A-100/ES/CRIOGELES ACTIVADOS POR GENES PARA REPARACION DE CARTILAGO
info:eu-repo/grantAgreement/AEI/Plan Estatal de Investigación Científica y Técnica y de Innovación 2017-2020/PID2020-113881RB-I00/ES
info:eu-repo/grantAgreement/EC/H2020/813440
http://creativecommons.org/licenses/by/4.0/
open access
© 2021 The Authors. Published by Elsevier B.V. This is an open access article under the CC BY license (http://creativecommons.org/licenses/by/4.0/)
Atribución 4.0 Internacional
Elsevier
oai:minerva.usc.es:10347/236142023-03-27T08:24:52Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Lidocaine-Loaded Solid Lipid Microparticles (SLMPs) Produced from Gas-Saturated Solutions for Wound Applications
López Iglesias, Clara
Quílez, Cristina
Barros, Joana
Velasco, Diego
Álvarez Lorenzo, Carmen Isabel
Jorcano, José L.
Monteiro, Fernando J.
García González, Carlos Alberto
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
SLMPs
Drug delivery
Lidocaine HCl
3D-bioprinting
PGSS technique
Wound healing
Pain
The delivery of bioactive agents using active wound dressings for the management of pain and infections offers improved performances in the treatment of wound complications. In this work, solid lipid microparticles (SLMPs) loaded with lidocaine hydrochloride (LID) were processed and the formulation was evaluated regarding its ability to deliver the drug at the wound site and through the skin barrier. The SLMPs of glyceryl monostearate (GMS) were prepared with different LID contents (0, 1, 2, 4, and 10 wt.%) using the solvent-free and one-step PGSS (Particles from Gas-Saturated Solutions) technique. PGSS exploits the use of supercritical CO2 (scCO2) as a plasticizer for lipids and as pressurizing agent for the atomization of particles. The SLMPs were characterized in terms of shape, size, and morphology (SEM), physicochemical properties (ATR-IR, XRD), and drug content and release behavior. An in vitro test for the evaluation of the influence of the wound environment on the LID release rate from SLMPs was studied using different bioengineered human skin substitutes obtained by 3D-bioprinting. Finally, the antimicrobial activity of the SLMPs was evaluated against three relevant bacteria in wound infections (Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa). SLMPs processed with 10 wt.% of LID showed a remarkable performance to provide effective doses for pain relief and preventive infection effects
2020-11-09T09:35:09Z
2020-11-09T09:35:09Z
2020
journal article
López-Iglesias, C.; Quílez, C.; Barros, J.; Velasco, D.; Alvarez-Lorenzo, C.; Jorcano, J.L.; Monteiro, F.J.; García-González, C.A. Lidocaine-Loaded Solid Lipid Microparticles (SLMPs) Produced from Gas-Saturated Solutions for Wound Applications. Pharmaceutics 2020, 12, 870
http://hdl.handle.net/10347/23614
10.3390/pharmaceutics12090870
1999-4923
eng
https://doi.org/10.3390/pharmaceutics12090870
http://creativecommons.org/licenses/by/4.0/
open access
© 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/)
Atribución 4.0 Internacional
MDPI
oai:minerva.usc.es:10347/224712021-05-21T13:22:19Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Potent in vitro α-glucosidase inhibition of secondary metabolites derived from dryopteris cycadina
Amin, Surriya
Ullah, Barkat
Ali, Mumtaz
Rauf, Abdur
Khan, Haroon
Uriarte Villares, Eugenio
Sobarzo Sánchez, Eduardo Marcelo
Universidade de Santiago de Compostela. Departamento de Química Orgánica
Universidade de Santiago de Compostela. Facultade de Farmacia
Dryopteris cycadina
Isolated compounds
α-glucosidase inhibition
Molecular docking
α-glucosidase is responsible for the hydrolysis of complex carbohydrates into simple
absorbable glucose and causes postprandial hyperglycemia. α-glucosidase inhibition is thus the ideal
target to prevent postprandial hyperglycemia. The present study was therefore designed to analyze
the effects of various compounds isolated from Dryopteris cycadina against α-glucosidase including
β-Sitosterol 1, β-Sitosterol3-O-β-D-glucopyranoside 2, 3, 5, 7-trihydroxy-2-(p-tolyl) chorman-4-one 3,
Quercetin-3-0-β-D-glucopyranoside (3/→0-3///)- β-D- Quercetin -3-0- β –D-galactopyranoside 4 and
5, 7, 4/
-Trihydroxyflavon-3-glucopyranoid 5. The in vitro spectrophotometric method was used for
the analysis of test compounds against possible inhibition. Similarly, molecular docking studies were
performed using the MOE software. These compounds showed concentration-dependent inhibition
on α-glucosidase, and compounds 1 (IC50: 143 ± 0.47 µM), 3 (IC50:133 ± 6.90 µM) and 5 (IC50: 146 ±
1.93 µM) were more potent than the standard drug, acarbose (IC50: 290 ± 0.54 µM). Computational
studies of these compounds strongly supported the in vitro studies and showed strong binding
receptor sensitivity. In short, the secondary metabolites isolated from D. cycadina demonstrated
potent α-glucosidase inhibition that were supported by molecular docking with a high docking score
2020-05-20T13:41:44Z
2020-05-20T13:41:44Z
2019
journal article
Amin, S.; Ullah, B.; Ali, M.; Rauf, A.; Khan, H.; Uriarte, E.; Sobarzo-Sánchez, E. (2019). Potent in vitro α-glucosidase inhibition of secondary metabolites derived from dryopteris cycadina. Molecules 24(3), 427; doi: 10.3390/molecules24030427
http://hdl.handle.net/10347/22471
10.3390/molecules24030427
1420-3049
eng
https://doi.org/10.3390/molecules24030427
http://creativecommons.org/licenses/by/4.0/
open access
© 2019 by the authors. Open Access. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/)
MDPI
oai:minerva.usc.es:10347/303292023-03-17T03:03:25Zcom_10347_2988com_10347_2889com_10347_227com_10347_2904com_10347_2890com_10347_2888com_10347_2927com_10347_2891col_10347_11762col_10347_12265col_10347_12292
Supramolecular fibrillation of peptide amphiphiles induces environmental responses in aqueous droplets
Booth, Richard
Insua López, Ignacio
Ahmed, Sahnawaz
Rioboo Vidal, Alicia
Montenegro García, Javier
Universidade de Santiago de Compostela. Centro de Investigación en Química Biolóxica e Materiais Moleculares
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Universidade de Santiago de Compostela. Departamento de Química Orgánica
Self-assembly
Supramolecular polymers
One-dimensional (1D) supramolecular polymers are commonly found in natural and synthetic systems to prompt functional responses that capitalise on hierarchical molecular ordering. Despite amphiphilic self-assembly being significantly studied in the context of aqueous encapsulation and autopoiesis, very little is currently known about the physico-chemical consequences and functional role of 1D supramolecular polymerisation confined in aqueous compartments. Here, we describe the different phenomena that resulted from the chemically triggered supramolecular fibrillation of synthetic peptide amphiphiles inside water microdroplets. The confined connection of suitable dormant precursors triggered a physically autocatalysed chemical reaction that resulted in functional environmental responses such as molecular uptake, fusion and chemical exchange. These results demonstrate the potential of minimalistic 1D supramolecular polymerisation to modulate the behaviour of individual aqueous entities with their environment and within communities
2023-03-16T10:08:10Z
2023-03-16T10:08:10Z
2021
journal article
Booth, R., Insua, I., Ahmed, S. et al. Supramolecular fibrillation of peptide amphiphiles induces environmental responses in aqueous droplets. Nat Commun 12, 6421 (2021). https://doi.org/10.1038/s41467-021-26681-2
2041-1723
http://hdl.handle.net/10347/30329
10.1038/s41467-021-26681-2
eng
https://doi.org/10.1038/s41467-021-26681-2
http://creativecommons.org/licenses/by/4.0/
open access
© The Author(s) 2021. This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in a credit line to the material. If material is not included in the article’s Creative Commons license and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this license, visit http://creativecommons.org/ licenses/by/4.0/
Atribución 4.0 Internacional
Nature
oai:minerva.usc.es:10347/212012020-04-07T02:01:34Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Creme tópico de capsaicina (8%) para o tratamento da síndrome da dor miofascial
Romero, Valéria
Rodrigues Lara, Juliana
Otero Espinar, Francisco Javier
Salgado, Manoel Henrique
Módolo, Norma Sueli Pinheiro
Barros, Guilherme Antonio Moreira
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Capsaicina
Administração tópica
Pontos-gatilho
Síndrome de dor miofascial
Capsaicin
Topical route
Trigger points
Myofascial pain syndrome
Justificativa:
A síndrome da dor miofascial é uma causa comum de dor musculoesquelética. O objetivo deste estudo foi avaliar a potencial ação analgésica de 8% do creme de capsaicina para uso tópico em pacientes com síndrome da dor miofascial.
Métodos:
Inicialmente, as formulações de creme de PLA (Placebo) e CPS (Capsaicina 8%) foram desenvolvidas e aprovadas de acordo com os requisitos atuais da agência de autoridade de saúde. Os 40 pacientes participantes foram distribuídos aleatoriamente e de forma duplo‐cega para os grupos PLA e CPS. Antes dos cremes serem administrados topicamente, de acordo com o grupo de alocação, o anestésico local foi usado por um período de 50 minutos diretamente na área de interesse. A administração ocorreu na área da pele sobre o ponto‐gatilho, o qual apresentou a área dolorida à palpação, em uma quantidade de 10 g por 30 minutos em área circular com diâmetro de 24 mm. Posteriormente, o creme foi removido e os parâmetros de tolerabilidade à pele foram avaliados. A dor foi medida antes e durante a aplicação da formulação, bem como 1 hora, 7 dias, 30 dias e 60 dias após o procedimento avaliado pela escala numérica verbal (0 a 10, com zero sem dor e dez a pior dor imaginável).
Resultados:
Nenhum paciente no grupo PLA experimentou hiperemia ou sensação de queimação no local de aplicação do creme, enquanto 85% dos que experimentaram no grupo CPS apresentaram hiperemia ou sensação de queimação 15 minutos. Essas queixas desapareceram 24 horas após a remoção do creme. O escore de dor no grupo CPS diminui de forma sustentada até o 60° dia de avaliação (p < 0,0001).
Conclusão:
A administração das formulações não causou lesões cutâneas agudas ou crônicas macroscópicas nos pacientes e a formulação de 8% de capsaicina foi benéfica e bem tolerada
Background: Myofascial pain syndrome is a common cause of musculoskeletal pain. The objective of this study was to evaluate the potential analgesic action of 8% capsaicin cream for topical use in patients with myofascial pain syndrome.
Methods: Initially, cream formulations of PLA (Placebo) and CPS (Capsaicin 8%) were developed and approved according to the current requirements of the health authority agency. The 40 participating patients were randomly assigned to the PLA and CPS groups in a double‐blind fashion. Before the creams were topically administered, according to the allocation group, the local anesthetic was used for a period of 50 minutes directly in the area of interest. The cream was applied to the area of the skin over the trigger point, represented by the area with pain at palpation, in an amount of 10 g for 30 minutes in a circular area of 24 mm diameter. Subsequently, the cream was removed and the skin tolerability parameters were evaluated. The pain was measured before and during the formulation application, as well as at 1 hour, 7 days, 30 days, and 60 days after the procedure, evaluated using a verbal numerical scale (from 0 to 10: with 0 = no pain and 10 = worst pain imaginable). Results: No patient in PLA Group had hyperemia or burning sensation at the site of application, while 85% of patients in CPS Group had hyperemia or burning sensation at 15 minutes. These complaints disappeared 24 hours after the cream was removed. The pain score in CPS Group decreased steadily up to the 60th day of evaluation (p < 0.0001).
Conclusion: Application of the formulations did not cause macroscopic acute or chronic skin lesions in patients, and the 8% capsaicin formulation was beneficial and well tolerated
2020-04-06T19:03:39Z
2020-04-06T19:03:39Z
2019
journal article
Romero, V., Rodrigues Lara, J., Otero-Espinar, F., Salgado, M.H., Pinheiro Modolo, N.S., Moreira de Barros, G.A. (2019). Creme tópico de capsaicina (8%) para o tratamento da síndrome da dor miofascial. "Revista Brasileira de Anestesiologia", 69(5), 432-438
0034-7094
http://hdl.handle.net/10347/21201
10.1016/j.bjan.2019.06.008
1806-907X
por
https://doi.org/10.1016/j.bjan.2019.06.008
https://creativecommons.org/licenses/by-nc-nd/4.0/
open access
© 2019 Sociedade Brasileira de Anestesiologia. Published by Elsevier Editora Ltda. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/)
Elsevier
oai:minerva.usc.es:10347/212032023-07-10T06:15:59Zcom_10347_2906com_10347_2890com_10347_2888com_10347_227com_10347_2904col_10347_15791col_10347_12265
Acute Toxicity Assessment: Macroscopic and Ultrastructural Effects in Mice Treated with Oral Tetrodotoxin
Abal Camaño, Paula
Louzao Ojeda, María Carmen
Vilariño del Río, Natalia
Rodríguez Vieytes, María Mercedes
Botana López, Luis Miguel
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Tetrodotoxin
Macroscopic alterations
Ultrastructural changes
Gastrointestinal effect
Mitochondria swelling
Rough endoplasmic reticulum swelling
Tetrodotoxin (TTX) is an extremely toxic marine compound produced by different genera of bacteria that can reach humans through ingestion mainly of pufferfish but also of other contaminated fish species, marine gastropods or bivalves. TTX blocks voltage-gated sodium channels inhibiting neurotransmission, which in severe cases triggers cardiorespiratory failure. Although TTX has been responsible for many human intoxications limited toxicological data are available. The recent expansion of TTX from Asian to European waters and diversification of TTX-bearing organisms entail an emerging risk of food poisoning. This study is focused on the acute toxicity assessment of TTX administered to mice by oral gavage following macroscopic and microscopic studies. Necropsy revealed that TTX induced stomach swelling 2 h after administration, even though no ultrastructural alterations were further detected. However, transmission electron microscopy images showed an increase of lipid droplets in hepatocytes, swollen mitochondria in spleens, and alterations of rough endoplasmic reticulum in intestines as hallmarks of the cellular damage. These findings suggested that gastrointestinal effects should be considered when evaluating human TTX poisoning.
2020-04-06T19:42:19Z
2020-04-06T19:42:19Z
2019
journal article
Abal, P., Louzao, M.C., Vilariño, N., Vyeites, M.R., Botana, L.M. (2019). Acute Toxicity Assessment: Macroscopic and Ultrastructural Effects in Mice Treated with Oral Tetrodotoxin. "Toxins", 11(6), 305
http://hdl.handle.net/10347/21203
10.3390/toxins11060305
2072-6651
eng
https://doi.org/10.3390/toxins11060305
info:eu-repo/grantAgreement/MINECO/Plan Estatal de Investigación Científica y Técnica y de Innovación 2013-2016/AGL2014-58210-R/ES/EVALUACION DE LA SEGURIDAD ALIMENTARIA DE PRODUCTOS PESQUEROS ASOCIADA A LA PRESENCIA DE TOXINAS MARINAS DE NUEVA APARICION EN AGUAS EUROPEAS
info:eu-repo/grantAgreement/MINECO/Plan Estatal de Investigación Científica y Técnica y de Innovación 2013-2016/AGL2016-78728-R/ES
https://creativecommons.org/licenses/by/4.0/
open access
© 2019 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/)
MDPI
oai:minerva.usc.es:10347/213252020-04-14T02:01:28Zcom_10347_2989com_10347_2889com_10347_227com_10347_2904com_10347_2890com_10347_2888col_10347_9764col_10347_12265
Gut microbiota, diet, and chronic diseases: the role played by oxidative stress
Vasquez, Elisardo C.
Pereira, Thiago M.C.
Campos Toimil, Manuel
Baldo, Marcelo P.
Peotta, Veronica A.
Universidade de Santiago de Compostela. Centro de Investigación en Medicina Molecular e Enfermidades Crónicas
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
2020-04-13T15:58:10Z
2020-04-13T15:58:10Z
2019
journal article
Vasquez, E., Pereira, T., Campos-Toimil, M., Baldo, M. and Peotta, V., 2019. Gut Microbiota, Diet, and Chronic Diseases: The Role Played by Oxidative Stress. Oxidative Medicine and Cellular Longevity, 2019, pp.1-3.
1942-0900
http://hdl.handle.net/10347/21325
10.1155/2019/7092032
1942-0994
eng
https://doi.org/10.1155/2019/7092032
https://creativecommons.org/licenses/by/4.0/
open access
Copyright © 2019 Elisardo C. Vasquez et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited
Hindawi
oai:minerva.usc.es:10347/225462020-05-26T02:00:53Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Effect of penetration enhancers on drug nail permeability from cyclodextrin/poloxamer-soluble polypseudorotaxane-based nail lacquers
Cutrín Gómez, Elena
Anguiano Igea, Soledad
Delgado Charro, M Begoña
Gómez Amoza, José Luis
Otero Espinar, Francisco Javier
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Transungual drug delivery
Nail
Medicated nail lacquers
Onychomycosis
Nail psoriasis
Polypseudorotaxanes
Methyl-β-cyclodextrin
Poloxamers
Ciclopirox olamine
Clobetasol propionate
Penetration enhancer
Nail delivery has interest for local treatment of nail diseases. Nevertheless, the low permeability of drugs in the nail plaque precludes the efficacy of local treatments. The use of penetration enhancers can increase drug permeability and improve the efficacy of the treatment of nail pathologies. In this work, different chemical substances have been evaluated as potential penetration enhancers. With this aim, the effect of different substances such as sodium lauryl sulfate (SLS), polyethylene glycol 300 (PEG 300), carbocysteine, N-acetylcysteine, lactic acid, potassium phosphate, Labrasol® and Labrafil® in the microstructure, nail surface and drug permeability has been evaluated. The models obtained by mercury intrusion porosimetry and PoreXpert™ software show a more porous structure in nails treated with different enhancers. Permeation studies with bovine hooves and nails revealed that all the hydroalcoholic lacquers developed, and particularly those prepared with SLS, provide better nail penetration of the drugs ciclopirox olamine and clobetasol propionate. Results have shown that the increase of the drug penetration in the nail is caused by the formation of a porous random microstructure and by the decrease of the contact angle between lacquers and the surface or the nail plaque. The presence of SLS produces an improvement in the spreading of the solution on the nail surface and promotes the penetration of the solution into the nail pores. The hydroalcoholic lacquer, elaborated with cyclodextrin/poloxamer soluble polypseudorotaxane and sodium lauryl sulfate as an enhancer, allowed the rate of diffusion and penetration of the active ingredient within the nail to be significantly higher than obtained with the reference lacquers when using either ciclopirox olamine or clobetasol propionate as the active ingredient
2020-05-25T14:48:59Z
2020-05-25T14:48:59Z
2018
journal article
Cutrín-Gómez, E.; Anguiano-Igea, S.; Delgado-Charro, M.B.; Gómez-Amoza, J.L.; Otero-Espinar, F.J. Effect of Penetration Enhancers on Drug Nail Permeability from Cyclodextrin/Poloxamer-Soluble Polypseudorotaxane-Based Nail Lacquers. Pharmaceutics 2018, 10, 273
http://hdl.handle.net/10347/22546
10.3390/pharmaceutics10040273
1999-4923
eng
https://doi.org/10.3390/pharmaceutics10040273
http://creativecommons.org/licenses/by/4.0/
open access
© 2018 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/)
MDPI
oai:minerva.usc.es:10347/306712024-03-04T08:25:37Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Contact lenses that transform gold into nanoparticles for prophylaxis of light-related events and photothermal therapy
Álvarez Lorenzo, Carmen Isabel
Vivero López, María
Concheiro Nine, Ángel Joaquín
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Contact lenses
Gold nanoparticles
Silicone hydrogel
Photothermal therapy
Autoclave
Light-filter medical device
Anisotropic gold particles
This work describes for first time how anisotropic gold nanoparticles (AuNPs) can be spontaneously formed inside preformed contact lenses (CLs) avoiding the use of additional reductant agents (reagent-free) through a precise tunning of the monomeric composition, the saline concentration, and the application of steam heat sterilization. Protocols to generate AuNPs in solution using inorganic or small organic reductants are widely available. Differently, gold precursors interactions with polymer networks have been overlooked and, thus, the interest of chemically cross-linked hydrogels as organic reductants is still to be elucidated. In the ocular field, incorporation of AuNPs to CLs may expand their applications in prophylaxis, therapy and diagnosis. To carry out the work, a variety of hydrogels and commercially available CLs were incubated with gold salt solution without any other chemical reagent. AuNPs formation was monitored by changes in localized surface plasmon resonance (LSPR) bands and quantifying the gold sorbed. Only silicone hydrogels induced AuNPs formation at room temperature in few days; methacrylic acid red-shifted the LSPR band (550–600 nm), while monomers bearing F hindered the reduction. Storage of hydrogels in the gold precursor solution allowed a gradual formation of anisotropic AuNPs, which could be stopped at any time by washing the hydrogel with water. The developed CLs behave as efficient filters against highly penetrant light and also exhibit photoresponsiveness as demonstrated as rapid (10 s), focused mild hyperthermia when irradiated with green, red and NIR lasers
2023-06-14T07:25:02Z
2023-06-14T07:25:02Z
2023
journal article
International Journal of Pharmaceutics 641 (2023) 123048
http://hdl.handle.net/10347/30671
10.1016/j.ijpharm.2023.123048
0378-5173
eng
https://doi.org/10.1016/j.ijpharm.2023.123048
info:eu-repo/grantAgreement/AEI/Plan Estatal de Investigación Científica y Técnica y de Innovación 2017-2020/PID2020-113881RB-I00/ES
http://creativecommons.org/licenses/by-nc-nd/4.0/
open access
© 2023 The Author(s). Published by Elsevier B.V. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/bync-nd/4.0/)
Elsevier
oai:minerva.usc.es:10347/211492020-11-06T09:33:30Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Antioxidant and neuroprotective potential of the Brown Seaweed Bifurcaria bifurcata in an in vitro Parkinson’s disease model
Silva, Joana M.
Alves, Celso
Freitas, Rafaela
Martins, Alice
Pinteus, Susete
Ribeiro, Joana
Gaspar, Helena
Alfonso Rancaño, María Amparo
Pedrosa, Rui
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
6-hydroxydopamine
Seaweeds
SH-SY5Y cells
Neuroprotection
Mitochondrial membrane potential
Caspase-3 activity
Eleganolone
Eleganonal
Neurodegenerative diseases
Bifurcaria bifurcata is a marine brown seaweed mainly found on the Atlantic coast. Herein, we report the antioxidant and neuroprotective activities of seven fractions (F1–F7) obtained by normal phase chromatography from the B. bifurcata dichloromethane extract, as well as of its two major isolated diterpenes. Total phenolic content of fractions was determined by the Folin–Ciocalteu method, while antioxidant activity was evaluated by the DPPH, ORAC, and FRAP assays. Neuroprotective effects were evaluated in a neurotoxic model induced by 6-hydroxydopamine (6-OHDA) in a human neuroblastoma cell line (SH-SY5Y), while the mechanisms associated to neuroprotection were investigated by the determination of mitochondrial membrane potential, H2O2 production, Caspase-3 activity, and by observation of DNA fragmentation. Fractions F4 and F5 exhibited the best neuroprotective and antioxidant activities, respectively. F4 fraction prevented changes in mitochondrial potential, and induced a reduction of H2O2 levels production and an increase in cell viability, suggesting that it may contain multi-target compounds acting on different pathways. Hence, this fraction was subjected to purification steps, affording the known diterpenes eleganolone and eleganonal. Both compounds exhibited antioxidant potential, being interesting candidates for further neuroprotective studies
2020-04-03T16:46:48Z
2020-04-03T16:46:48Z
2019
journal article
Silva, J.; Alves, C.; Freitas, R.; Martins, A.; Pinteus, S.; Ribeiro, J.; Gaspar, H.; Alfonso, A.; Pedrosa, R. Antioxidant and Neuroprotective Potential of the Brown Seaweed Bifurcaria bifurcata in an in vitro Parkinson’s Disease Model. Mar. Drugs 2019, 17, 85
http://hdl.handle.net/10347/21149
10.3390/md17020085
1660-3397
eng
https://doi.org/10.3390/md17020085
open access
© 2019 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/)
MDPI
oai:minerva.usc.es:10347/321002024-02-01T14:02:49Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Influence of the surface properties of nanocapsules on their interaction with intestinal barriers
Santalices Ramos, Irene
Torres, Dolores
Lozano, María Victoria
Arroyo-Jiménez, María del Mar
Alonso, María José
Santander Ortega, Manuel J.
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Poloxamer
Chitosan
Polyarginine
Nanocarrier
Nanocapsule
Colloidal
Stability
Lipolysis
Mucoadhesion
Mucodiffusion,
Oral administration
Despite the convenience of the oral route for drug administration, the existence of
different physiological barriers associated with the intestinal tract greatly lowers the
bioavailability of many active compounds. We have previously suggested the potential
polymeric nanocapsules, consisting of an oily core surrounded by a polymer shell, as oral
drug delivery carriers. Here we present a systematic study of the influence of the surface
properties of these nanocapsules on their interaction with the intestinal barriers. Two
different surfactants, Pluronic®F68 (PF68) and F127 (PF127), and two polymeric shells,
chitosan (CS) and polyarginine (PARG) were chosen for the formulation of the
nanocapsules. We analyzed nine different combinations of these polymers and
surfactants, and studied the effect of each specific combination on their colloidal stability,
enzymatic degradation, and mucoadhesion/mucodiffusion. Our results indicate that both,
the polymer shell and the surfactants located at the oil/water interface, influence the
interaction of the nanocapsules with the intestinal barriers. More interestingly, according
to our observations, the shell components of the nanosystems may have either synergic
or disruptive effects on their capacity to overcome the intestinal barriers
2024-01-30T12:17:44Z
2024-01-30T12:17:44Z
2018
journal article
Irene Santalices, Dolores Torres, Mª Victoria Lozano, Mª Mar Arroyo-Jiménez, María José Alonso, Manuel J. Santander-Ortega, Influence of the surface properties of nanocapsules on their interaction with intestinal barriers, European Journal of Pharmaceutics and Biopharmaceutics, Volume 133, 2018, Pages 203-213
0939-6411
http://hdl.handle.net/10347/32100
10.1016/j.ejpb.2018.09.023
eng
https://doi.org/10.1016/j.ejpb.2018.09.02
FEDER Funds; Ref 2014/043
FPU program (No. FPU13/02015)
TRANS‐INT European Consortium −FP7, under grant agreement No. 281035
http://creativecommons.org/licenses/by-nc-nd/4.0/
open access
CC BY-NC-ND
Elsevier
oai:minerva.usc.es:10347/235912023-07-10T06:12:39Zcom_10347_2895com_10347_2890com_10347_2888com_10347_227com_10347_2904col_10347_12328col_10347_12265
Acute Cardiotoxicity Evaluation of the Marine Biotoxins OA, DTX-1 and YTX
Fernández Ferreiro, Sara
Carrera González, María Cristina
Vilariño del Río, Natalia
Louzao Ojeda, María Carmen
Santamarina Pernas, Germán
González Cantalapiedra, Antonio
Botana López, Luis Miguel
Universidade de Santiago de Compostela. Departamento de Ciencias Clínicas Veterinarias
Universidade de Santiago de Compostela. Departamento de Farmacoloxía
Okadaic acid
Dynophysistoxins
Yessotoxin
Cardiotoxicity
hERG
ECG
Cardiac biomarkers
Phycotoxins are marine toxins produced by phytoplankton that can get accumulated in filter feeding shellfish. Human intoxication episodes occur due to contaminated seafood consumption. Okadaic acid (OA) and dynophysistoxins (DTXs) are phycotoxins responsible for a severe gastrointestinal syndrome called diarrheic shellfish poisoning (DSP). Yessotoxins (YTXs) are marine toxins initially included in the DSP class but currently classified as a separated group. Food safety authorities from several countries have regulated the content of DSPs and YTXs in shellfish to protect human health. In mice, OA and YTX have been associated with ultrastructural heart damage in vivo. Therefore, this study explored the potential of OA, DTX-1 and YTX to cause acute heart toxicity. Cardiotoxicity was evaluated in vitro by measuring hERG (human èter-a-go-go gene) channel activity and in vivo using electrocardiogram (ECG) recordings and cardiac damage biomarkers. The results demonstrated that these toxins do not exert acute effects on hERG channel activity. Additionally, in vivo experiments showed that these compounds do not alter cardiac biomarkers and ECG in rats acutely. Despite the ultrastructural damage to the heart reported for these toxins, no acute alterations of heart function have been detected in vivo, suggesting a functional compensation in the short term
2020-11-06T11:52:08Z
2020-11-06T11:52:08Z
2015
journal article
Ferreiro, S.F.; Carrera, C.; Vilariño, N.; Louzao, M.C.; Santamarina, G.; Cantalapiedra, A.G.; Botana, L.M. Acute Cardiotoxicity Evaluation of the Marine Biotoxins OA, DTX-1 and YTX. Toxins 2015, 7, 1030-1047
http://hdl.handle.net/10347/23591
10.3390/toxins7041030
2072-6651
eng
https://doi.org/10.3390/toxins7041030
info:eu-repo/grantAgreement/EC/FP7/265409
info:eu-repo/grantAgreement/EC/FP7/315285
info:eu-repo/grantAgreement/EC/FP7/312184
http://creativecommons.org/licenses/by/4.0/
open access
© 2015 by the authors; licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/4.0/)
Atribución 4.0 Internacional
MDPI
oai:minerva.usc.es:10347/235922023-07-10T06:12:18Zcom_10347_2906com_10347_2890com_10347_2888com_10347_227com_10347_2904col_10347_15791col_10347_12265
Experimental Basis for the High Oral Toxicity of Dinophysistoxin 1: A Comparative Study of DSP
Fernández, Diego A.
Louzao Ojeda, María Carmen
Fraga, María
Vilariño del Río, Natalia
Rodríguez Vieytes, María Mercedes
Botana López, Luis Miguel
Universidade de Santiago de Compostela. Departamento de Farmacoloxía
Universidade de Santiago de Compostela. Departamento de Fisioloxía
Okadaic acid
Dinophysistoxin-1
Dinophysistoxin-2
Caco-2
Intestinal permeability
Trans-epithelial electric resistance
Occludin
Annexin V
Luminex
Immunoassay
Okadaic acid (OA) and its analogues, dinophysistoxin 1 (DTX1) and dinophysistoxin 2 (DTX2), are lipophilic and heat-stable marine toxins produced by dinoflagellates, which can accumulate in filter-feeding bivalves. These toxins cause diarrheic shellfish poisoning (DSP) in humans shortly after the ingestion of contaminated seafood. Studies carried out in mice indicated that DSP poisonous are toxic towards experimental animals with a lethal oral dose 2–10 times higher than the intraperitoneal (i.p.) lethal dose. The focus of this work was to study the absorption of OA, DTX1 and DTX2 through the human gut barrier using differentiated Caco-2 cells. Furthermore, we compared cytotoxicity parameters. Our data revealed that cellular viability was not compromised by toxin concentrations up to 1 μM for 72 h. Okadaic acid and DTX2 induced no significant damage; nevertheless, DTX1 was able to disrupt the integrity of Caco-2 monolayers at concentrations above 50 nM. In addition, confocal microscopy imaging confirmed that the tight-junction protein, occludin, was affected by DTX1. Permeability assays revealed that only DTX1 was able to significantly cross the intestinal epithelium at concentrations above 100 nM. These data suggest a higher oral toxicity of DTX1 compared to OA and DTX2
2020-11-06T11:53:30Z
2020-11-06T11:53:30Z
2014
journal article
Fernández, D.A.; Louzao, M.C.; Fraga, M.; Vilariño, N.; Vieytes, M.R.; Botana, L.M. Experimental Basis for the High Oral Toxicity of Dinophysistoxin 1: A Comparative Study of DSP. Toxins 2014, 6, 211-228
http://hdl.handle.net/10347/23592
10.3390/toxins6010211
2072-6651
eng
https://doi.org/10.3390/toxins6010211
info:eu-repo/grantAgreement/EC/FP7/211326
info:eu-repo/grantAgreement/EC/FP7/265896
info:eu-repo/grantAgreement/EC/FP7/265409
info:eu-repo/grantAgreement/EC/FP7/315285
info:eu-repo/grantAgreement/EC/FP7/312184
info:eu-repo/grantAgreement/MICINN/Plan Nacional de I+D+i 2008-2011/AGL2009-13581-C02-01/ES/Evaluacion De Los Riesgos De Salud Publica Debidos A Toxinas Marinas De Aguas Templadas En Las Costas Europeas Y Del Efecto Sinergico Con Otras Toxinas Habituales En Estas Latitudes. Subproyecto 2
http://creativecommons.org/licenses/by/3.0/
open access
© 2014 by the authors; licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/)
MDPI
oai:minerva.usc.es:10347/161312023-07-10T06:12:40Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Evaluation of the impact of mild steaming and heat treatment on the concentration of okadaic acid, dinophysistoxin-2 and dinophysistoxin-3 in mussels
Rodríguez Filgueiras, Inés
Alfonso Rancaño, María Amparo
Antelo Queijo, Álvaro
Álvarez, Mercedes
Botana López, Luis Miguel
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Steaming
Okadaic acid
Mass spectrometry
Dinophysistoxin
This study explores the effect of laboratory and industrial steaming on mussels with toxin
concentrations above and below the legal limit. We used mild conditions for steaming, 100 ˝C for 5 min in industrial processing, and up to 20 min in small-scale laboratory steaming. Also, we studied the effect of heat on the toxin concentration of mussels obtained from two different locations and the effect of heat on the levels of dinophysistoxins 3 (DTX3) in both the mussel matrix and in pure form (7-O-palmitoyl okadaic ester and 7-O-palmytoleyl okadaic ester). The results show that the loss of water due to steaming was very small with a maximum of 9.5%, that the toxin content remained unchanged with no concentration effect or increase in toxicity, and that dinophysistoxins 3 was hydrolyzed or degraded to a certain extent under heat treatment. The use of liquid-certified matrix showed a 55% decrease of dinophysistoxins 3 after 10 min steaming, and a 50% reduction in total toxicity after treatment with an autoclave (121 ˝C for 20 min)
2017-11-10T13:50:34Z
2017-11-10T13:50:34Z
2016-06
journal article
Rodríguez, I., Alfonso, A., Antelo, A., Alvarez, M., & Botana, L. M. (2016). Evaluation of the impact of mild steaming and heat treatment on the concentration of okadaic acid, dinophysistoxin-2 and dinophysistoxin-3 in mussels. Toxins, 8(6), 175.
2072-6651
http://hdl.handle.net/10347/16131
10.3390/toxins8060175
eng
http://doi.org/10.3390/toxins8060175
info:eu-repo/grantAgreement/EC/FP7/312184
info:eu-repo/grantAgreement/MINECO/Plan Estatal de Investigación Científica y Técnica y de Innovación 2013-2016/AGL2014-58210-R/ES/EVALUACION DE LA SEGURIDAD ALIMENTARIA DE PRODUCTOS PESQUEROS ASOCIADA A LA PRESENCIA DE TOXINAS MARINAS DE NUEVA APARICION EN AGUAS EUROPEAS
open access
Copyright by the authors; licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC-BY) license (http://creativecommons.org/licenses/by/4.0/
MDPI
oai:minerva.usc.es:10347/216112020-04-22T02:01:28Zcom_10347_2989com_10347_2889com_10347_227com_10347_2904com_10347_2890com_10347_2888col_10347_9764col_10347_12265
Natural and cross-inducible anti-SIV antibodies in Mauritian cynomolgus macaques
Li, Hongzhao
Nykoluk, Mikaela
Li, Lin
Liu, Lewis R.
Omange, Robert W.
Soule, Geoff
Schroeder, Lukas T.
Toledo, Nikki
Kashem, Mohammad Abul
Correia Pinto, Jorge F.
Liang, Binhua
Schultz-Darken, Nancy
Alonso Fernández, María José
Whitney, James B.
Plummer, Francis A.
Luo, Ma
Universidade de Santiago de Compostela. Centro de Investigación en Medicina Molecular e Enfermidades Crónicas
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Cynomolgus macaques are an increasingly important nonhuman primate model for HIV vaccine research. SIV-free animals without pre-existing anti-SIV immune responses are generally needed to evaluate the effect of vaccine-induced immune responses against the vaccine epitopes. Here, in order to select such animals for vaccine studies, we screened 108 naïve female Mauritian cynomolgus macaques for natural (baseline) antibodies to SIV antigens using a Bio-Plex multiplex system. The antigens included twelve 20mer peptides overlapping the twelve SIV protease cleavage sites (-10/+10), respectively (PCS peptides), and three non-PCS Gag or Env peptides. Natural antibodies to SIV antigens were detected in subsets of monkeys. The antibody reactivity to SIV was further confirmed by Western blot using purified recombinant SIV Gag and Env proteins. As expected, the immunization of monkeys with PCS antigens elicited anti-PCS antibodies. However, unexpectedly, antibodies to non-PCS peptides were also induced, as shown by both Bio-Plex and Western blot analyses, while the non-PCS peptides do not share sequence homology with PCS peptides. The presence of natural and vaccine cross-inducible SIV antibodies in Mauritian cynomolgus macaques should be considered in animal selection, experimental design and result interpretation, for their best use in HIV vaccine research
2020-04-21T20:20:20Z
2020-04-21T20:20:20Z
2017
journal article
Li H, Nykoluk M, Li L, Liu LR, Omange RW, Soule G, et al. (2017) Natural and cross-inducible anti-SIV antibodies in Mauritian cynomolgus macaques. PLoS ONE 12(10): e0186079. https://doi.org/10.1371/journal.pone.0186079
http://hdl.handle.net/10347/21611
10.1371/journal.pone.0186079
1932-6203
eng
https://doi.org/10.1371/journal.pone.0186079
http://creativecommons.org/licenses/by/4.0/
open access
© 2017 Li et al. This is an open access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited
Atribución 4.0 Internacional
PLOS
oai:minerva.usc.es:10347/267302022-04-01T08:05:24Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Targeting joint inflammation for osteoarthritis management through stimulus-sensitive hyaluronic acid based intra-articular hydrogels
Díaz Rodríguez, Patricia
Mariño Lijó, Cibrán
Vázquez, José Antonio
Caeiro Rey, José Ramón
Landín Pérez, Mariana
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Hyaluronic acid
Intra-articular hydrogels
Thermo-sensitive systems
Anti-inflammatory activity
Osteoarthritis
Numerous therapeutic strategies have been developed for osteoarthritis (OA) management, including intra-articular (IA) injections. The ideal IA formulation should control cartilage degradation and restore synovial fluid viscosity. To this end, we propose to combine thermo-sensitive polymers (poloxamers) with hyaluronic acid (HA) to develop suitable beta-lapachone (βLap) loaded IA formulations. The development of IA formulations with these components entails several difficulties: low βLap solubility, unknown βLap therapeutic dose and the bonded commitment of easy administration and viscosupplementation. An optimized formulation was designed using artificial intelligence tools based on the experimental results of a wide variety of hydrogels and its therapeutic capacity was evaluated on an ex vivo OA model. The formulation presented excellent rheological properties and significantly decreased the secretion of degradative (MMP13) and pro-inflammatory (CXCL8) molecules. Therefore, the developed formulation is a promising candidate for OA treatment restoring the synovial fluid rheological properties while decreasing inflammation and cartilage degradation
2021-08-09T12:30:48Z
2021-08-09T12:30:48Z
2021
journal article
Materials Science and Engineering: C 2021, 128: 112254. https://doi.org/10.1016/j.msec.2021.112254
0928-4931
http://hdl.handle.net/10347/26730
10.1016/j.msec.2021.112254
eng
https://doi.org/10.1016/j.msec.2021.112254
http://creativecommons.org/licenses/by-nc-nd/4.0/
open access
© 2021 The Author(s). Published by Elsevier B.V. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/)
Attribution-NonCommercial-NoDerivatives 4.0 Internacional
Elsevier
oai:minerva.usc.es:10347/262602021-05-22T02:04:51Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Targeting Multiple Signal Transduction Pathways of SARS-CoV-2: Approaches to COVID-19 Therapeutic Candidates
Fakhri, Sajad
Nouri, Zeinab
Moradi, Seyed Zachariah
Küpeli Akkol, Esra
Piri, Sana
Sobarzo Sánchez, Eduardo Marcelo
Farzaei, Mohammad Hosein
Echeverría, Javier
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Coronavirus
SARS-CoV-2
COVID-19
Signaling pathway
Inflammation
Oxidative stress
Apoptosis
Autophagy
Natural products
Due to the complicated pathogenic pathways of coronavirus disease 2019 (COVID-19), related medicinal therapies have remained a clinical challenge. COVID-19 highlights the urgent need to develop mechanistic pathogenic pathways and effective agents for preventing/treating future epidemics. As a result, the destructive pathways of COVID-19 are in the line with clinical symptoms induced by severe acute coronary syndrome (SARS), including lung failure and pneumonia. Accordingly, revealing the exact signaling pathways, including inflammation, oxidative stress, apoptosis, and autophagy, as well as relative representative mediators such as tumor necrosis factor-α (TNF-α), nuclear factor erythroid 2-related factor 2 (Nrf2), Bax/caspases, and Beclin/LC3, respectively, will pave the road for combating COVID-19. Prevailing host factors and multiple steps of SARS-CoV-2 attachment/entry, replication, and assembly/release would be hopeful strategies against COVID-19. This is a comprehensive review of the destructive signaling pathways and host–pathogen interaction of SARS-CoV-2, as well as related therapeutic targets and treatment strategies, including potential natural products-based candidates
2021-05-21T13:14:26Z
2021-05-21T13:14:26Z
2021
journal article
Molecules 2021, 26(10), 2917; https://doi.org/10.3390/molecules26102917
http://hdl.handle.net/10347/26260
10.3390/molecules26102917
1420-3049
eng
https://doi.org/10.3390/molecules26102917
http://creativecommons.org/licenses/by/4.0/
open access
© 2021 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/)
Atribución 4.0 Internacional
MDPI
oai:minerva.usc.es:10347/322582024-02-05T10:11:14Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Novel coumarin-pyridazine hybrids as selective MAO-B inhibitors for the Parkinson’s disease therapy
Rodríguez Enríquez, Fernanda
Costas Lago, María
Besada, Pedro
Alonso-Pena, Miguel
Torres-Terán, Iria
Viña, Dolores
Fontenla, Jose A.
Sturlese, Mattia
Moro, Stefano
Quezada, Elías
Terán, Carmen
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Coumarin-Pyridazine hybrids
MAO-B
Parkinson´s disease
In vivo study
SAR study
The 3-pyridazinylcoumarin scaffold was previously reported as an efficient core for the discovery of reversible and selective inhibitors of MAO-B, a validated drug target for PD therapy which also plays an important role in the AD progress. Looking for its structural optimization, novel compounds of hybrid structure coumarin-pyridazine, differing in polarizability and lipophilicity properties, were synthesized and tested against the two MAO
isoforms, MAO-A and MAO-B (compounds 17a-f and 18a-f).
All the designed compounds selectively inhibited the MAO-B isoenzyme, exhibiting many of them IC50 values ranging from sub-micromolar to nanomolar grade and lacking neuronal toxicity. The 7-bromo-3-(6-bromopyridazin-3-yl)coumarin (18c), the most potent compound of these series (IC50 = 60 nM), was subjected to further in vivo studies in a reserpine-induced mouse PD model. The obtained results suggest a promising potential for 18c as antiparkinsonian agent.
Molecular modeling studies also provided valuable information about the enzyme-drug interactions and the potential pharmacokinetic profile of the novel compounds.
2024-02-02T12:34:14Z
2024-02-02T12:34:14Z
2020
journal article
Bioorganic Chemistry 104 (2020) 104203
0045-2068
http://hdl.handle.net/10347/32258
j.bioorg.2020.104203
1090-2120
eng
https://doi.org/10.1016/j.bioorg.2020.104203
open access
CC BY-NC-ND
Elsevier Inc.
oai:minerva.usc.es:10347/217592020-04-26T02:01:03Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Novel Hyaluronic Acid-Chitosan Nanoparticles for Ocular Gene Therapy
Fuente Freire, María de la
Seijo Rey, María Begoña
Alonso Fernández, María José
Universidade de Santiago de Compostela. Departamento de Farmacia e Tecnoloxía Farmacéutica
purpose. Gene therapy offers a promising alternative for the treatment of ocular diseases. However, the implementation of this type of therapy is actually hampered by the lack of an efficient ocular gene delivery carrier. The main objective of the present work was to assess the effectiveness and investigate the mechanism of action of a new type of nanoparticle made of two bioadhesive polysaccharides, hyaluronic acid (HA) and chitosan (CS), intended for the delivery of genes to the cornea and conjunctiva.
methods. The nanoparticles were obtained by a very mild ionotropic gelation technique. They were loaded with either the model plasmid pEGFP or pβ-gal. Transfection and toxicological studies were conducted in human corneal epithelial (HCE) and normal human conjunctival (IOBA-NHC) cell lines. The mechanism of internalization of the nanoparticles by the corneal and conjunctival cells was investigated by using fluorescence confocal microscopy.
results. The nanoparticles had a size in the range of 100 to 235 nm and a ζ-potential of −30 to +28 mV. The results of the transfection studies showed that HA-CS nanoparticles were able to provide high transfection levels (up to 15% of cells transfected), without affecting cell viability. The confocal images indicated that HA-CS nanoparticles were internalized by fluid endocytosis and that this endocytic process was mediated by the hyaluronan receptor CD44.
conclusions. The results give evidence of the potential of HA-CS nanoparticles for the targeting and further transfer of genes to the ocular surface
2020-04-25T17:32:12Z
2020-04-25T17:32:12Z
2008
journal article
Investigative Ophthalmology & Visual Science May 2008, Vol.49, 2016-2024. doi:https://doi.org/10.1167/iovs.07-1077
0146-0404
http://hdl.handle.net/10347/21759
10.1167/iovs.07-1077
1552-5783
eng
https://doi.org/10.1167/iovs.07-1077
open access
Copyright © Association for Research in Vision and Ophthalmology
Arvo Journals
oai:minerva.usc.es:10347/312022024-02-23T13:39:40Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Supercritical fluid (SCF)-assisted preparation of cyclodextrin-based poly(pseudo)rotaxanes for transdermal purposes
Cardoso, Gleidson
García González, Carlos Alberto
Santos-Rosales, Víctor
Taveira, Stephania Fleury
Cunha-Filho, Marcilio
Concheiro Nine, Ángel Joaquín
Álvarez Lorenzo, Carmen Isabel
Marreto, Ricardo Neves
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Cyclodextrin
Permeation enhancer
Solid dispersion
Microstructure
This study aims to investigate the effect of the preparation of solid dispersions using supercritical CO2 (scCO2) on the physicochemical properties and the performance of supramolecular gels based on polymer-cyclodextrin (CD) interactions (named poly(pseudo)rotaxanes, PPR) envisaging a transdermal administration. Solid dispersions containing Soluplus®, the antihypertensive drug carvedilol (CAR), and CD (αCD or HPβCD) were prepared and characterized by HPLC, XRPD, FTIR, and DSC. PPRs prepared from solid dispersions (SCF gels) and the corresponding physical mixtures (PM gels) were analyzed regarding rheology, morphology, in vitro drug diffusion, and ex vivo drug skin permeation. The application of scCO2 led to the loss of the crystalline lattice of CAR while preserving its chemical identity. On the contrary, αCD crystals were still present in the SCF solid dispersions. SCF gels were more uniform than their corresponding PM, and the supercritical treatment resulted in changes in the rheological behavior, reducing the viscosity. CAR in vitro diffusion was significantly higher (p < 0.05) for the αCD-based SCF gel than its corresponding PM gel. Drug skin permeation showed a significant increase in drug flux from CD-based SCF gels (containing αCD or HPβCD) compared to corresponding PM gels. Additionally, the pretreatment of the skin with αCD exhibited increased CAR permeation, suggesting an interaction between αCD and the skin membrane. Results evidenced that SCF processing decisively modified the properties of the supramolecular gels, particularly those prepared with αCD
2023-11-07T13:01:52Z
2023-11-07T13:01:52Z
2023-08-09
journal article
Drug Deliv. and Transl. Res. (2023)
2190-393X
http://hdl.handle.net/10347/31202
10.1007/s13346-023-01385-w
2190-3948
eng
https://doi.org/10.1007/s13346-023-01385-w
info:eu-repo/grantAgreement/AEI/Plan Estatal de Investigación Científica y Técnica y de Innovación 2017-2020/PID2020-113881RB-I00/ES/ARQUITECTURAS 5D PARA MEDICINA REGENERATIVA Y TERAPIA LOCALIZADA/
http://creativecommons.org/licenses/by/4.0/
open access
© The Author(s) 2023. This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons licence, and indicate if changes were made
Atribución 4.0 Internacional
Springer
oai:minerva.usc.es:10347/267602023-07-10T06:11:33Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Cyclophilins A, B, and C Role in Human T Lymphocytes Upon Inflammatory Conditions
Gegunde Mosquera, Sandra
Alfonso Rancaño, María Amparo
Alvariño Romero, Rebeca
Alonso López, Eva
Botana López, Luis Miguel
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Cyclophilin
Inflammation
Cyclophilin A inhibitors
CD147 receptor
T lymphocyte
Migration
Cyclophilins (Cyps) are a group of peptidyl-prolyl cis/trans isomerases that play crucial roles in regulatory mechanisms of cellular physiology and pathology in several inflammatory conditions. Their receptor, CD147, also participates in the development and progression of the inflammatory response. Nevertheless, the main function of Cyps and their receptor are yet to be deciphered. The release of CypA and the expression of the CD147 receptor in activated T lymphocytes were already described, however, no data are available about other Cyps in these cells. Therefore, in the present work intra and extracellular CypA, B and C levels were measured followed by induced inflammatory conditions. After activation of T lymphocytes by incubation with concanavalin A, both intra and extracellular Cyps levels and the CD147 membrane receptor expression were increased leading to cell migration towards circulating CypA and CypB as chemoattractants. When CypA was modulated by natural and synthetic compounds, the inflammatory cascade was avoided including T cell migration. Our results strengthen the relationship between CypA, B, and C, their receptor, and the inflammatory process in human T lymphocytes, associating CypC with these cells for the first time
2021-08-10T12:49:10Z
2021-08-10T12:49:10Z
2021
journal article
Front. Immunol. 2021, 12:609196. doi: 10.3389/fimmu.2021.609196
http://hdl.handle.net/10347/26760
10.3389/fimmu.2021.609196
1664-3224
eng
https://doi.org/10.3389/fimmu.2021.609196
info:eu-repo/grantAgreement/EC/H2020/778069
http://creativecommons.org/licenses/by/4.0/
open access
Copyright © 2021 Gegunde, Alfonso, Alvariño, Alonso and Botana. This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.
Atribución 4.0 Internacional
Frontiers Media
oai:minerva.usc.es:10347/211472020-04-05T14:22:40Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Current Stage of Marine Ceramic Grafts for 3D Bone Tissue Regeneration
Díaz Rodríguez, Patricia
López Álvarez, Miriam
Serra, Julia
González, Pío
Landín Pérez, Mariana
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Marine ceramic grafts
Calcium phosphate
Bone tissue regeneration
Osteoinductive properties
Structural strength
Dissolution rate
Bioceramic scaffolds are crucial in tissue engineering for bone regeneration. They usually
provide hierarchical porosity, bioactivity, and mechanical support supplying osteoconductive properties
and allowing for 3D cell culture. In the case of age-related diseases such as osteoarthritis and
osteoporosis, or other bone alterations as alveolar bone resorption or spinal fractures, functional
tissue recovery usually requires the use of grafts. These bone grafts or bone void fillers are usually
based on porous calcium phosphate grains which, once disposed into the bone defect, act as
scaffolds by incorporating, to their own porosity, the intergranular one. Despite their routine use
in traumatology and dental applications, specific graft requirements such as osteoinductivity or
balanced dissolution rate are still not completely fulfilled. Marine origin bioceramics research opens
the possibility to find new sources of bone grafts given the wide diversity of marine materials still
largely unexplored. The interest in this field has also been urged by the limitations of synthetic
or mammalian-derived grafts already in use and broadly investigated. The present review covers
the current stage of major marine origin bioceramic grafts for bone tissue regeneration and their
promising properties. Both products already available on the market and those in preclinical phases
are included. To understand their clear contribution to the field, the main clinical requirements and
the current available biological-derived ceramic grafts with their advantages and limitations have
been collected.
2020-04-03T16:35:19Z
2020-04-03T16:35:19Z
2019
journal article
Diaz-Rodriguez, P.; López-Álvarez, M.; Serra, J.; González, P.; Landín, M. Current Stage of Marine Ceramic Grafts for 3D Bone Tissue Regeneration. Mar. Drugs 2019, 17, 471
http://hdl.handle.net/10347/21147
10.3390/md17080471
1660-3397
eng
https://doi.org/10.3390/md17080471
open access
© 2019 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/)
MDPI
oai:minerva.usc.es:10347/225472020-05-26T02:00:45Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Polyurethanes as new excipients in nail therapeutics
Gregorí Valdes, Barbara S.
Serro, Ana Paula
Marto, Joana
Santos, Rui Galhano dos
Cutrín Gómez, Elena
Otero Espinar, Francisco Javier
Bordado, João Moura
Ribeiro, Helena Margarida
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Nail lacquers
Polyurethane
Onychomycosis
Topical treatment
Terbinafine hydrochloride
Ciclopirox olamine
Onychomycosis affects about 15% of the population. This disease causes physical and psychosocial discomfort to infected patients. Topical treatment (creams, solutions, gels, colloidal carriers, and nail lacquers) is usually the most commonly required due to the high toxicity of oral drugs. Currently, the most common topical formulations (creams and lotions) present a low drug delivery to the nail infection. Nail lacquers appear to increase drug delivery and simultaneously improve the effectiveness of treatment with increased patient compliance. These formulations leave a polymer film on the nail plate after solvent evaporation. The duration of the film residence in the nail constitutes an important property of nail lacquer formulation. In this study, a polyurethane polymer was used to delivery antifungals drugs, such as terbinafine hydrochloride (TH) and ciclopirox olamine (CPX) and the influence of its concentration on the properties of nail lacquer formulations was assessed. The nail lacquer containing the lowest polymer concentration (10%) was the most effective regarding the in vitro release, permeation, and antifungal activity. It has also been demonstrated that the application of PU-based nail lacquer improves the nail plate, making it smooth and uniform and reduces the porosity contributing to the greater effectiveness of these vehicles. To conclude, the use of polyurethane in nail formulations is promising for nail therapeutics
2020-05-25T14:54:15Z
2020-05-25T14:54:15Z
2018
journal article
Valdes, B.S.G.; Serro, A.P.; Marto, J.; Galhano dos Santos, R.; Cutrín Gómez, E.; Otero-Espinar, F.J.; Moura Bordado, J.; Margarida Ribeiro, H. Polyurethanes as New Excipients in Nail Therapeutics. Pharmaceutics 2018, 10, 276
http://hdl.handle.net/10347/22547
10.3390/pharmaceutics10040276
1999-4923
eng
https://doi.org/10.3390/pharmaceutics10040276
http://creativecommons.org/licenses/by/4.0/
open access
© 2018 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/)
MDPI
oai:minerva.usc.es:10347/236312020-11-11T03:00:27Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Screening of Bacterial Quorum Sensing Inhibitors in a Vibrio fischeri LuxR-Based Synthetic Fluorescent E. coli Biosensor
Qin, Xiaofei
Vila Sanjurjo, Celina
Singh, Ratna
Philipp, Bodo
Goycoolea, Francisco M.
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Compounds screening
Quorum sensing inhibition
Antibacterial
Molecular docking
A library of 23 pure compounds of varying structural and chemical characteristics was screened for their quorum sensing (QS) inhibition activity using a synthetic fluorescent Escherichia coli biosensor that incorporates a modified version of lux regulon of Vibrio fischeri. Four such compounds exhibited QS inhibition activity without compromising bacterial growth, namely, phenazine carboxylic acid (PCA), 2-heptyl-3-hydroxy-4-quinolone (PQS), 1H-2-methyl-4-quinolone (MOQ) and genipin. When applied at 50 µM, these compounds reduced the QS response of the biosensor to 33.7% ± 2.6%, 43.1% ± 2.7%, 62.2% ± 6.3% and 43.3% ± 1.2%, respectively. A series of compounds only showed activity when tested at higher concentrations. This was the case of caffeine, which, when applied at 1 mM, reduced the QS to 47% ± 4.2%. In turn, capsaicin, caffeic acid phenethyl ester (CAPE), furanone and polygodial exhibited antibacterial activity when applied at 1mM, and reduced the bacterial growth by 12.8% ± 10.1%, 24.4% ± 7.0%, 91.4% ± 7.4% and 97.5% ± 3.8%, respectively. Similarly, we confirmed that trans-cinnamaldehyde and vanillin, when tested at 1 mM, reduced the QS response to 68.3% ± 4.9% and 27.1% ± 7.4%, respectively, though at the expense of concomitantly reducing cell growth by 18.6% ± 2.5% and 16% ± 2.2%, respectively. Two QS natural compounds of Pseudomonas aeruginosa, namely PQS and PCA, and the related, synthetic compounds MOQ, 1H-3-hydroxyl-4-quinolone (HOQ) and 1H-2-methyl-3-hydroxyl-4-quinolone (MHOQ) were used in molecular docking studies with the binding domain of the QS receptor TraR as a target. We offer here a general interpretation of structure-function relationships in this class of compounds that underpins their potential application as alternatives to antibiotics in controlling bacterial virulence
2020-11-10T11:07:07Z
2020-11-10T11:07:07Z
2020
journal article
Qin, X.; Vila-Sanjurjo, C.; Singh, R.; Philipp, B.; Goycoolea, F.M. Screening of Bacterial Quorum Sensing Inhibitors in a Vibrio fischeri LuxR-Based Synthetic Fluorescent E. coli Biosensor. Pharmaceuticals 2020, 13, 263
http://hdl.handle.net/10347/23631
10.3390/ph13090263
1424-8247
eng
https://doi.org/10.3390/ph13090263
http://creativecommons.org/licenses/by/4.0/
open access
© 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/)
Atribución 4.0 Internacional
MDPI
oai:minerva.usc.es:10347/236152020-11-10T03:01:10Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Transungual Delivery, Anti-Inflammatory Activity, and In Vivo Assessment of a Cyclodextrin Polypseudorotaxanes Nail Lacquer
Fernández Campos, Francisco
Navarro, Francesc
Corrales, Adrian
Picas, Jordi
Pena, Eloy
González, Jordi
Otero Espinar, Francisco Javier
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Nail lacquers
Cyclodextrins
Methylsulfonylmethane
Active penetration
Biotin
A new cyclodextrin polypseudorotaxanes nail lacquer (Regenail®) containing biotin, methyl sulphonyl methane (MSM), and dimethylsilanediol salicylate was developed and evaluated in vitro and in vivo. The product was developed to improve nail status and diminish signs of pathological nail alterations. A reference product (Betalfatrus®) was used for comparative purposes. An in vitro permeation experiment in hooves showed high MSM and biotin absorption. The content of sulfur and silicon in hooves was also found to be higher compared with the reference product. MSM was tested in human keratinocytes, exhibiting a good cytotoxicity profile and anti-inflammatory activity by the reduction in IL-8 and TNF-α under LPS stimuli. A clinical study was performed to check product safety and efficacy against nail brittleness and alterations such as Beau’s lines and onychorrhexis. A reduction in both alterations and in surface roughness without alteration of nail structure was observed, with a good level of patient acceptance and satisfaction
2020-11-09T09:42:40Z
2020-11-09T09:42:40Z
2020
journal article
Fernández-Campos, F.; Navarro, F.; Corrales, A.; Picas, J.; Pena, E.; González, J.; Otero-Espinar, F.J. Transungual Delivery, Anti-Inflammatory Activity, and In Vivo Assessment of a Cyclodextrin Polypseudorotaxanes Nail Lacquer. Pharmaceutics 2020, 12, 730
http://hdl.handle.net/10347/23615
10.3390/pharmaceutics12080730
1999-4923
eng
https://doi.org/10.3390/pharmaceutics12080730
http://creativecommons.org/licenses/by/4.0/
open access
© 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/)
Atribución 4.0 Internacional
MDPI
oai:minerva.usc.es:10347/267472023-07-10T06:11:42Zcom_10347_2919com_10347_2891com_10347_2888com_10347_227com_10347_2921com_10347_2904com_10347_2890col_10347_10699col_10347_15784col_10347_12265
Hybrid Methacrylated Gelatin and Hyaluronic Acid Hydrogel Scaffolds. Preparation and Systematic Characterization for Prospective Tissue Engineering Applications
Velasco Rodríguez, Brenda
Diaz Vidal, Tania
Rosales Rivera, Luis Carlos
García González, Carlos Alberto
Álvarez Lorenzo, Carmen Isabel
Al-Modlej, Abeer
Domínguez Arca, Vicente
Prieto Estévez, Gerardo
Barbosa Fernández, Silvia
Soltero Martinez, José Félix Armando
Taboada Antelo, Pablo
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Universidade de Santiago de Compostela. Departamento de Física Aplicada
Universidade de Santiago de Compostela. Departamento de Física de Partículas
Gelatin
Hyaluronic acid
Hydrogel
Hybrid scaffolds
Tissue engineering
Porosity
Hyaluronic acid (HA) and gelatin (Gel) are major components of the extracellular matrix of different tissues, and thus are largely appealing for the construction of hybrid hydrogels to combine the favorable characteristics of each biopolymer, such as the gel adhesiveness of Gel and the better mechanical strength of HA, respectively. However, despite previous studies conducted so far, the relationship between composition and scaffold structure and physico-chemical properties has not been completely and systematically established. In this work, pure and hybrid hydrogels of methacroyl-modified HA (HAMA) and Gel (GelMA) were prepared by UV photopolymerization and an extensive characterization was done to elucidate such correlations. Methacrylation degrees of ca. 40% and 11% for GelMA and HAMA, respectively, were obtained, which allows to improve the hydrogels’ mechanical properties. Hybrid GelMA/HAMA hydrogels were stiffer, with elastic modulus up to ca. 30 kPa, and porous (up to 91%) compared with pure GelMA ones at similar GelMA concentrations thanks to the interaction between HAMA and GelMA chains in the polymeric matrix. The progressive presence of HAMA gave rise to scaffolds with more disorganized, stiffer, and less porous structures owing to the net increase of mass in the hydrogel compositions. HAMA also made hybrid hydrogels more swellable and resistant to collagenase biodegradation. Hence, the suitable choice of polymeric composition allows to regulate the hydrogels´ physical properties to look for the most optimal characteristics required for the intended tissue engineering application
2021-08-10T12:43:26Z
2021-08-10T12:43:26Z
2021
journal article
Int. J. Mol. Sci. 2021, 22(13), 6758; https://doi.org/10.3390/ijms22136758
http://hdl.handle.net/10347/26747
10.3390/ijms22136758
1422-0067
eng
https://doi.org/10.3390/ijms22136758
info:eu-repo/grantAgreement/MINECO/Plan Estatal de Investigación Científica y Técnica y de Innovación 2013-2016/MAT2016-80266-R/ES
info:eu-repo/grantAgreement/AEI/Plan Estatal de Investigación Científica y Técnica y de Innovación 2017-2020/PID2019-109517RB-I00/ES/NUEVOS NANOTRANSPORTADORES BIOMIMETICOS YPLATAFORMAS IN VITRO PARA LA VALIDACION EXITOSA DE LA TERAGNOSTICA PARA LA ATEROSCLEROSIS
http://creativecommons.org/licenses/by/4.0/
open access
© 2021 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/)
Atribución 4.0 Internacional
MDPI
oai:minerva.usc.es:10347/211452023-07-10T06:18:20Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227com_10347_2912col_10347_12265col_10347_13405
Pharmacokinetics of Intravitreal Anti-VEGF Drugs in Age-Related Macular Degeneration
García Quintanilla, Laura
Luaces Rodríguez, Andrea
Gil Martínez, María
Mondelo García, Cristina
Maroñas Amigo, Olalla
Mangas Sanjuán, Víctor
González Barcia, Miguel
Zarra Ferro, Irene
Aguiar Fernández, Pablo
Otero Espinar, Francisco Javier
Fernández Ferreiro, Anxo
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Universidade de Santiago de Compostela. Departamento de Psiquiatría, Radioloxía, Saúde Pública, Enfermaría e Medicina
Vascular endothelial growth factor/antagonists & inhibitors
Ranibizumab
Aflibercept
Bevacizumab
Age-Related Macular Degeneration
Pharmacokinetics
Intravitreal
Intravitreal administration of anti-vascular endothelial growth factor (VEGF) antibodies
has become the standard treatment for Age-Related Macular Degeneration; however, the knowledge
of their pharmacokinetics is limited. A comprehensive review of the preclinical and clinical
pharmacokinetic data that were obtained in different studies with intravitreal bevacizumab,
ranibizumab, and aflibercept has been conducted. Moreover, the factors that can influence the
vitreous pharmacokinetics of these drugs, as well as the methods that were used in the studies
for analytical determination, have been exposed. These anti-VEGF drugs present different charge
and molecular weights, which play an important role in vitreous distribution and elimination.
The pharmacokinetic parameters that were collected differ depending on the species that were
involved in the studies and on physiological and pathological conditions, such as vitrectomy and
lensectomy. Knowledge of the intravitreal pharmacokinetics of the anti-VEGF drugs that were used
in clinical practice is of vital importance.
2020-04-03T16:23:24Z
2020-04-03T16:23:24Z
2019
journal article
García-Quintanilla, L.; Luaces-Rodríguez, A.; Gil-Martínez, M.; Mondelo-García, C.; Maroñas, O.; Mangas-Sanjuan, V.; González-Barcia, M.; Zarra-Ferro, I.; Aguiar, P.; Otero-Espinar, F.J.; Fernández-Ferreiro, A. Pharmacokinetics of Intravitreal Anti-VEGF Drugs in Age-Related Macular Degeneration. Pharmaceutics 2019, 11, 365
http://hdl.handle.net/10347/21145
10.3390/pharmaceutics11080365
1999-4923
eng
https://doi.org/10.3390/pharmaceutics11080365
info:eu-repo/grantAgreement/AEI/Plan Estatal de Investigación Científica y Técnica y de Innovación 2017-2020/RTI2018-099597-B-100/ES
open access
© 2019 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/)
MDPI
oai:minerva.usc.es:10347/238152023-07-10T06:21:43Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Micelles of Progesterone for Topical Eye Administration: Interspecies and Intertissues Differences in Ex Vivo Ocular Permeability
Alambiaga Caravaca, Adrián M.
Calatayud Pascual, María Aracely
Rodilla, Vicent
Concheiro Nine, Ángel Joaquín
López Castellano, Alicia
Álvarez Lorenzo, Carmen Isabel
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Progesterone
Retinitis pigmentosa
Interspecies ocular permeability differences
Polymeric micelles
Soluplus
Pluronic
Ocular drug delivery
Solubility
Hen’s egg-chorioallantoic membrane test (HET-CAM) assay
Progesterone (PG) may provide protection to the retina during retinitis pigmentosa, but its topical ocular supply is hampered by PG poor aqueous solubility and low ocular bioavailability. The development of efficient topical ocular forms must face up to two relevant challenges: Protective barriers of the eyes and lack of validated ex vivo tests to predict drug permeability. The aims of this study were: (i) To design micelles using Pluronic F68 and Soluplus copolymers to overcome PG solubility and permeability; and (ii) to compare drug diffusion through the cornea and sclera of three animal species (rabbit, porcine, and bovine) to investigate interspecies differences. Micelles of Pluronic F68 (3–4 nm) and Soluplus (52–59 nm) increased PG solubility by one and two orders of magnitude, respectively and exhibited nearly a 100% encapsulation efficiency. Soluplus systems showed in situ gelling capability in contrast to the low viscosity Pluronic F68 micelles. The formulations successfully passed the hen’s egg-chorioallantoic membrane test (HET-CAM) test. PG penetration through rabbit cornea and sclera was faster than through porcine or bovine cornea, although the differences were also formulation-dependent. Porcine tissues showed intermediate permeability between rabbit and bovine. Soluplus micelles allowed greater PG accumulation in cornea and sclera whereas Pluronic F68 promoted a faster penetration of lower PG doses
2020-11-26T11:10:30Z
2020-11-26T11:10:30Z
2020
journal article
Alambiaga-Caravaca, A.M.; Calatayud-Pascual, M.A.; Rodilla, V.; Concheiro, A.; López-Castellano, A.; Alvarez-Lorenzo, C. Micelles of Progesterone for Topical Eye Administration: Interspecies and Intertissues Differences in Ex Vivo Ocular Permeability. Pharmaceutics 2020, 12, 702
http://hdl.handle.net/10347/23815
10.3390/pharmaceutics12080702
1999-4923
eng
https://doi.org/10.3390/pharmaceutics12080702
info:eu-repo/grantAgreement/AEI/Plan Estatal de Investigación Científica y Técnica y de Innovación 2017-2020/SAF2017-83118-R/ES/ARQUITECTURAS POLIMERICAS 3D ACTIVAS PARA MEDICINA REGENERATIVA Y TERAPIA LOCALIZADA
http://creativecommons.org/licenses/by/4.0/
open access
© 2020 by the author. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/)
Atribución 4.0 Internacional
MDPI
oai:minerva.usc.es:10347/123022023-03-27T08:28:38Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Polysaccharide-based aerogel microspheres for oral drug delivery
García González, Carlos Alberto
Jin, Ming
Gerth, J.
Álvarez Lorenzo, Carmen Isabel
Smirnova, I.
Universidade de Santiago de Compostela. Departamento de Farmacia e Tecnoloxía Farmacéutica
Polysaccharide-based aerogel
Ketoprofen
Benzoic acid
Supercritical impregnation
Drug release kinetics
NOTICE: this is the author’s version of a work that was accepted for publication in Carbohydrate polymers. Changes resulting from the publishing process, such as peer review, editing, corrections, structural formatting, and other quality control mechanisms may not be reflected in this document. Changes may have been made to this work since it was submitted for publication. A definitive version was subsequently published in Carbohydrate Polymers
Volume 117, 6 March 2015, Pages 797–806, doi:10.1016/j.carbpol.2014.10.045
Polysaccharide-based aerogels in the form of microspheres were investigated as carriers of poorly water soluble drugs for oral administration. These bio-based carriers may combine the biocompatibility of polysaccharides and the enhanced drug loading capacity of dry aerogels. Aerogel microspheres from starch, pectin and alginate were loaded with ketoprofen (anti-inflammatory drug) and benzoic acid (used in the management of urea cycle disorders) via supercritical CO2-assisted adsorption. Amount of drug loaded depended on the aerogel matrix structure and composition and reached values up to 1.0 × 10−3 and 1.7 × 10−3 g/m2 for ketoprofen and benzoic acid in starch microspheres. After impregnation, drugs were in the amorphous state in the aerogel microspheres. Release behavior was evaluated in different pH media (pH 1.2 and 6.8). Controlled drug release from pectin and alginate aerogel microspheres fitted Gallagher–Corrigan release model (R2 > 0.99 in both cases), with different relative contribution of erosion and diffusion mechanisms depending on the matrix composition. Release from starch aerogel microspheres was driven by dissolution, fitting the first-order kinetics due to the rigid starch aerogel structure, and showed different release rate constant (k1) depending on the drug (0.075 and 0.160 min−1 for ketoprofen and benzoic acid, respectively). Overall, the results point out the possibilities of tuning drug loading and release by carefully choosing the polysaccharide used to prepare the aerogels.
2015-02-13T08:56:44Z
2017-08-29T01:00:16Z
2015-03-06
journal article
C.A. García-González, M. Jin, J. Gerth, C. Alvarez-Lorenzo, I. Smirnova, Polysaccharide-based aerogel microspheres for oral drug delivery, Carbohydrate Polymers, Volume 117, 6 March 2015, Pages 797-806, ISSN 0144-8617, http://dx.doi.org/10.1016/j.carbpol.2014.10.045
0144-8617
E-ISSN 1879-1344
http://hdl.handle.net/10347/12302
10.1016/j.carbpol.2014.10.045
eng
http://dx.doi.org/10.1016/j.carbpol.2014.10.045
open access
Elsevier
oai:minerva.usc.es:10347/330292024-03-21T09:21:42Zcom_10347_2989com_10347_2889com_10347_227com_10347_2904com_10347_2890com_10347_2888col_10347_9764col_10347_12265
Integrating bioprinting, cell therapies and drug delivery towards in vivo regeneration of cartilage, bone and osteochondral tissue
Abbadessa, Anna
Ronca, Alfredo
Salerno, Aurelio
Universidade de Santiago de Compostela. Centro de Investigación en Medicina Molecular e Enfermidades Crónicas
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Bioprinted scafolds
Bone
Cartilage
Osteochondral tissue
Growth factors
Spatio-temporal drug release
The biological and biomechanical functions of cartilage, bone and osteochondral tissue are naturally orchestrated by a complex crosstalk between zonally dependent cells and extracellular matrix components. In fact, this crosstalk involves biomechanical signals and the release of biochemical cues that direct cell fate and regulate tissue morphogenesis and remodelling in vivo. Three-dimensional bioprinting introduced a paradigm shift in tissue engineering and regenerative medicine, since it allows to mimic native tissue anisotropy introducing compositional and architectural gradients. Moreover, the growing synergy between bioprinting and drug delivery may enable to replicate cell/extracellular matrix reciprocity and dynamics by the careful control of the spatial and temporal patterning of bioactive cues. Although significant advances have been made in this direction, unmet challenges and open research questions persist. These include, among others, the optimization of scaffold zonality and architectural features; the preservation of the bioactivity of loaded active molecules, as well as their spatio-temporal release; the in vitro scaffold maturation prior to implantation; the pros and cons of each animal model and the graft-defect mismatch; and the in vivo non-invasive monitoring of new tissue formation. This work critically reviews these aspects and reveals the state of the art of using three-dimensional bioprinting, and its synergy with drug delivery technologies, to pattern the distribution of cells and/or active molecules in cartilage, bone and osteochondral engineered tissues. Most notably, this work focuses on approaches, technologies and biomaterials that are currently under in vivo investigations, as these give important insights on scaffold performance at the implantation site and its interaction/integration with surrounding tissues
2024-03-06T16:28:47Z
2024-03-06T16:28:47Z
2023
journal article
2190-393X
http://hdl.handle.net/10347/33029
10.1007/s13346-023-01437-1
2190-3948
eng
https://doi.org/10.1007/s13346-023-01437-1
http://creativecommons.org/licenses/by/4.0/
open access
© 2023. The Author(s).Open Access This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons licence, and indicate if changes were made. The images or other third party material in this article are included in the article's Creative Commons licence, unless indicated otherwise in a credit line to the material. If material is not included in the article's Creative Commons licence and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this licence, visit http://creativecommons.org/licenses/by/4.0/
Atribución 4.0 Internacional
Springer
oai:minerva.usc.es:10347/212402023-07-10T06:17:06Zcom_10347_2989com_10347_2889com_10347_227com_10347_2904com_10347_2890com_10347_2888col_10347_9764col_10347_12265
Interspecies differences in protein expression do not impact the spatiotemporal regulation of glycoprotein VI mediated activation
Dunster, Joanne L.
Unsworth, Amanda J.
Bye, Alexander P.
Haining, Elizabeth J.
Sowa, Marcin A.
Di, Ying
Sage, Tanya
Pallin, Chiara
Pike, Jeremy A.
Hardy, Alexander T.
Nieswandt, Bernhard
García Alonso, Ángel
Watson, Steve P.
Poulter, Natalie S.
Gibbins, Jonathan M.
Pollitt, Alice Y.
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Universidade de Santiago de Compostela. Centro de Investigación en Medicina Molecular e Enfermidades Crónicas
GPVI
Mathematical modelling
Platelet
Syk
Accurate protein quantification is a vital prerequisite for generating meaningful predictions when using systems biology approaches, a method that is increasingly being used to unravel the complexities of subcellular interactions and as part of the drug discovery process. Quantitative proteomics, flow cytometry, and western blotting have been extensively used to define human platelet protein copy numbers, yet for mouse platelets, a model widely used for platelet research, evidence is largely limited to a single proteomic dataset in which the total amount of proteins was generally comparatively higher than those found in human platelets.
2020-04-07T18:19:28Z
2020-04-07T18:19:28Z
2019
journal article
Dunster, JL, Unsworth, AJ, Bye, AP, et al. Interspecies differences in protein expression do not impact the spatiotemporal regulation of glycoprotein VI mediated activation. J Thromb Haemost. 2020; 18: 485– 496. https://doi.org/10.1111/jth.14673
1538-7933
http://hdl.handle.net/10347/21240
10.1111/jth.14673
1538-7836
eng
https://doi.org/10.1111/jth.14673
info:eu-repo/grantAgreement/EC/H2020/766118
https://creativecommons.org/licenses/by/4.0/
open access
© 2019 The Authors and the Journal of Thrombosis and Haemostasis. This is an open access article under the terms of the Creative Commons Attribution License, which permits use, distribution and reproduction in any medium, provided the original work is properly cited
Wiley
oai:minerva.usc.es:10347/329852024-03-06T01:03:06Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Langmuir monolayer studies of non-ionic surfactants and DOTMA for the design of ophthalmic niosomes
Kattar, Axel
Lage, Emílio V.
Casas Parada, Matilde
Concheiro Nine, Ángel Joaquín
Álvarez Lorenzo, Carmen Isabel
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Universidade de Santiago de Compostela. Departamento de Química Física
Langmuir monolayer
Niosome
Cholesterol
Tween 60
DOTMA
π-A isotherm
The worldwide increase in diabetes entails a rise in associated diseases, with diabetic retinopathy on the forefront of the ocular complications. To overcome the challenges posed by ocular barriers, self-assembled nanocarriers have gathered increasing attention in recent years, with niosomes revealing themselves to be suitable for the delivery of a variety of drugs. This study investigated the mechanical properties of Langmuir monolayers comprising cholesterol, Tween 60, and 1,2-di-O-octadecenyl-3-trimethylammonium propane (DOTMA), both individually and in binary and ternary systems. The cholesterol monolayer was characterized by an L-shaped isotherm, reflecting two surface aggregation states. Tween 60 exhibited expanded conformation and progressive aggregation, transitioning through a phase change. The addition of cholesterol to Tween 60 resulted in a subtle reduction in surface compressional modulus. The compression isotherms highlighted the stabilizing effect of cholesterol on the monolayer, affecting the film's resistance to compression. The introduction of DOTMA in Tween 60 monolayers revealed concentration-dependent effects, where the compression resistance of the film was proportional to DOTMA concentration. Ternary systems of cholesterol, DOTMA and Tween 60 exhibited unique behavior, with DOTMA enhancing film stability and cholesterol modulating this effect. Temperature and subphase ionic strength variations further exacerbated the effects of DOTMA concentration. Brewster Angle Microscopy confirmed the absence of microdomains in the compressed monolayer, supporting the hypothesis of a monolayer collapse. Overall, the research provided valuable insights into the intricate interactions and mechanical behavior of these surfactant systems and the feasibility of obtaining cationic niosome-based drug delivery.
2024-03-05T09:16:52Z
2024-03-05T09:16:52Z
2024
journal article
Heliyon Volume 10, Issue 4, 29 February 2024, e25887
http://hdl.handle.net/10347/32985
10.1016/j.heliyon.2024.e25887
2405-8440
eng
http://creativecommons.org/licenses/by-nc-nd/4.0/
open access
© 2024 The Authors. Published by Elsevier B.V. This is an open access article under the CC BY-NC-ND license
Attribution-NonCommercial-NoDerivatives 4.0 Internacional
Elsevier
oai:minerva.usc.es:10347/213122020-04-14T02:00:57Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Development, Characterization, and In Vitro Evaluation of Resveratrol-Loaded Poly-(ε-caprolactone) Microcapsules Prepared by Ultrasonic Atomization for Intra-Articular Administration
Luzardo Álvarez, Asteria María
Lamela Gómez, Iván
Otero Espinar, Francisco Javier
Blanco Méndez, José
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Drug delivery system
Microcapsules
Photodegradation
Ultrasound
Antioxidant
Site-specific delivery
Resveratrol
Intra-articular administration of drugs to the joint in the treatment of joint disease has the potential to minimize the systemic bioavailability and the usual side-effects associated with oral drug administration. In this work, a drug delivery system is proposed to achieve an anti-inflammatory local effect using resveratrol (RSV). This study aims to develop microcapsules made of poly-(ε-caprolactone) (PCL) by ultrasonic atomization to preserve the antioxidant activity of RSV, to prevent its degradation and to suppress the inflammatory response in activated RAW 264.7 macrophages. An experimental design was performed to build a mathematical model that could estimate the effect of nozzle power and polymer concentration on particle size and encapsulation efficiency. RSV-loaded microcapsules showed adequate morphology, particle size, and loading efficiency properties. RSV formulations exhibited negligible cytotoxicity and an efficient amelioration of inflammatory responses, in terms of Nitric Oxide (NO), ROS (Reactive Oxygen Species), and lipid peroxidation in macrophages. Thus, RSV-loaded microcapsules merit consideration as a drug delivery system suitable for intra-articular administration in inflammatory disorders affecting the joint
2020-04-13T05:48:37Z
2020-04-13T05:48:37Z
2019
journal article
Luzardo-Álvarez, A.; Lamela-Gómez, I.; Otero-Espinar, F.; Blanco-Méndez, J. Development, Characterization, and In Vitro Evaluation of Resveratrol-Loaded Poly-(ε-caprolactone) Microcapsules Prepared by Ultrasonic Atomization for Intra-Articular Administration. Pharmaceutics 2019, 11, 249
http://hdl.handle.net/10347/21312
10.3390/pharmaceutics11060249
1999-4923
eng
https://doi.org/10.3390/pharmaceutics11060249
https://creativecommons.org/licenses/by/4.0/
open access
© 2019 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/)
MDPI
oai:minerva.usc.es:10347/213482023-07-10T06:18:07Zcom_10347_2919com_10347_2891com_10347_2888com_10347_227com_10347_2904com_10347_2890com_10347_2925col_10347_10699col_10347_12265col_10347_9937
Three-Dimensional Hybrid Mesoporous Scaffolds for Simvastatin Sustained Delivery with in Vitro Cell Compatibility
Vargas Osorio, Zulema
Luzardo Álvarez, Asteria María
Piñeiro Redondo, Yolanda
Vázquez Vázquez, Carlos
Gómez Amoza, José Luis
Blanco Méndez, José
Otero Espinar, Francisco Javier
Rivas Rey, José
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Universidade de Santiago de Compostela. Departamento de Física Aplicada
Universidade de Santiago de Compostela. Departamento de Química Física
The development of scaffolds with suitable physicochemical and mechanical properties allowing for the
structural regeneration of injured bone and recovery of the natural biological functionality is still a challenge in the tissue
engineering field. Nanostructured materials with added theranostic abilities, together with an interconnected hierarchy of pores,
offer the possibility to provide a new generation of bone implants. In this work, scaffolds with highly porous and resistant threedimensional structures have been successfully developed by homogeneously embedding mesoporous silica nanostructures in a
bioactive matrix of chitosan/κ-carrageenan. Moreover, magnetite (Fe3O4) nanoparticles were also added to the mesoporous
scaffold to include additional magnetic functionalities for diagnostic or therapeutic actions. The complete physicochemical
characterization shows mesoporous materials with a wide range of interconnected pores, remarkable surface roughness, and
large effective surface area, suitable for cell adhesion. In accordance to these properties, a simvastatin loading and release assay
showed high loading capacities and sustained release over a long period of time. Together with a suitable resistance against
degradation and biocompatible performance assessed by cell viability assays, these scaffolds show interesting features for
delivering drugs with activity in bone regeneration processes.
2020-04-13T22:47:23Z
2020-04-13T22:47:23Z
2019
journal article
Vargas-Osorio, Z., Luzardo-Álvarez, A., Piñeiro, Y., Vázquez-Vázquez, C., Gómez-Amoza, J.L., Blanco-Méndez, J., Otero Espinar, F.J., Rivas, J. (2019) Three-Dimensional Hybrid Mesoporous Scaffolds for Simvastatin Sustained Delivery with in Vitro Cell Compatibility. "ACS Omega", 4 (3), 5496-5508
http://hdl.handle.net/10347/21348
10.1021/acsomega.8b03676
2470-1343
eng
https://doi.org/10.1021/acsomega.8b03676
info:eu-repo/grantAgreement/EC/H2020/686009
open access
Copyright © 2019 American Chemical Society. This is an open access article published under an ACS AuthorChoice License, which permits
copying and redistribution of the article or any adaptations for non-commercial purposes
American Chemical Society
oai:minerva.usc.es:10347/239892021-01-09T03:06:15Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
From Ethnomedicine to Plant Biotechnology and Machine Learning: The Valorization of the Medicinal Plant Bryophyllum sp.
García Pérez, Pascual
Lozano Milo, Eva
Landín Pérez, Mariana
Gallego, Pedro Pablo
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Bryophyllum
Traditional medicine
Secondary metabolism
Bioactive and phenolic compounds
Bufadienolides
Antioxidants
Cytotoxic activity
Plant tissue culture
Artificial intelligence
The subgenus Bryophyllum includes about 25 plant species native to Madagascar, and is widely used in traditional medicine worldwide. Different formulations from Bryophyllum have been employed for the treatment of several ailments, including infections, gynecological disorders, and chronic diseases, such as diabetes, neurological and neoplastic diseases. Two major families of secondary metabolites have been reported as responsible for these bioactivities: phenolic compounds and bufadienolides. These compounds are found in limited amounts in plants because they are biosynthesized in response to different biotic and abiotic stresses. Therefore, novel approaches should be undertaken with the aim of achieving the phytochemical valorization of Bryophyllum sp., allowing a sustainable production that prevents from a massive exploitation of wild plant resources. This review focuses on the study of phytoconstituents reported on Bryophyllum sp.; the application of plant tissue culture methodology as a reliable tool for the valorization of bioactive compounds; and the application of machine learning technology to model and optimize the full phytochemical potential of Bryophyllum sp. As a result, Bryophyllum species can be considered as a promising source of plant bioactive compounds, with enormous antioxidant and anticancer potential, which could be used for their large-scale biotechnological exploitation in cosmetic, food, and pharmaceutical industries
2020-12-15T13:17:37Z
2020-12-15T13:17:37Z
2020
journal article
García-Pérez, P.; Lozano-Milo, E.; Landin, M.; Gallego, P.P. From Ethnomedicine to Plant Biotechnology and Machine Learning: The Valorization of the Medicinal Plant Bryophyllum sp.. Pharmaceuticals 2020, 13, 444
http://hdl.handle.net/10347/23989
10.3390/ph13120444
1424-8247
eng
https://doi.org/10.3390/ph13120444
http://creativecommons.org/licenses/by/4.0/
open access
© 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
Atribución 4.0 Internacional
MDPI
oai:minerva.usc.es:10347/234892023-07-10T06:17:57Zcom_10347_2989com_10347_2889com_10347_227com_10347_2904com_10347_2890com_10347_2888com_10347_2927com_10347_2891col_10347_9764col_10347_12265col_10347_12292
Potent and selective MAO-B inhibitory activity: Amino- versus nitro-3-arylcoumarin derivatives
Matos, Maria João Correia Pinto Carvalho de
Rodríguez Enríquez, Fernanda
Vilar, Santiago
Santana Penín, María Lourdes
Uriarte Villares, Eugenio
Hripcsak, George
Estrada, Martín
Rodríguez Franco, María Isabel
Viña Castelao, María Dolores
Universidade de Santiago de Compostela. Centro de Investigación en Medicina Molecular e Enfermidades Crónicas
Universidade de Santiago de Compostela. Departamento de Farmacoloxía
Universidade de Santiago de Compostela. Departamento de Química Orgánica
3-Arylcoumarins
Perkin reaction
Monoamine oxidase inhibitors
PAMPA assay
ADME theoretical properties
Docking studies
In this study we synthesized and evaluated a new series of amino and nitro 3-arylcoumarins as hMAO-A and hMAO-B inhibitors. Compounds 2, 3, 5 and 6 presented a better activity and selectivity profile against the hMAO-B isoform (IC50 values between 2 and 6 nM) than selegiline. In general, the amino derivatives (4–6) proved to be more selective against MAO-B than the nitro derivatives (1–3). Additionally, a theoretical study of some physicochemical properties, PAMPA and reversibility assays for the most potent derivative, and molecular docking simulations were carried out to further explain the pharmacological results, and to identify the hypothetical binding mode for the compounds inside the hMAO-B
2020-10-29T12:03:35Z
2020-10-29T12:03:35Z
2015
journal article
Bioorganic & Medicinal Chemistry Letters. Volume 25, Issue 3, 1 February 2015, Pages 642-648. https://doi.org/10.1016/j.bmcl.2014.12.001
0960-894X
http://hdl.handle.net/10347/23489
10.1016/j.bmcl.2014.12.001
eng
https://doi.org/10.1016/j.bmcl.2014.12.001
info:eu-repo/grantAgreement/FCT/SFRH/SFRH%2FBPD%2F95345%2F2013/PT
http://creativecommons.org/licenses/by-nc-nd/4.0/
open access
© 2014 Elsevier Ltd. This manuscript version is made available under the CC-BY-NC-ND 4.0 license (http://creativecommons.org/licenses/by-nc-nd/4.0/)
Attribution-NonCommercial-NoDerivatives 4.0 Internacional
Elsevier
oai:minerva.usc.es:10347/241882021-01-15T03:01:53Zcom_10347_2896com_10347_2890com_10347_2888com_10347_227com_10347_2904col_10347_15763col_10347_12265
Characterization of New Proteomic Biomarker Candidates in Mucopolysaccharidosis Type IVA
Álvarez González, José Víctor
Bravo López, Susana Belén
Chantada Vázquez, María del Pilar
Colón Mejeras, Cristóbal
Castro López, María José de
Morales, Montserrat
Vitoria, Isidro
Tomatsu, Shunji
Otero Espinar, Francisco Javier
Couce Pico, María de la Luz
Universidade de Santiago de Compostela. Departamento de Ciencias Forenses, Anatomía Patolóxica, Xinecoloxía e Obstetricia, e Pediatría
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Biomarkers
Enzyme replacement therapy
Lysosomal disorders
Proteomics
Mucopolysaccharidosis type IVA (MPS IVA) is a lysosomal storage disease caused by mutations in the N-acetylgalactosamine-6-sulfatase (GALNS) gene. Skeletal dysplasia and the related clinical features of MPS IVA are caused by disruption of the cartilage and its extracellular matrix, leading to a growth imbalance. Enzyme replacement therapy (ERT) with recombinant human GALNS has yielded positive results in activity of daily living and endurance tests. However, no data have demonstrated improvements in bone lesions and bone grow thin MPS IVA after ERT, and there is no correlation between therapeutic efficacy and urine levels of keratan sulfate, which accumulates in MPS IVA patients. Using qualitative and quantitative proteomics approaches, we analyzed leukocyte samples from healthy controls (n = 6) and from untreated (n = 5) and ERT-treated (n = 8, sampled before and after treatment) MPS IVA patients to identify potential biomarkers of disease. Out of 690 proteins identified in leukocytes, we selected a group of proteins that were dysregulated in MPS IVA patients with ERT. From these, we identified four potential protein biomarkers, all of which may influence bone and cartilage metabolism: lactotransferrin, coronin 1A, neutral alpha-glucosidase AB, and vitronectin. Further studies of cartilage and bone alterations in MPS IVA will be required to verify the validity of these proteins as potential biomarkers of MPS IVA
2021-01-14T13:59:29Z
2021-01-14T13:59:29Z
2021
journal article
Álvarez, V.J.; Bravo, S.B.; Chantada-Vazquez, M.P.; Colón, C.; De Castro, M.J.; Morales, M.; Vitoria, I.; Tomatsu, S.; Otero-Espinar, F.J.; Couce, M.L. Characterization of New Proteomic Biomarker Candidates in Mucopolysaccharidosis Type IVA. Int. J. Mol. Sci. 2021, 22, 226
http://hdl.handle.net/10347/24188
10.3390/ijms22010226
1422-0067
eng
https://doi.org/10.3390/ijms22010226
http://creativecommons.org/licenses/by/4.0/
open access
© 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/)
Atribución 4.0 Internacional
MDPI
oai:minerva.usc.es:10347/331142024-03-21T09:21:42Zcom_10347_2906com_10347_2890com_10347_2888com_10347_227com_10347_2904col_10347_15791col_10347_12265
Application of a multi-toxin detect method to analyze mycotoxins occurrence in plant-based beverages
Rodríguez Cañás, Inés
González Jartín, Jesús María
Alfonso Rancaño, María Amparo
Alvariño Romero, Rebeca
Rodríguez Vieytes, María Mercedes
Botana López, Luis Miguel
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Universidade de Santiago de Compostela. Departamento de Fisioloxía
Mycotoxin
UHPLC
Mass spectrometry
Plant-based beverages
In recent years, plant-based beverages have gained popularity on the market due to environmental and ethical concerns, as well as milk intolerances and allergies. However, raw materials employed in the manufacture of these products are susceptible to mycotoxin contamination. For this reason, a new method based on a QuEChERS extraction procedure followed by ultra-high performance liquid chromatography coupled with tandem mass spectrometry (UHPLC-MS/MS) detection was developed for the analysis of 29 mycotoxins in oat, rice, soy, and almond beverages. The method was validated in terms of linearity, detection and quantification limits, matrix effect, recoveries, accuracy and precision. Satisfactory performance characteristics were achieved, with recoveries above 70% for most mycotoxins. Several commercial samples were analyzed, aflatoxins were frequently detected in rice and almond beverages, while T-2 and HT-2 toxins were identified in oat-based products. In addition, emerging mycotoxins such as enniatins and beauvericin were detected in the four types of beverages
2024-03-11T16:01:33Z
2024-03-11T16:01:33Z
2024
journal article
Food Chemistry, Volume 434, 2024, 137427
http://hdl.handle.net/10347/33114
eng
https://doi.org/10.1016/j.foodchem.2023.137427
http://creativecommons.org/licenses/by-nc-nd/4.0/
open access
©2023 The Author(s).Published by Elsevier Ltd.This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/)
Attribution-NonCommercial-NoDerivatives 4.0 Internacional
Elsevier
oai:minerva.usc.es:10347/262292021-05-21T02:04:48Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Redefining dilute and shoot: The evolution of the technique and its application in the analysis of foods and biological matrices by liquid chromatography mass spectrometry
Greer, Brett
Chevallier, Olivier P.
Quinn, Brian
Botana López, Luis Miguel
Elliot, Christopher T.
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Dilute-and-shoot
Liquid chromatography
Mass spectrometry
Sample preparation
Food analysis
Bioanalysis
Mycotoxin
Multi-class
With laboratories seeking to expand analytical capabilities and create multi-class, multi-analyte methods, there has been a shift toward generic sample clean-up techniques such as “dilute-and-shoot”. Advantages of this methodology include its simplicity, minimal analyte losses, high sample throughput and number of analyte classes included. The evolution of dilute-and-shoot has permitted its use across a variety of matrices including food and biological and in various scientific fields such as food, forensics and environmental. The versatility of the technique permits the expansion of current fields of research without the usual laborious method development. There can be issues with matrix effects and robust quantitation as analyte number increases. This review provides an overview of the technique combined with liquid chromatography mass spectrometry, highlighting its power in facilitating multi-class analysis. Coupled with increases in instrument performance there is potential to employ this methodology in expanding analytical capabilities in many areas of life science research
2021-05-20T10:31:34Z
2021-05-20T10:31:34Z
2021
journal article
Trends in Analytical Chemistry, 141 (2021), 116284
0165-9936
http://hdl.handle.net/10347/26229
10.1016/j.trac.2021.116284
eng
https://doi.org/10.1016/j.trac.2021.116284
http://creativecommons.org/licenses/by-nc-nd/4.0/
open access
© 2021 The Authors. Published by Elsevier B.V. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/)
Attribution-NonCommercial-NoDerivatives 4.0 Internacional
Elsevier
oai:minerva.usc.es:10347/240612021-01-09T03:09:22Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Rifabutin-Loaded Nanostructured Lipid Carriers as a Tool in Oral Anti-Mycobacterial Treatment of Crohn’s Disease
Rouco Taboada, Helena
Díaz Rodríguez, Patricia
Gaspar, Diana P.
Gonçalves, Lídia
Cuerva Vidales, Miguel
Remuñán López, María del Carmen
Almeida, António J.
Landín Pérez, Mariana
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Rifabutin
Nanostructured lipid carriers
Cell uptake
Caco-2 cells
Oral administration
Crohn’s disease
Oral anti-mycobacterial treatment of Crohn’s disease (CD) is limited by the low aqueous solubility of drugs, along with the altered gut conditions of patients, making uncommon their clinical use. Hence, the aim of the present work is focused on the in vitro evaluation of rifabutin (RFB)-loaded Nanostructured lipid carriers (NLC), in order to solve limitations associated to this therapeutic approach. RFB-loaded NLC were prepared by hot homogenization and characterized in terms of size, polydispersity, surface charge, morphology, thermal stability, and drug payload and release. Permeability across Caco-2 cell monolayers and cytotoxicity and uptake in human macrophages was also determined. NLC obtained were nano-sized, monodisperse, negatively charged, and spheroidal-shaped, showing a suitable drug payload and thermal stability. Furthermore, the permeability profile, macrophage uptake and selective intracellular release of RFB-loaded NLC, guarantee an effective drug dose administration to cells. Outcomes suggest that rifabutin-loaded NLC constitute a promising strategy to improve oral anti-mycobacterial therapy in Crohn’s disease
2020-12-17T12:47:28Z
2020-12-17T12:47:28Z
2020
journal article
Rouco, H.; Diaz-Rodriguez, P.; Gaspar, D.P.; Gonçalves, L.M.D.; Cuerva, M.; Remuñán-López, C.; Almeida, A.J.; Landin, M. Rifabutin-Loaded Nanostructured Lipid Carriers as a Tool in Oral Anti-Mycobacterial Treatment of Crohn’s Disease. Nanomaterials 2020, 10, 2138
http://hdl.handle.net/10347/24061
10.3390/nano10112138
2079-4991
eng
https://doi.org/10.3390/nano10112138
http://creativecommons.org/licenses/by/4.0/
open access
© 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/)
Atribución 4.0 Internacional
MDPI
oai:minerva.usc.es:10347/316392024-01-09T01:02:54Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Gracilin A Derivatives Target Early Events in Alzheimer’s Disease: inVitro Effects on Neuroinflammation and Oxidative Stress
Alvariño Romero, Rebeca
Alonso López, Eva
Abbasov, Mikail E.
Chaheine, Christian M.
Conner, Michael L.
Romo, Daniel
Alfonso Rancaño, María Amparo
Botana López, Luis Miguel
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Universidade de Santiago de Compostela. Departamento de Fisioloxía
Gracilin
Neuroinflammation
Antioxidant
Alzheimer’s disease
Nrf2
Neuroprotection
The search for compounds capable of targeting early pathological changes of Alzheimer̀s disease (AD), such as oxidative stress and neuroinflammation, is an important challenge. Gracilin A derivatives were recently synthesized, using a pharmacophore-directed retrosynthesis (PDR) strategy, and found to possess potent neuroprotective effects. In this work, the previously described derivatives 1–7 which demonstrated mitochondrial-mediated, antioxidant effects were chosen for further study. The ability of compounds to modulate the expression of antioxidant genes (CAT, GPx, SODs, and Nrf2) was determined in SH-SY5Y cells, and the simplified derivatives 2 and 3 were found to be the most effective. The anti-neuroinflammatory properties of all derivatives were assessed in BV2 microglial cells activated with lipopolysaccharide (LPS). Several derivatives decreased the release of cytokines (Il-1β, IL-6, GM-CSF, and TNF-α) and other damaging molecules (ROS, NO) and also regulated the translocation of Nrf2 and NFκB, and reduced p38 activation. These protective effects were confirmed in a trans-well coculture with BV2 and SH-SY5Y cells and several derivatives increased SH-SY5Y survival. This present work demonstrates the neuroprotective properties of gracilin A derivatives, making them promising candidate drugs for AD. Particularly, derivatives 2 and 3 showed the greatest potential as lead compounds for further development
2023-12-22T12:59:16Z
2023-12-22T12:59:16Z
2019
journal article
Alvariño, R., Alonso, E., Abbasov, M.E., Chaheine, C.M., Conner, M.L., Romo, D., Alfonso, A., Botana, L.M. (2019). Gracilin A Derivatives Target Early Events in Alzheimer’s Disease: in Vitro Effects on Neuroinflammation and Oxidative Stress. ACS Chemical Neuroscience,10 (9), 4102-4111
http://hdl.handle.net/10347/31639
10.1021/acschemneuro.9b00329
eng
info:eu-repo/grantAgreement/MINECO//AGL2014-58210-R/ES/EVALUACION DE LA SEGURIDAD ALIMENTARIA DE PRODUCTOS PESQUEROS ASOCIADA A LA PRESENCIA DE TOXINAS MARINAS DE NUEVA APARICION EN AGUAS EUROPEAS/
info:eu-repo/grantAgreement/MINECO//PI16%2F01830/ES/PAPEL DE LAS CICLOFILINAS Y SU RECEPTOR EMPRIM (CD147) EN LAS ENFERMEDADES ATEROSCLERÓTICAS Y SU MODULACIÓN CON COMPUESTOS DE ORIGEN MARINO/
info:eu-repo/grantAgreement/EC/H2020/778069/EU
052964
open access
American Chemical Society
oai:minerva.usc.es:10347/236322023-03-27T08:15:41Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Cyclodextrin Cationic Polymer-Based Nanoassemblies to Manage Inflammation by Intra-Articular Delivery Strategies
Cordaro, Annalaura
Zagami, Roberto
Malanga, Milo
Venkatesan, Jagadeesh Kumar
Álvarez Lorenzo, Carmen Isabel
Cucchiarini, Magali
Piperno, Anna
Mazzaglia, Antonino
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Polymeric cyclodextrins
IL-1β
Human marrow-derived mesenchymal stromal cells
Rhodamine
Injectable nanobioplatforms capable of locally fighting the inflammation in osteoarticular diseases, by reducing the number of administrations and prolonging the therapeutic effect is highly challenging. β-Cyclodextrin cationic polymers are promising cartilage-penetrating candidates by intra-articular injection due to the high biocompatibility and ability to entrap multiple therapeutic and diagnostic agents, thus monitoring and mitigating inflammation. In this study, nanoassemblies based on poly-β-amino-cyclodextrin (PolyCD) loaded with the non-steroidal anti-inflammatory drug diclofenac (DCF) and linked by supramolecular interactions with a fluorescent probe (adamantanyl-Rhodamine conjugate, Ada-Rhod) were developed to manage inflammation in osteoarticular diseases. PolyCD@Ada-Rhod/DCF supramolecular nanoassemblies were characterized by complementary spectroscopic techniques including UV-Vis, steady-state and time-resolved fluorescence, DLS and ζ-potential measurement. Stability and DCF release kinetics were investigated in medium mimicking the physiological conditions to ensure control over time and efficacy. Biological experiments evidenced the efficient cellular internalization of PolyCD@Ada-Rhod/DCF (within two hours) without significant cytotoxicity in primary human bone marrow-derived mesenchymal stromal cells (hMSCs). Finally, polyCD@Ada-Rhod/DCF significantly suppressed IL-1β production in hMSCs, revealing the anti-inflammatory properties of these nanoassemblies. With these premises, this study might open novel routes to exploit original CD-based nanobiomaterials for the treatment of osteoarticular diseases
2020-11-10T11:07:23Z
2020-11-10T11:07:23Z
2020
journal article
Cordaro, A.; Zagami, R.; Malanga, M.; Venkatesan, J.K.; Alvarez-Lorenzo, C.; Cucchiarini, M.; Piperno, A.; Mazzaglia, A. Cyclodextrin Cationic Polymer-Based Nanoassemblies to Manage Inflammation by Intra-Articular Delivery Strategies. Nanomaterials 2020, 10, 1712
http://hdl.handle.net/10347/23632
10.3390/nano10091712
2079-4991
eng
https://doi.org/10.3390/nano10091712
http://creativecommons.org/licenses/by/4.0/
open access
© 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/)
Atribución 4.0 Internacional
MDPI
oai:minerva.usc.es:10347/212292020-04-08T02:01:11Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Proteomic analysis in morquio a cells treated with immobilized enzymatic replacement therapy on nanostructured lipid systems
Álvarez González, José Víctor
Bravo López, Susana Belén
García Vence, María
Castro López, María José de
Luzardo Álvarez, Asteria María
Colón Mejeras, Cristóbal
Tomatsu, Shunji
Otero Espinar, Francisco Javier
Couce Pico, María de la Luz
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Enzyme replacement therapy
Lysosomal disorders
Nanoparticles
Proteomics
[ENG]Morquio A syndrome, or mucopolysaccharidosis type IVA (MPS IVA), is a lysosomal storage disease due to mutations in the N-acetylgalactosamine-6-sulfatase (GALNS) gene. Systemic skeletal dysplasia and the related clinical features of MPS IVA are due to disruption of cartilage and its extracellular matrix, leading to an imbalance of growth. Enzyme replacement therapy (ERT) with recombinant human GALNS, alpha elosulfase, provides a systemic treatment. However, this therapy has a limited impact on skeletal dysplasia because the infused enzyme cannot penetrate cartilage and bone. Therefore, an alternative therapeutic approach to reach the cartilage is an unmet challenge. We have developed a new drug delivery system based on a nanostructure lipid carrier with the capacity to immobilize enzymes used for ERT and to target the lysosomes. This study aimed to assess the effect of the encapsulated enzyme in this new delivery system, using in vitro proteomic technology. We found a greater internalization of the enzyme carried by nanoparticles inside the cells and an improvement of cellular protein routes previously impaired by the disease, compared with conventional ERT. This is the first qualitative and quantitative proteomic assay that demonstrates the advantages of a new delivery system to improve the MPS IVA ERT
2020-04-07T16:34:15Z
2020-04-07T16:34:15Z
2019
journal article
Álvarez, J.V.; Bravo, S.B.; García-Vence, M.; De Castro, M.J.; Luzardo, A.; Colón, C.; Tomatsu, S.; Otero-Espinar, F.J.; Couce, M.L. Proteomic Analysis in Morquio A Cells Treated with Immobilized Enzymatic Replacement Therapy on Nanostructured Lipid Systems. Int. J. Mol. Sci. 2019, 20, 4610
http://hdl.handle.net/10347/21229
10.3390/ijms20184610
1422-0067
eng
https://www.mdpi.com/1422-0067/20/18/4610
https://creativecommons.org/licenses/by/4.0/
open access
© 2019 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/)
MDPI
oai:minerva.usc.es:10347/242502021-01-21T03:01:06Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Shoot tip necrosis of in vitro plant cultures: a reappraisal of possible causes and solutions
Teixeira da Silva, Jaime A.
Nezami Alanagh, Esmaeil
Barreal, M. Esther
Kher, Mafatlal M.
Wicaksono, Adhityo
Gulyás, Andrea
Hidvégi, Norbert
Magyar Tábori, Katalin
Mendler Drienyovszki, Nóra
Márton, László
Landín Pérez, Mariana
Gallego, Pedro Pablo
Driver, John A.
Dobránszki, Judit
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Boron
Calcium
Chloride
In vitro shoots
Mineral nutrient deficiency
Physiological disorder
Plant growth regulators
Shoot tip necrosis is a physiological condition and disorder that can arise in plantlets or shoots in vitro that results in death of the shoot tip. This condition, which can spread basipetally and affect the emergence of axillary shoots from buds lower down the stem, is due to the cessation of apical dominance. STN can occur at both shoot multiplication and rooting stages. One of the most common factors that cause STN is nutrient deficiency or imbalance. Moreover, the presence or absence of plant growth regulators (auxins or cytokinins) at specific developmental stages may impact STN. The cytokinin to auxin ratio within an in vitro plant can be modified by varying the concentration of cytokinins used in the culture medium. The supply of nutrients to in vitro shoots or plantlets might also affect their hormonal balance, thus modifying the occurrence of STN. High relative humidity within culture vessels and hyperhydricity are associated with STN. An adequate supply of calcium as the divalent cation (Ca2+) can hinder STN by inhibiting the accumulation of phenolic compounds and thus programmed cell death. Moreover, the level of Ca2+ affects auxin transport and ethylene production, and higher ethylene production, which can occur as a result of high relative humidity in or poor ventilation of the in vitro culture vessel, induces STN. High relative humidity can decrease the mobility of Ca2+ within a plant, resulting in Ca2+ deficiency and STN. STN of in vitro shoots or plantlets can be halted or reversed by altering the basal medium, mainly the concentration of Ca2+, adjusting the levels of auxins or cytokinins, or modifying culture conditions. This review examines the literature related to STN, seeks to discover the associated factors and relations between them, proposes practical solutions, and attempts to better understand the mechanism(s) underlying this condition in vitro
2021-01-20T11:01:47Z
2021-01-20T11:01:47Z
2020
journal article
Teixeira da Silva, J.A., Nezami-Alanagh, E., Barreal, M.E. et al. Shoot tip necrosis of in vitro plant cultures: a reappraisal of possible causes and solutions. Planta 252, 47 (2020). https://doi.org/10.1007/s00425-020-03449-4
0032-0935
http://hdl.handle.net/10347/24250
10.1007/s00425-020-03449-4
1432-2048
eng
https://doi.org/10.1007/s00425-020-03449-4
http://creativecommons.org/licenses/by/4.0/
open access
© The Author(s) 2020. Open Access. This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons licence, and indicate if changes were made. The images or other third party material in this article are included in the article's Creative Commons licence, unless indicated otherwise in a credit line to the material. If material is not included in the article's Creative Commons licence and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this licence, visit http://creativecommons.org/licenses/by/4.0/
Atribución 4.0 Internacional
Springer
oai:minerva.usc.es:10347/213902020-04-15T02:02:35Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Ocular biodistribution studies using molecular imaging
Castro Balado, Ana
Mondelo García, Cristina
González Barcia, Miguel
Zarra Ferro, Irene
Otero Espinar, Francisco Javier
Ruibal Morell, Álvaro
Aguiar Fernández, Pablo
Fernández Ferreiro, Anxo
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Ocular biodistribution
Ocular permanence
Molecular imaging
PET
SPECT
MRI
Classical methodologies used in ocular pharmacokinetics studies have difficulties to obtain information about topical and intraocular distribution and clearance of drugs and formulations. This is associated with multiple factors related to ophthalmic physiology, as well as the complexity and invasiveness intrinsic to the sampling. Molecular imaging is a new diagnostic discipline for in vivo imaging, which is emerging and spreading rapidly. Recent developments in molecular imaging techniques, such as positron emission tomography (PET), single-photon emission computed tomography (SPECT) and magnetic resonance imaging (MRI), allow obtaining reliable pharmacokinetic data, which can be translated into improving the permanence of the ophthalmic drugs in its action site, leading to dosage optimisation. They can be used to study either topical or intraocular administration. With these techniques it is possible to obtain real-time visualisation, localisation, characterisation and quantification of the compounds after their administration, all in a reliable, safe and non-invasive way. None of these novel techniques presents simultaneously high sensitivity and specificity, but it is possible to study biological procedures with the information provided when the techniques are combined. With the results obtained, it is possible to assume that molecular imaging techniques are postulated as a resource with great potential for the research and development of new drugs and ophthalmic delivery systems
2020-04-14T16:27:04Z
2020-04-14T16:27:04Z
2019
journal article
Castro-Balado, A.; Mondelo-García, C.; González-Barcia, M.; Zarra-Ferro, I.; Otero-Espinar, F.J.; Ruibal-Morell, Á.; Aguiar, P.; Fernández-Ferreiro, A. Ocular Biodistribution Studies Using Molecular Imaging. Pharmaceutics 2019, 11, 237
http://hdl.handle.net/10347/21390
10.3390/pharmaceutics11050237
1999-4923
eng
https://doi.org/10.3390/pharmaceutics11050237
https://creativecommons.org/licenses/by/4.0/
open access
© 2019 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/)
MDPI
oai:minerva.usc.es:10347/323182024-02-06T01:02:51Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Aporphine Alkaloids and their Antioxidant Medical Application: From Antineoplastic Agents to Motor Dysfunction Diseases
Nabavi, Seyed M.
Uriarte, Eugenio
Fontenla, Jose A.
Rastrelli, Luca
Sobarzo Sánchez, Eduardo Marcelo
Aporphines
Oxoaporphines
antioxidant
free radical scavengers
oxidative stress
Parkinson´s disease
anticancer
antinociceptive
The published manuscript is available at EurekaSelect via https://www.eurekaselect.com/openurl/content.php?genre=article&doi=10.2174/1385272820666161017165735
One of the biggest challenges in the modern medicine and the food industry is to
provide with compounds that should have the property to be antioxidant that, proportionally, can
be accompanied with pharmacological activities to be used in chronic clinical treatments. This
means, compounds that can extend the shelf life of foods and drugs avoiding its decomposition
by oxidation and, at the same time, to afford potent drugs against various diseases with minor
side effects. Thus, aporphine alkaloids have been the group of nitrogen compounds more studied
and with a wide therapeutic application. Examples such as (−)-boldine (12), (−)-liridinine (15),
(+)-lirinidine (16) and glaucine (24) have been studied for its interesting antioxidant activity and,
in case of 24, synthetic modifications have managed to generate derivatives that exhibit more
efficient antioxidant activity in comparison with carboxy group-containing agent alone and
aporphine derivative alone. Thus, clinical treatment against oxidative stress-related diseases, as
Parkinson´s disease, anticancer, antinociceptive, therapeutic applications among other mentioned
in this review, they give the possibility of using these aporphine alkaloids of low cytotoxicity as
an excellent alternative tool in the development of new therapeutic patterns using the duplicity;
biologically active ingredient-antioxidant.
2024-02-05T09:40:22Z
2024-02-05T09:40:22Z
2017
journal article
Current Organic Chemistry, 2017, 21, 342-347
1385-2728
http://hdl.handle.net/10347/32318
10.2174/1385272820666161017165735
1875-5348
eng
open access
Betham Science
oai:minerva.usc.es:10347/320102024-02-05T10:13:54Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Discovery and optimization of 3-thiophenylcoumarins as novel agents against Parkinson’s disease: Synthesis, in vitro and in vivo studies
Rodríguez Enríquez, Fernanda
Viña, Dolores
Uriarte, Eugenio
Fontenla, Jose A.
Matos, Maria João Correia Pinto Carvalho de
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
3-Thiophenylcoumarins
Parkinson´s disease
DPPH scavengers
Neuroprotectors
Open field test
Monoamine oxidase B inhibitors
Monoamine oxidase B (MAO-B) inhibitors are still receiving great attention as promising therapeutic agents for central nervous system disorders. This study explores, for the first time, the potential of 3-thiophenylcoumarins as in vitro and in vivo agents against Parkinsońs disease
2024-01-29T08:07:43Z
2020
journal article
Bioorganic Chemistry 101 (2020) 103986
0045-2068
http://hdl.handle.net/10347/32010
10.1016/j.bioorg.2020.103986
1090-2120
eng
https://doi.org/10.1016/j.bioorg.2020.103986
open access
CC BY-NC-ND
Elsevier Inc.
oai:minerva.usc.es:10347/227002020-05-30T02:01:13Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227com_10347_2926com_10347_2891col_10347_12265col_10347_15773
Modeling the OEC with two new biomimetic models: preparations, structural characterization, and water photolysis studies of a Ba–Mn box type complex and a Mn4N6 Planar-diamond cluster
Rouco Méndez, Lara
Fernández García, María Isabel
Pedrido Castiñeiras, Rosa María
Botana López, Luis Miguel
Esteban Gómez, David
Platas Iglesias, Carlos
Maneiro Maneiro, Marcelino
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Artificial photosynthesis
Photocatalyst
Water splitting
Manganese
The oxygen-evolving complex (OEC) is the native enzyme that catalyzes the oxidation of water in natural photosynthesis. Two new classes of manganese cluster complexes of formula Ba2Mn2L12(H3L1)2(CH3OH)4 1 and Mn4L26Cl2 2 were prepared (H4L1 = N,N′-(ethane-1,2-diyl)bis(2-hydroxybenzamide); L2 = methyl picolinimidate) and characterized by standard techniques including microanalysis, IR spectroscopy, ESI spectrometry, and magnetic susceptibility measurements. X-ray diffraction studies of these complexes revealed (i) a box-type structure for 1 formed by two redox-active manganese(III) ions and two barium(II) ions connected by two bridging bisamido-bisphenoxy ligand molecules; and (ii) a planar-diamond array for Mn4N6 cluster 2 where the picolinimidates act as chelating ligands through the two nitrogen atoms. The ability of 1 and 2 to split water has been studied by means of water photolysis experiments. In these experiments, the oxygen evolution was measured in aqueous media in the presence of p-benzoquinone (acting as the hydrogen acceptor), the reduction of which was followed by UV-spectroscopy. The relevant photolytic activity found for 1 is in contrast to the inactivity of 2 in the photolytic experiments. This different behavior is discussed on the basis of the structure of the biomimetic models and the proposed reaction mechanism for this process supported by DFT calculations
2020-05-29T17:54:56Z
2020-05-29T17:54:56Z
2018
journal article
Rouco, L.; Fernández-García, M.I.; Pedrido, R.; Botana, L.M.; Esteban-Gómez, D.; Platas-Iglesias, C.; Maneiro, M. Modeling the OEC with Two New Biomimetic Models: Preparations, Structural Characterization, and Water Photolysis Studies of a Ba–Mn Box Type Complex and a Mn4N6 Planar-Diamond Cluster. Catalysts 2018, 8, 382
http://hdl.handle.net/10347/22700
10.3390/catal8090382
2073-4344
eng
https://doi.org/10.3390/catal8090382
http://creativecommons.org/licenses/by/4.0/
open access
© 2018 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/)
MDPI
oai:minerva.usc.es:10347/303872023-07-10T06:11:34Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Diabetic eye: associated diseases, drugs in clinic, and role of self-assembled carriers in topical treatment
Kattar, Axel
Concheiro Nine, Ángel Joaquín
Álvarez Lorenzo, Carmen Isabel
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Diabetic eye
Topical ocular delivery
Liposomes
Polymeric micelles
Niosomes
Clinical trials
Introduction: Diabetes is a pandemic disease that causes relevant ocular pathologies. Diabetic retinopathy, macular edema, cataracts, glaucoma, or keratopathy strongly impact the quality of life of the patients. In addition to glycemic control, intense research is devoted to finding more efficient ocular drugs and improved delivery systems that can overcome eye barriers. Areas covered: The aim of this review is to revisit first the role of diabetes in the development of chronic eye diseases. Then, commercially available drugs and new candidates in clinical trials are tackled together with the pros and cons of their administration routes. Subsequent sections deal with self-assembled drug carriers suitable for eye instillation combining patient-friendly administration with high ocular bioavailability. Performance of topically administered polymeric micelles, liposomes, and niosomes for the management of diabetic eye diseases is analyzed in the light of ex vivo and in vivo results and outcomes of clinical trials. Expert opinion: Self-assembled carriers are being shown useful for efficient delivery of not only a variety of small drugs but also macromolecules (e.g. antibodies) and genes. Successful design of drug carriers may offer alternatives to intraocular injections and improve the treatment of both anterior and posterior segments diabetic eye diseases
2023-03-27T11:01:17Z
2023-03-27T11:01:17Z
2021
journal article
Expert Opinion on Drug Delivery, 18:11, 1589-1607 (2021)
1742-5247
http://hdl.handle.net/10347/30387
10.1080/17425247.2021.1953466
eng
https://doi.org/10.1080/17425247.2021.1953466
info:eu-repo/grantAgreement/EC/H2020/813440-ORBITAL-Ocular Research by Integrated Training and Learning
http://creativecommons.org/licenses/by-nc-nd/4.0/
open access
© 2021 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. This is an Open Access article distributed under the terms of the Creative Commons Attribution-NonCommercial-NoDerivatives License (http://creativecommons.org/licenses/by-nc-nd/4.0/), which permits non-commercial re-use, distribution, and reproduction in any medium, provided the original work is properly cited, and is not altered, transformed, or built upon in any way
Taylor & Francis
oai:minerva.usc.es:10347/210602023-07-10T06:18:04Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Structure elucidation and biological evaluation of Maitotoxin-3, a Homologue of Gambierone, from Gambierdiscus belizeanus
Boente Juncal, Andrea
Álvarez, Mercedes
Antelo Queijo, Álvaro
Rodríguez Filgueiras, Inés
Calabro, Kevin
Vale González, María del Carmen
Thomas, Olivier P.
Botana López, Luis Miguel
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
44-methylgambierone
Gambierone
Maitotoxin
Gambierdiscus belizeanus
Cytosolic calcium concentration
Glutamate receptors
Neurotoxicity
Ciguatera
Maitotoxin-3
Gambierdiscus species are the producers of the marine toxins ciguatoxins and maitotoxins which cause worldwide human intoxications recognized as Ciguatera Fish Poisoning. A deep chemical investigation of a cultured strain of G. belizeanus, collected in the Caribbean Sea, led to the identification of a structural homologue of the recently described gambierone isolated from the same strain. The structure was elucidated mainly by comparison of NMR and MS data with those of gambierone and ascertained by 2D NMR data analyses. Gratifyingly, a close inspection of the MS data of the new 44-methylgambierone suggests that this toxin would actually correspond to the structure of maitotoxin-3 (MTX3, m/z 1039.4957 for the protonated adduct) detected in 1994 in a Pacific strain of Gambierdiscus and recently shown in routine monitoring programs. Therefore, this work provides for the first time the chemical identification of the MTX3 molecule by NMR. Furthermore, biological data confirmed the similar activities of both gambierone and 44-methylgambierone. Both gambierone and MTX3 induced a small increase in the cytosolic calcium concentration but only MTX3 caused cell cytotoxicity at micromolar concentrations. Moreover, chronic exposure of human cortical neurons to either gambierone or MTX3 altered the expression of ionotropic glutamate receptors, an effect already described before for the synthetic ciguatoxin CTX3C. However, even when gambierone and MTX3 affected glutamate receptor expression in a similar manner their effect on receptor expression differed from that of CTX3C, since both toxins decreased AMPA receptor levels while increasing N-methyl-d-aspartate (NMDA) receptor protein. Thus, further studies should be pursued to clarify the similarities and differences in the biological activity between the known ciguatoxins and the new identified molecule as well as its contribution to the neurological symptoms of ciguatera
2020-04-01T13:48:14Z
2020-04-01T13:48:14Z
2019
journal article
Boente-Juncal, A.; Álvarez, M.; Antelo, Á.; Rodríguez, I.; Calabro, K.; Vale, C.; Thomas, O.P.; Botana, L.M. Structure Elucidation and Biological Evaluation of Maitotoxin-3, a Homologue of Gambierone, from Gambierdiscus belizeanus. Toxins 2019, 11, 79
http://hdl.handle.net/10347/21060
10.3390/toxins11020079
2072-6651
eng
https://www.mdpi.com/2072-6651/11/2/79
info:eu-repo/grantAgreement/EC/H2020/778069
info:eu-repo/grantAgreement/MINECO/Plan Estatal de Investigación Científica y Técnica y de Innovación 2013-2016/AGL2014-58210-R/ES/EVALUACION DE LA SEGURIDAD ALIMENTARIA DE PRODUCTOS PESQUEROS ASOCIADA A LA PRESENCIA DE TOXINAS MARINAS DE NUEVA APARICION EN AGUAS EUROPEAS
info:eu-repo/grantAgreement/MINECO/Plan Estatal de Investigación Científica y Técnica y de Innovación 2013-2016/AGL2016-78728-R/ES
http://creativecommons.org/licenses/by/4.0/
open access
© 2019 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/)
MDPI
oai:minerva.usc.es:10347/235812023-07-10T06:21:44Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Imprinted Contact Lenses for Ocular Administration of Antiviral Drugs
Varela García, Ángela
Gómez Amoza, José Luis
Concheiro Nine, Ángel Joaquín
Álvarez Lorenzo, Carmen Isabel
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Drug-eluting contact lens
Molecularly imprinted hydrogel
Antiviral drug
Sustained release
Cornea penetration
Sclera penetration
A variety of ocular diseases are caused by viruses, and most treatments rely on the use of systemic formulations and eye drops. The efficient ocular barriers that oppose antiviral drug penetration have prompted the development of improved topical delivery platforms. The aim was to design hydrogel contact lenses endowed with an affinity for acyclovir (ACV) and its prodrug valacyclovir (VACV), first-choice drugs against herpes simplex virus (HSV) ocular keratitis, and that can sustain the release of therapeutic doses during daily wearing. Functional monomers suitable for interaction with these drugs were screened using computational modeling. Imprinted and non-imprinted hydrogels were prepared with various contents in the functional monomer methacrylic acid (MAA) and characterized in terms of swelling, transmittance, mechanical properties, and ocular compatibility (hen’s egg test on chorioallantoic membrane (HET-CAM) assay). The values were in the range typical of soft contact lenses. Compared to ACV, the capability to load VACV was remarkably higher due to stronger electrostatic interactions with MAA. The advantages of the imprinting technology were evidenced for VACV. Stability of VACV loading solution/hydrogels under steam heat sterilization and subsequent drug release was investigated. Permeability studies through bovine and porcine cornea and sclera of the drug released from the hydrogels revealed that VACV accumulates in the cornea and can easily cross the sclera, which may facilitate the treatment of both anterior and posterior eye segments diseases
2020-11-06T10:56:47Z
2020-11-06T10:56:47Z
2020
journal article
Varela-Garcia, A.; Gomez-Amoza, J.L.; Concheiro, A.; Alvarez-Lorenzo, C. Imprinted Contact Lenses for Ocular Administration of Antiviral Drugs. Polymers 2020, 12, 2026
http://hdl.handle.net/10347/23581
10.3390/polym12092026
2073-4360
eng
https://doi.org/10.3390/polym12092026
info:eu-repo/grantAgreement/AEI/Plan Estatal de Investigación Científica y Técnica y de Innovación 2017-2020/SAF2017-83118-R/ES/ARQUITECTURAS POLIMERICAS 3D ACTIVAS PARA MEDICINA REGENERATIVA Y TERAPIA LOCALIZADA
http://creativecommons.org/licenses/by/4.0/
open access
© 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/)
Atribución 4.0 Internacional
MDPI
oai:minerva.usc.es:10347/240692021-01-09T03:09:35Zcom_10347_2919com_10347_2891com_10347_2888com_10347_227com_10347_2904com_10347_2890col_10347_10699col_10347_12265
Modeling of the Production of Lipid Microparticles Using PGSS® Technique
López Iglesias, Clara
López Iglesias, Enriqueta
Fernández Pérez, Josefa
Landín Pérez, Mariana
García González, Carlos Alberto
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Universidade de Santiago de Compostela. Departamento de Física Aplicada
Lipid microparticles
PGSS®
Supercritical CO2
Modeling
Solvent-free technology
Solid lipid microparticles (SLMPs) are attractive carriers as delivery systems as they are stable, easy to manufacture and can provide controlled release of bioactive agents and increase their efficacy and/or safety. Particles from Gas-Saturated Solutions (PGSS®) technique is a solvent-free technology to produce SLMPs, which involves the use of supercritical CO2 (scCO2) at mild pressures and temperatures for the melting of lipids and atomization into particles. The determination of the key processing variables is crucial in PGSS® technique to obtain reliable and reproducible microparticles, therefore the modelling of SLMPs production process and variables control are of great interest to obtain quality therapeutic systems. In this work, the melting point depression of a commercial lipid (glyceryl monostearate, GMS) under compressed CO2 was studied using view cell experiments. Based on an unconstrained D-optimal design for three variables (nozzle diameter, temperature and pressure), SLMPs were produced using the PGSS® technique. The yield of production was registered and the particles characterized in terms of particle size distribution. Variable modeling was carried out using artificial neural networks and fuzzy logic integrated into neurofuzzy software. Modeling results highlight the main effect of temperature to tune the mean diameter SLMPs, whereas the pressure-nozzle diameter interaction is the main responsible in the SLMPs size distribution and in the PGSS® production yield
2020-12-17T13:05:40Z
2020-12-17T13:05:40Z
2020
journal article
López-Iglesias, C.; López, E.R.; Fernández, J.; Landin, M.; García-González, C.A. Modeling of the Production of Lipid Microparticles Using PGSS® Technique. Molecules 2020, 25, 4927
http://hdl.handle.net/10347/24069
10.3390/molecules25214927
1420-3049
eng
https://doi.org/10.3390/molecules25214927
http://creativecommons.org/licenses/by/4.0/
open access
© 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/)
Atribución 4.0 Internacional
MDPI
oai:minerva.usc.es:10347/183732020-02-13T14:41:51Zcom_10347_2989com_10347_2889com_10347_227com_10347_2904com_10347_2890com_10347_2888col_10347_9764col_10347_12265
Advances on the formulation of proteins using nanotechnologies
Santalices Ramos, Irene
Gonella, Andrea
Torres López, María Dolores Ramona
Alonso Fernández, María José
Universidade de Santiago de Compostela. Centro de Investigación en Medicina Molecular e Enfermidades Crónicas
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Protein delivery
Peptide delivery
Lipid formulation
Polymeric formulation
Nanocapsule
Nanoparticle
Liposome
Microemulsion
This is the accepted manuscript of the following article: Santalices, I., Gonella, A., Torres, D., & Alonso, M. (2017). Advances on the formulation of proteins using nanotechnologies. Journal Of Drug Delivery Science And Technology, 42, 155-180. doi: 10.1016/j.jddst.2017.06.018
Therapeutic proteins and peptides are very attractive from the pharmaceutical point of view due to their high potency and selectivity. Nonetheless, their instability and low bioavailability make their adminis- tration through non parenteral routes very difficult, a fact that hampers their efficient exploitation in therapeutics. Since the 70's, significant amount of research in the area of drug delivery and nanotech- nology has been done with the final goal of overcoming those hurdles. In particular, biodegradable and biocompatible lipid and polymer-based nanocarriers have emerged as promising delivery platforms to enable the administration of proteins and peptides. This review provides an overview of the mostly explored nanotechnologies to date intended to produce lipidic and polymeric nanocarriers for protein/ peptide delivery. The basic principles of the different techniques are discussed, and the main factors involved in the drug association and release, are analyzed. Finally, a brief overview of the potential applications of these protein/peptide-loaded nanocarriers, highlighting the nanomedicines that have reached the market or the clinical development phase, is provided
2019-03-13T19:07:47Z
2019-03-13T19:07:47Z
2017-12
journal article
Santalices, I., Gonella, A., Torres, D., & Alonso, M. (2017). Advances on the formulation of proteins using nanotechnologies. Journal Of Drug Delivery Science And Technology, 42, 155-180. doi: 10.1016/j.jddst.2017.06.018
1773-2247
http://hdl.handle.net/10347/18373
10.1016/j.jddst.2017.06.018
eng
https://doi.org/10.1016/j.jddst.2017.06.018
open access
© 2017 Elsevier Ltd. This manuscript version is made available under the CC-BY-NC-ND 4.0 license (http://creativecommons.org/licenses/by-nc-nd/4.0/) Attribution-NonCommercial-NoDerivatives 4.0 Internacional
Elsevier
oai:minerva.usc.es:10347/213332020-04-14T02:01:36Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227com_10347_2927com_10347_2891col_10347_12265col_10347_12292
Engineering, on-demand manufacturing, and scaling-up ofpolymeric nanocapsules
Crecente Campo, José
Alonso Fernández, María José
Universidade de Santiago de Compostela. Centro de Investigación en Medicina Molecular e Enfermidades Crónicas
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
High-throughput screening
Layer-by-layer
Microfluidics
Nanocapsules
Particle size
Scale-up
Polymeric nanocapsules are versatile delivery systems with the capacity to load lipophilic drugs in their oily nucleus and hydrophilic drugs in their polymeric shell. The objective of this work was to expand the technological possibilities to prepare customized nanocapsules. First, we adapted the solvent displacement technique to modulate the particle size of the resulting nanocapsules in the 50–500 nm range. We also produced nanosystems with a shell made of one or multiple polymer layers i.e. chitosan, dextran sulphate, hyaluronate, chondroitin sulphate, and alginate. In addition, we identified the conditions to translate the process into a miniaturized high-throughput tailor-made fabrication that enables massive screening of formulations. Finally, the production of the nanocapsules was scaled-up both in a batch production, and also using microfluidics. The versatility of the properties of these nanocapsules and their fabrication technologies is expected to propel their advance from bench to clinic
2020-04-13T20:40:34Z
2020-04-13T20:40:34Z
2019
journal article
Crecente‐Campo, J, Alonso, MJ. Engineering, on‐demand manufacturing, and scaling‐up of polymeric nanocapsules. Bioengineering & Translational Medicine. 2019; 4: 38– 50. https://doi.org/10.1002/btm2.10118
http://hdl.handle.net/10347/21333
10.1002/btm2.1011850
2380-6761
eng
https://doi.org/10.1002/btm2.10118
https://creativecommons.org/licenses/by/4.0/
open access
© 2018 The Authors. Bioengineering & Translational Medicine published by Wiley Periodicals, Inc. on behalf of The American Institute of Chemical Engineers. This is an open access article under the terms of the Creative Commons Attribution License, which permits use, distribution and reproduction in any medium, provided the original work is properly cited
Willey
oai:minerva.usc.es:10347/238182021-01-09T03:02:23Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
A Novel NMDA Receptor Antagonist Protects against Cognitive Decline Presented by Senescent Mice
Companys Alemany, Júlia
Turcu, Andreea L.
Bellver Sanchis, Aina
Loza García, María Isabel
Brea Floriani, José Manuel
Canudas, Anna M.
Leiva, Rosana
Vázquez, Santiago
Pallàs, Mercè
Griñán Ferré, Christian
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
NMDAR antagonist
Cognitive decline
Neurodegeneration
Aging
Alzheimer’s disease
Oxidative stress
BDNF
Apoptosis
Alzheimer’s disease (AD) is the leading cause of dementia. Non-competitive N-Methyl-D-aspartate (NMDA) receptor antagonist memantine improved cognition and molecular alterations after preclinical treatment. Nevertheless, clinical results are discouraging. In vivo efficacy of the RL-208, a new NMDA receptor blocker described recently, with favourable pharmacokinetic properties was evaluated in Senescence accelerated mice prone 8 (SAMP8), a mice model of late-onset AD (LOAD). Oral administration of RL-208 improved cognitive performance assessed by using the three chamber test (TCT), novel object recognition test (NORT), and object location test (OLT). Consistent with behavioural results, RL-208 treated-mice groups significantly changed NMDAR2B phosphorylation state levels but not NMDAR2A. Calpain-1 and Caspase-3 activity was reduced, whereas B-cell lymphoma-2 (BCL-2) levels increased, indicating reduced apoptosis in RL-208 treated SAMP8. Superoxide Dismutase 1 (SOD1) and Glutathione Peroxidase 1 (GPX1), as well as a reduction of hydrogen peroxide (H2O2), was also determined in RL-208 mice. RL-208 treatment induced an increase in mature brain-derived neurotrophic factor (mBDNF), prevented Tropomyosin-related kinase B full-length (TrkB-FL) cleavage, increased protein levels of Synaptophysin (SYN) and Postsynaptic density protein 95 (PSD95). In whole, these results point out to an improvement in synaptic plasticity. Remarkably, RL-208 also decreased the protein levels of Cyclin-Dependent Kinase 5 (CDK5), as well as p25/p35 ratio, indicating a reduction in kinase activity of CDK5/p25 complex. Consequently, lower levels of hyperphosphorylated Tau (p-Tau) were found. In sum, these results demonstrate the neuroprotectant role of RL-208 through NMDAR blockade
2020-11-26T11:11:32Z
2020-11-26T11:11:32Z
2020
journal article
Companys-Alemany, J.; Turcu, A.L.; Bellver-Sanchis, A.; Loza, M.I.; Brea, J.M.; Canudas, A.M.; Leiva, R.; Vázquez, S.; Pallàs, M.; Griñán-Ferré, C. A Novel NMDA Receptor Antagonist Protects against Cognitive Decline Presented by Senescent Mice. Pharmaceutics 2020, 12, 284
http://hdl.handle.net/10347/23818
10.3390/pharmaceutics12030284
1999-4923
eng
https://doi.org/10.3390/pharmaceutics12030284
http://creativecommons.org/licenses/by/4.0/
open access
© 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/)
Atribución 4.0 Internacional
MDPI
oai:minerva.usc.es:10347/238142023-07-10T06:16:59Zcom_10347_2989com_10347_2889com_10347_227com_10347_2904com_10347_2890com_10347_2888col_10347_9764col_10347_12265
Design of Polymeric Nanocapsules for Intranasal Vaccination against Mycobacterium Tuberculosis: Influence of the Polymeric Shell and Antigen Positioning
Diego González, Lara
Crecente Campo, José
Paul, Matthew John
Singh, Mahavir
Reljic, Rajko
Alonso Fernández, María José
González Fernández, África
Simón Vázquez, Rosana
Universidade de Santiago de Compostela. Centro de Investigación en Medicina Molecular e Enfermidades Crónicas
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
6 kDa early secretory antigenic target (ESAT-6)
10 kDa culture filtrate protein (CFP-10)
Vaccination
Imiquimod
Toll-like receptor-7 (TLR-7)
Antibodies
Cytokines
Complement system
Reactive oxygen species (ROS)
Tuberculosis (TB) is the leading cause of death from a single infectious microorganism and Bacillus Calmette Guerin (BCG), the only authorized vaccine, does not confer protection against pulmonary TB. Based on the hypothesis that mucosal protection could help to prevent the infection at the site of entrance, the objective of this work was to develop an intranasal vaccine against Mycobacterium tuberculosis (Mtb), the microorganism that causes TB. Our approach consisted of the use of polymeric nanocapsules (NCs) with an oily core and a polymer shell made of chitosan (CS) or inulin/polyarginine (INU/pArg). The immunostimulant Imiquimod, a Toll-like receptor-7 (TLR-7) agonist, was encapsulated in the oily core and a fusion protein, formed by two antigens of Mtb, was absorbed either onto the NC surface (CS:Ag and INU:pArg:Ag) or between two polymer layers (INU:Ag:pArg) in order to assess the influence of the antigen positioning on the immune response. Although CS NCs were more immunostimulant than the INU/pArg NCs in vitro, the in vivo experiments showed that INU:pArg:Ag NCs were the only prototype inducing an adequate immunoglobulin A (IgA) response. Moreover, a previous immunization with BCG increased the immune response for CS NCs but, conversely, decreased for INU/pArg NCs. Further optimization of the antigen and the vaccination regime could provide an efficacious vaccine, using the INU:pArg:Ag NC prototype as nanocarrier
2020-11-26T11:09:59Z
2020-11-26T11:09:59Z
2020
journal article
Diego-González, L.; Crecente-Campo, J.; Paul, M.J.; Singh, M.; Reljic, R.; Alonso, M.J.; González-Fernández, Á.; Simón-Vázquez, R. Design of Polymeric Nanocapsules for Intranasal Vaccination against Mycobacterium Tuberculosis: Influence of the Polymeric Shell and Antigen Positioning. Pharmaceutics 2020, 12, 489
http://hdl.handle.net/10347/23814
10.3390/pharmaceutics12060489
1999-4923
eng
https://doi.org/10.3390/pharmaceutics12060489
info:eu-repo/grantAgreement/EC/H2020/643558
http://creativecommons.org/licenses/by/4.0/
open access
© 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/)
Atribución 4.0 Internacional
MDPI
oai:minerva.usc.es:10347/294862023-07-10T06:21:41Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Synergistic effect of environmental food pollutants: pesticides and marine biotoxins
Raposo García, Sandra
Costas Sánchez, Celia
Louzao Ojeda, María Carmen
Vale González, María del Carmen
Botana López, Luis Miguel
Universidade de Santiago de Compostela. Departamento de Farmacoloxía
Universidade de Santiago de Compostela. Facultade de Veterinaria
Ciguatoxins
Deltamethrin
Sodium channels
Synergism
Emerging marine biotoxins such as ciguatoxins and pyrethroid compounds, widely used in agriculture, are independently treated as environmental toxicants. Their maximum residue levels in food components are set without considering their possible synergistic effects as consequence of their interaction with the same cellular target. There is an absolute lack of data on the possible combined cellular effects that biological and chemical pollutants, may have. Nowadays, an increasing presence of ciguatoxins in European Coasts has been reported and these toxins can affect human health. Similarly, the increasing use of phytosanitary products for control of food plagues has raised exponentially during the last decades due to climate change. The lack of data and regulation evaluating the combined effect of environmental pollutants with the same molecular target led us to analyse their in vitro effects. In this work, the effects of ciguatoxins and pyrethroids in human sodium channels were investigated. The results presented in this study indicate that both types of compounds have a profound synergistic effect in voltage-dependent sodium channels. These food pollutants act by decreasing the maximum peak inward sodium currents and hyperpolarizing the sodium channels activation, effects that are boosted by the simultaneous presence of both compounds. A fact that highlights the need to re-evaluate their limits in feedstock as well as their potential in vivo toxicity considering that they act on the same cellular target. Moreover, this work sets the cellular basis to further apply this type of studies to other water and food pollutants that may act synergistically and thus implement the corresponding regulatory limits taking into account its presence in a healthy diet
2022-11-30T09:02:26Z
2022-11-30T09:02:26Z
2022
journal article
Science of The Total Environment 858 (2023) 160111
http://hdl.handle.net/10347/29486
10.1016/j.scitotenv.2022.160111
0048-9697
eng
https://doi.org/10.1016/j.scitotenv.2022.160111
info:eu-repo/grantAgreement/AEI/Plan Estatal de Investigación Científica y Técnica y de Innovación 2017-2020/PID 2020-11262RB-C21/ES
info:eu-repo/grantAgreement/EC/H2020 778069-EMERTOX
info:eu-repo/grantAgreement/EC/EAPA-998-2018
info:eu-repo/grantAgreement/EC/EAPA-317-2016
http://creativecommons.org/licenses/by-nc/4.0/
open access
© 2023 The Authors. Published by Elsevier B.V. This work is licenced under a CC Attribution-NonCommercial 4.0 International licence (CC BY-NC 4.0)
Elsevier
oai:minerva.usc.es:10347/299662023-07-10T06:11:12Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
In vitro–in vivo correlation of drug release profiles from medicated contact lenses using an in vitro eye blink model
Mota, Ana F. Pereira da
Vivero López, María
Garg, Piyush
Phan, Chau-Minh
Concheiro Nine, Ángel Joaquín
Jones, Lyndon
Álvarez Lorenzo, Carmen Isabel
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Drug-eluting contact lenses
Eye blink model
In vitro–in vivo correlations
Pravastatin sodium
Resveratrol
There is still a paucity of information on how in vitro release profiles from drug-loaded contact lenses (CLs) recorded in 3D printed eye models correlate with in vivo profiles. This work aims to evaluate the release profiles of two drug-loaded CLs in a 3D in vitro eye blink model and compare the obtained results with the release in a vial and the drug levels in tear fluid previously obtained from an animal in vivo study. In vitro release in the eye model was tested at two different flow rates (5 and 10 µL/min) and a blink speed of 1 blink/10 s. Model CLs were loaded with two different drugs, hydrophilic pravastatin and hydrophobic resveratrol. The release of both drugs was more sustained and lower in the 3D eye model compared to the in vitro release in vials. Interestingly, both drugs presented similar release patterns in the eye model and in vivo, although the total amount of drugs released in the eye model was significantly lower, especially for resveratrol. Strong correlations between percentages of pravastatin released in the eye model and in vivo were found. These findings suggest that the current 3D printed eye blink model could be a useful tool to measure the release of ophthalmic drugs from medicated CLs. Nevertheless, physiological parameters such as the composition of the tear fluid and eyeball surface, tear flow rates, and temperature should be optimized in further studies
2023-01-20T11:58:26Z
2023-01-20T11:58:26Z
2022
journal article
Pereira-da-Mota, A.F., Vivero-Lopez, M., Garg, P. et al. In vitro–in vivo correlation of drug release profiles from medicated contact lenses using an in vitro eye blink model. Drug Deliv. and Transl. Res. (2022). https://doi.org/10.1007/s13346-022-01276-6
2190-393X
http://hdl.handle.net/10347/29966
10.1007/s13346-022-01276-6
2190-3948
eng
https://doi.org/10.1007/s13346-022-01276-6
info:eu-repo/grantAgreement/AEI/Plan Estatal de Investigación Científica y Técnica y de Innovación 2017-2020/PID2020-113881RB-I00/ES
http://creativecommons.org/licenses/by/4.0/
open access
© The Author(s) 2022. This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons licence, and indicate if changes were made. The images or other third party material in this article are included in the article's Creative Commons licence, unless indicated otherwise in a credit line to the material. If material is not included in the article's Creative Commons licence and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this licence, visit http://creativecommons.org/licenses/by/4.0/
Atribución 4.0 Internacional
Springer
oai:minerva.usc.es:10347/183592023-07-10T06:17:01Zcom_10347_2989com_10347_2889com_10347_227com_10347_2904com_10347_2890com_10347_2888col_10347_9764col_10347_12265
Synthetic nanocarriers for the delivery of polynucleotides to the eye
Mendes Saraiva, Sofia
Castro López, Vanessa
Pañeda Vázquez-Prada, Covadonga
Alonso Fernández, María José
Universidade de Santiago de Compostela. Centro de Investigación en Medicina Molecular e Enfermidades Crónicas
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Polynucleotides
Nanocarriers
Ocular polynucleotide delivery
Anterior segment
Posterior segment
Eye
This is the accepted manuscript of the following article: Saraiva, S., Castro-López, V., Pañeda, C., & Alonso, M. (2017). Synthetic nanocarriers for the delivery of polynucleotides to the eye. European Journal Of Pharmaceutical Sciences, 103, 5-18. doi: 10.1016/j.ejps.2017.03.001
This review is a comprehensive analysis of the progress made so far on the delivery of polynucleotide-based therapeutics to the eye, using synthetic nanocarriers. Attention has been addressed to the capacity of different nanocarriers for the specific delivery of polynucleotides to both, the anterior and posterior segments of the eye, with emphasis on their ability to (i) improve the transport of polynucleotides across the different eye barriers; (ii) promote their intracellular penetration into the target cells; (iii) protect them against degradation and, (iv) deliver them in a long-term fashion way. Overall, the conclusion is that despite the advantages that nanotechnology may offer to the area of ocular polynucleotide-based therapies (especially AS-ODN and siRNA delivery), the knowledge disclosed so far is still limited. This fact underlines the necessity of more fundamental and product-oriented research for making the way of the said nanotherapies towards clinical translation
2019-03-13T12:48:49Z
2019-03-13T12:48:49Z
2017-05-30
journal article
Saraiva, S., Castro-López, V., Pañeda, C., & Alonso, M. (2017). Synthetic nanocarriers for the delivery of polynucleotides to the eye. European Journal Of Pharmaceutical Sciences, 103, 5-18. doi: 10.1016/j.ejps.2017.03.001
0928-0987
http://hdl.handle.net/10347/18359
10.1016/j.ejps.2017.03.001
eng
https://doi.org/10.1016/j.ejps.2017.03.001
info:eu-repo/grantAgreement/EC/H2020/642028
http://creativecommons.org/licenses/by-nc-nd/4.0/
open access
© 2017 Elsevier Ltd. This manuscript version is made available under the CC-BY-NC-ND 4.0 license (http://creativecommons.org/licenses/by-nc-nd/4.0/) Attribution-NonCommercial-NoDerivatives 4.0 Internacional
Elsevier
oai:minerva.usc.es:10347/213112023-07-10T06:17:53Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Bromotryptamine and Bromotyramine Derivatives from the Tropical Southwestern Pacific Sponge Narrabeena nigra
Miguel Gordo, María
Gegunde Mosquera, Sandra
Calabro, Kevin
Jennings, Laurence K.
Alfonso Rancaño, María Amparo
Genta-Jouve, Grégory
Vacelet, Jean
Botana López, Luis Miguel
Thomas, Olivier P.
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Futuna
Porifera
Narrabeena
Coral reefs
Aromatic alkaloids
Bromotryptamine
Bromotyramine
Neuroprotective agents
So far, the Futuna Islands located in the Central Indo-Pacific Ocean have not been inventoried for their diversity in marine sponges and associated chemical diversity. As part of the Tara Pacific expedition, the first chemical investigation of the sponge Narrabeena nigra collected around the Futuna Islands yielded 18 brominated alkaloids: seven new bromotryptamine derivatives 1–7 and one new bromotyramine derivative 8 together with 10 known metabolites of both families 9–18. Their structures were deduced from extensive analyses of nuclear magnetic resonance (NMR) and high-resolution mass spectrometry (HRMS) data. In silico metabolite anticipation using the online tool MetWork revealed the presence of a key and minor biosynthetic intermediates. These 18 compounds showed almost no cytotoxic effect up to 10 µM on human neuroblastoma SH-SY5Y and microglia BV2 cells, and some of them exhibited an interesting neuroprotective activity by reducing oxidative damage
2020-04-13T05:40:48Z
2020-04-13T05:40:48Z
2019
journal article
Miguel-Gordo, M.; Gegunde, S.; Calabro, K.; Jennings, L.K.; Alfonso, A.; Genta-Jouve, G.; Vacelet, J.; Botana, L.M.; Thomas, O.P. Bromotryptamine and Bromotyramine Derivatives from the Tropical Southwestern Pacific Sponge Narrabeena nigra. Mar. Drugs 2019, 17, 319
http://hdl.handle.net/10347/21311
10.3390/md17060319
1660-3397
eng
https://doi.org/10.3390/md17060319
info:eu-repo/grantAgreement/EC/H2020/778069
info:eu-repo/grantAgreement/MINECO/Plan Estatal de Investigación Científica y Técnica y de Innovación 2013-2016/AGL2014-58210-R/ES/EVALUACION DE LA SEGURIDAD ALIMENTARIA DE PRODUCTOS PESQUEROS ASOCIADA A LA PRESENCIA DE TOXINAS MARINAS DE NUEVA APARICION EN AGUAS EUROPEAS
info:eu-repo/grantAgreement/MINECO/Plan Estatal de Investigación Científica y Técnica y de Innovación 2013-2016/AGL2016-78728-R/ES
http://creativecommons.org/licenses/by/4.0/
open access
© 2019 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/)
MDPI
oai:minerva.usc.es:10347/232402022-03-31T01:00:08Zcom_10347_2989com_10347_2889com_10347_227com_10347_2904com_10347_2890com_10347_2888col_10347_9764col_10347_12265
mRNA-activated matrices encoding transcription factors as primers of cell differentiation in tissue engineering
Martínez Ledo, Adriana
Senra, Ana
Rilo Álvarez, Héctor
Borrajo Alonso, Erea
Vidal Figueroa, Anxo
Alonso Fernández, María José
García Fuentes, Marcos
Universidade de Santiago de Compostela. Centro de Investigación en Medicina Molecular e Enfermidades Crónicas
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Universidade de Santiago de Compostela. Departamento de Fisioloxía
GAMs
3D transfection
mRNA
Transcription factors
Lineage priming
Tissue engineering
Gene-activated matrices (GAMs) encoding pivotal transcription factors (TFs) represent a powerful tool to direct stem cell specification for tissue engineering applications. However, current TF-based GAMs activated with pDNA, are challenged by their low transfection efficiency and delayed transgene expression. Here, we report a GAM technology activated with mRNAs encoding TFs SOX9 (cartilage) and MYOD (muscle). We find that these mRNA-GAMs induce a higher and faster TF expression compared to pDNA-GAMs, especially in the case of RNase resistant mRNA sequences. This potent TF expression was translated into a high synthesis of cartilage- and muscle-specific markers, and ultimately, into successful tissue specification in vitro. Additionally, we show that the expression of tissue-specific markers can be further modulated by altering the properties of the mRNA-GAM environment. These results highlight the value of this GAM technology for priming cell lineage specification, a key centerpiece for future tissue engineering devices.
2020-07-31T10:50:11Z
2022-03-31T01:00:08Z
2020
journal article
Ledo, A. M., Senra, A., Rilo-Alvarez, H., Borrajo, E., Vidal, A., Alonso, M. J., & Garcia-Fuentes, M. (2020). mRNA-activated matrices encoding transcription factors as primers of cell differentiation in tissue engineering. Biomaterials, 247, 120016-120016.
0142-9612
http://hdl.handle.net/10347/23240
10.1016/j.biomaterials.2020.120016
eng
https://doi.org/10.1016/j.biomaterials.2020.120016
http://creativecommons.org/licenses/by-nc-nd/4.0/
http://creativecommons.org/licenses/by-nc-nd/4.0/
embargoed access
© 2020 Elsevier Ltd. This manuscript version is made available under the CC-BY-NC-ND 4.0 license (http://creativecommons.org/licenses/by-nc-nd/4.0/)
Elsevier
oai:minerva.usc.es:10347/232482020-09-02T02:00:51Zcom_10347_2989com_10347_2889com_10347_227com_10347_2904com_10347_2890com_10347_2888col_10347_9764col_10347_12265
Co-delivery of RNAi and Chemokine by Polyarginine Nanocapsules Enables the Modulation of Myeloid-Derived Suppressor Cells
Martínez Ledo, Adriana
Sasso, Maria A.
Bronte, Vincenzo
Marigo, Ilaria
Boyd, Ben J.
García Fuentes, Marcos
Alonso Fernández, María José
Universidade de Santiago de Compostela. Centro de Investigación en Medicina Molecular e Enfermidades Crónicas
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Nanocapsules
RNAi
C/EBPβ
CCL2
MDSCs
Myeloid-Derived Suppressor Cells (MDSCs), immunosuppressive cells that promote tumor growth, represent an attractive target in cancer immunotherapy. However, the clinical success of this strategy is limited by the lack of efficient drug delivery vehicles targeting this cell compartment. The objective of this work was to develop a delivery carrier, multilayer polymer nanocapsules, with the capacity to co-encapsulate two types of immunomodulatory drugs, a chemokine and an RNAi sequence, aimed at reverting MDSC-mediated immunosuppression. The chemokine CCL2, intended to attract monocyte-macrophage MDSCs, was encapsulated within the L2 inverse micellar aqueous domains of the lipid core of these nanocapsules. On the other hand, two different RNAi sequences that modulate the CCAAT/enhancer-binding protein beta (C/EBPβ) pathway, shC/EBPβ and miR 142-3p, were successfully associated to their polymer shell. These RNAi sequences were covered by subsequent layers of polyarginine and hyaluronic acid, thereby creating multi-layered assemblies that protected them and facilitated their targeted delivery. The in vitro studies performed in primary MDSCs cultures showed the capacity of miR 142-3p-loaded nanocapsules to reduce the highly immunosuppressive monocyte- macrophage subset. Additionally, the encapsulation of CCL2 within the nanocapsules induced a potent monocyte-macrophage chemoattraction that could be used to direct the therapy to these cell subsets. Finally, in vitro and in vivo studies showed the capacity of shC/EBPβ-loaded nanocapsules to downregulate C/EBPβ levels in MDSCs and to reduce monocyte differentiation into tumor-associated macrophages in an MCA-203 fibrosarcoma mice model. In conclusion, the multilayer polymer nanocapsules described here are efficient vehicles for the co-delivery of proteins and RNA, and are potential candidates as nanomedicines for the modulation of MDSCs.
2020-09-01T06:47:33Z
2020-09-01T06:47:33Z
2019
journal article
Journal of Controlled Release. Volume 295, 10 February 2019, Pages 60-73
0168-3659
http://hdl.handle.net/10347/23248
10.1016/j.jconrel.2018.12.041
eng
https://doi.org/10.1016/j.jconrel.2018.12.041
http://creativecommons.org/licenses/by-nc-nd/4.0/
open access
© 2018 Elsevier B.V. This manuscript version is made available under the CC-BY-NC-ND 4.0 license (http://creativecommons.org/licenses/by-nc-nd/4.0/)
Elsevier
oai:minerva.usc.es:10347/160232020-04-11T09:46:22Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Effects of Brassicaceae Isothiocyanates on Prostate Cancer
Novío Mallón, Silvia
CARTEA, ELENA
Soengas, Pilar
Freire Garabal, Manuel
Núñez-Iglesias, María Jesús
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Universidade de Santiago de Compostela. Departamento de Psiquiatría, Radioloxía e Saúde Pública
Angiogenesis
Apoptosis
Carcinogenesis
Cell cycle
Chemoprevention
Epigenetics
Isothiocyanates
Metastasis
Prostate cancer
Therapy resistance
Despite the major progress made in the field of cancer biology, cancer is still one of the leading causes of mortality, and prostate cancer (PCa) is one of the most encountered malignancies among men. The effective management of this disease requires developing better anticancer agents with greater efficacy and fewer side effects. Nature is a large source for the development of chemotherapeutic agents, with more than 50% of current anticancer drugs being of natural origin. Isothiocyanates (ITCs) are degradation products from glucosinolates that are present in members of the family Brassicaceae. Although they are known for a variety of therapeutic effects, including antioxidant, immunostimulatory, anti-inflammatory, antiviral and antibacterial properties, nowadays, cell line and animal studies have additionally indicated the chemopreventive action without causing toxic side effects of ITCs. In this way, they can induce cell cycle arrest, activate apoptosis pathways, increase the sensitivity of resistant PCa to available chemodrugs, modulate epigenetic changes and downregulate activated signaling pathways, resulting in the inhibition of cell proliferation, progression and invasion-metastasis. The present review summarizes the chemopreventive role of ITCs with a particular emphasis on specific molecular targets and epigenetic alterations in in vitro and in vivo cancer animal models
2017-10-21T13:14:57Z
2017-10-21T13:14:57Z
2016-05-12
journal article
Novío, S.; Cartea, M.E.; Soengas, P.; Freire-Garabal, M.; Núñez-Iglesias, M.J. Effects of Brassicaceae Isothiocyanates on Prostate Cancer. Molecules 2016, 21, 626
1420-3049
http://hdl.handle.net/10347/16023
10.3390/molecules21050626
eng
https://doi.org/10.3390/molecules21050626
open access
© 2016 by the authors; licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC-BY) license (http://creativecommons.org/licenses/by/4.0/)
MDPI
oai:minerva.usc.es:10347/235872023-07-10T06:12:31Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
First Detection of Tetrodotoxin in Greek Shellfish by UPLC-MS/MS Potentially Linked to the Presence of the Dinoflagellate Prorocentrum minimum
Vlamis, Aristidis
Katikou, Panagiota
Rodríguez Filgueiras, Inés
Rey López, Verónica
Alfonso Rancaño, María Amparo
Papazachariou, Angelos
Zacharaki, Thetis
Botana López, Ana María
Botana López, Luis Miguel
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Aegean Sea
Emerging biotoxins
Mediterranean Sea
Cultured mussels
Mytilus galloprovincialis
Prorocentrum minimum
Tetrodotoxin
Toxic episode
UPLC-MS/MS
Venerupin shellfish toxin
During official shellfish control for the presence of marine biotoxins in Greece in year 2012, a series of unexplained positive mouse bioassays (MBA) for lipophilic toxins with nervous symptomatology prior to mice death was observed in mussels from Vistonikos Bay–Lagos, Rodopi. This atypical toxicity coincided with (a) absence or low levels of regulated and some non-regulated toxins in mussels and (b) the simultaneous presence of the potentially toxic microalgal species Prorocentrum minimum at levels up to 1.89 × 103 cells/L in the area’s seawater. Further analyses by different MBA protocols indicated that the unknown toxin was hydrophilic, whereas UPLC-MS/MS analyses revealed the presence of tetrodotoxins (TTXs) at levels up to 222.9 μg/kg. Reviewing of official control data from previous years (2006–2012) identified a number of sample cases with atypical positive to asymptomatic negative MBAs for lipophilic toxins in different Greek production areas, coinciding with periods of P. minimum blooms. UPLC-MS/MS analysis of retained sub-samples from these cases revealed that TTXs were already present in Greek shellfish since 2006, in concentrations ranging between 61.0 and 194.7 μg/kg. To our knowledge, this is the earliest reported detection of TTXs in European bivalve shellfish, while it is also the first work to indicate a possible link between presence of the toxic dinoflagellate P. minimum in seawater and that of TTXs in bivalves. Confirmed presence of TTX, a very heat-stable toxin, in filter-feeding mollusks of the Mediterranean Sea, even at lower levels to those inducing symptomatology to humans, indicates that this emerging risk should be seriously taken into account by the EU to protect the health of shellfish consumers
2020-11-06T11:00:57Z
2020-11-06T11:00:57Z
2015
journal article
Vlamis, A.; Katikou, P.; Rodriguez, I.; Rey, V.; Alfonso, A.; Papazachariou, A.; Zacharaki, T.; Botana, A.M.; Botana, L.M. First Detection of Tetrodotoxin in Greek Shellfish by UPLC-MS/MS Potentially Linked to the Presence of the Dinoflagellate Prorocentrum minimum. Toxins 2015, 7, 1779-1807
http://hdl.handle.net/10347/23587
10.3390/toxins7051779
2072-6651
eng
https://doi.org/10.3390/toxins7051779
info:eu-repo/grantAgreement/EC/FP7/312184
http://creativecommons.org/licenses/by/4.0/
open access
© 2015 by the authors; licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/4.0/)
Atribución 4.0 Internacional
MDPI
oai:minerva.usc.es:10347/213222023-07-10T06:17:53Zcom_10347_2989com_10347_2889com_10347_227com_10347_2904com_10347_2890com_10347_2888col_10347_9764col_10347_12265
Polysaccharide nanoparticles can efficiently modulate the immune response against anHIV peptide antigen
Gómez Dacoba, Tamara
Omange, Robert W.
Li, Hongzhao
Crecente Campo, José
Luo, Ma
Alonso Fernández, María José
Universidade de Santiago de Compostela. Centro de Investigación en Medicina Molecular e Enfermidades Crónicas
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
HIV vaccine
Peptide antigen
Polysaccharide
Nanovaccine
Poly(I:C)
Nanoparticle
Antigen encapsulation
The development of an effective HIV vaccine continues to be a major health challenge since, so far, only the RV144 trial has demonstrated a modest clinical efficacy. Recently, the targeting of the 12 highly conserved protease cleavage sites (PCS1–12) has been presented as a strategy seeking to hamper the maturation and infectivity of HIV. To pursue this line of research, and because peptide antigens have low immunogenicity, we have included these peptides in engineered nanoparticles, aiming at overcoming this limitation. More specifically, we investigated whether the covalent attachment of a PCS peptide (PCS5) to polysaccharide-based nanoparticles, and their coadministration with polyinosinic:polycytidylic acid (poly(I:C)), improved the generated immune response. To this end, PCS5 was first conjugated to two different polysaccharides (chitosan and hyaluronic acid) through either a stable or a cleavable bond and then associated with an oppositely charged polymer (dextran sulfate and chitosan) and poly(I:C) to form the nanoparticles. Nanoparticles associating PCS5 by ionic interactions were used in this study as the control formulation. In vivo, all nanosystems elicited high anti-PCS5 antibodies. Nanoparticles containing PCS5 conjugated and poly(I:C) seemed to induce the strongest activation of antigen-presenting cells. Interestingly, T cell activation presented different kinetics depending on the prototype. These findings show that both the nanoparticle composition and the conjugation of the HIV peptide antigen may play an important role in the generation of humoral and cellular responses
2020-04-13T15:22:20Z
2020-04-13T15:22:20Z
2019
journal article
Dacoba T.G., Omange R.W., Li H., Crecente-Campo J., Luo M., Alonso M.J., Polysaccharide nanoparticles can efficiently modulate the immune response against an HIV peptide antigen, ACS Nano, 13, 4947–4959 (2019) (DOI: 10.1021/acsnano.8b07662)
1936-0851
http://hdl.handle.net/10347/21322
10.1021/acsnano.8b07662
1936-086X
eng
https://doi.org/10.1021/acsnano.8b07662
info:eu-repo/grantAgreement/EC/H2020/646142
open access
Copyright © 2019 American Chemical Society. This is an open access article published under an ACS AuthorChoice License, which permits copying and redistribution of the article or any adaptations for non-commercial purposes
American Chemical Society
oai:minerva.usc.es:10347/213912023-07-10T06:21:36Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
High serum cyclophilin C levels as a risk factor marker for coronary artery disease
Alfonso Rancaño, María Amparo
Bayón Lorenzo, Jeremías
Gegunde Mosquera, Sandra
Alonso López, Eva
Alvariño Romero, Rebeca
Santás Álvarez, Melisa
Testa Fernández, Ana
Ríos Vázquez, Ramón
González Juanatey, Carlos
Botana López, Luis Miguel
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Cyclophilins
Coronary artery disease
Cyclophilins (Cyps) are ubiquitous proteins that belong to the immunophilins family consistently
associated with infammatory and cardiovascular diseases. While levels of CypA have been extensively
studied, less data are available for other Cyps. The purpose of this case-control study was to determine
the relationship of Cyps (A, B, C and D) with coronary artery disease (CAD) and eight infammation
markers. Serum levels of Cyps, interleukins and metalloproteinases were measured in serum collected
from 84 subjects. Participants were divided into two sub-groups based on CAD diagnosis: 40 CAD
patients and 44 control volunteers. Serum levels of CypA, CypB and CypC, IL-1β and IL-6 were
signifcantly higher in CAD patients. Bivariate correlation analysis revealed a signifcant positive
correlation between Cyps and several blood and biochemical parameters. When the ability of Cyps levels
for CAD diagnosis was evaluated, higher sensitivity and selectivity values were obtained with CypC
(c-statistic 0.891, p<0.001) indicating that it is a good marker of CAD disease, while less conclusive
results were obtained with CypA (c-statistic 0.748, p<0.001) and CypB (c-statistic 0.655, p<0.014). In
addition, signifcant correlations of traditional CAD risk factors and CypC were observed. In summary,
high levels of CypC are a risk factor for CAD and therefore it can be proposed as a new biomarker for this
disease
2020-04-14T16:36:43Z
2020-04-14T16:36:43Z
2019
journal article
Alfonso, A., Bayón, J., Gegunde, S. et al. High Serum Cyclophilin C levels as a risk factor marker for Coronary Artery Disease. Sci Rep 9, 10576 (2019). https://doi.org/10.1038/s41598-019-46988-x
http://hdl.handle.net/10347/21391
10.1038/s41598-019-46988-x
2045-2322
eng
https://doi.org/10.1038/s41598-019-46988-x
info:eu-repo/grantAgreement/MINECO/Plan Estatal de Investigación Científica y Técnica y de Innovación 2013-2016/AGL2016-78728-R/ES
https://creativecommons.org/licenses/by/4.0/
open access
© The Author(s) 2019. Open Access. This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in a credit line to the material. If material is not included in the article’s Creative Commons license and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this license, visit http://creativecommons.org/licenses/by/4.0/
Nature Publishing Group
oai:minerva.usc.es:10347/306072023-07-10T06:11:22Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Lipidic lyotropic liquid crystals: insights on biomedical applications
Blanco Fernández, Guillermo
Blanco Fernandez, Bárbara
Fernández Ferreiro, Anxo
Otero Espinar, Francisco Javier
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Liquid crystals
Drug delivery
Imaging
Tissue engineering
Glycerol monooleate
Liquid crystals (LCs) possess unique physicochemical properties, translatable into a wide range of applications. To date, lipidic lyotropic LCs (LLCs) have been extensively explored in drug delivery and imaging owing to the capability to encapsulate and release payloads with different characteristics. The current landscape of lipidic LLCs in biomedical applications is provided in this review. Initially, the main properties, types, methods of fabrication and applications of LCs are showcased. Then, a comprehensive discussion of the main biomedical applications of lipidic LLCs accordingly to the application (drug and biomacromolecule delivery, tissue engineering and molecular imaging) and route of administration is examined. Further discussion of the main limitations and perspectives of lipidic LLCs in biomedical applications are also provided
2023-05-26T06:38:43Z
2023-05-26T06:38:43Z
2023
journal article
Advances in Colloid and Interface Science 313 (2023) 102867
http://hdl.handle.net/10347/30607
10.1016/j.cis.2023.102867
0001-8686
eng
https://doi.org/10.1016/j.cis.2023.102867
info:eu-repo/grantAgreement/AEI/Plan Estatal de Investigación Científica y Técnica y de Innovación 2017-2020/RTI2018-099597-B-100
http://creativecommons.org/licenses/by/4.0/
open access
© 2023 The Authors. Published by Elsevier B.V. This is an open access article under the CC BY license (http://creativecommons.org/licenses/by/4.0/)
Elsevier
oai:minerva.usc.es:10347/276872023-07-10T06:11:25Zcom_10347_2989com_10347_2889com_10347_227com_10347_2904com_10347_2890com_10347_2888col_10347_9764col_10347_12265
Nanotechnologies for the delivery of biologicals: historical perspective and current landscape
Durán-Lobato, Matilde
López Estévez, Ana María
Cordeiro, Ana Sara
Gómez Dacoba, Tamara
Crecente Campo, José
Torres López, María Dolores Ramona
Alonso Fernández, María José
Universidade de Santiago de Compostela. Centro de Investigación en Medicina Molecular e Enfermidades Crónicas
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Drug delivery
Protein delivery
Peptide delivery
mAbs
Transmucosal
Oral
Nasal
Vaccine
Oncologicals
Biological macromolecule-based therapeutics irrupted in the pharmaceutical scene generating a great hope due to their outstanding specificity and potency. However, given their susceptibility to degradation and limited capacity to overcome biological barriers new delivery technologies had to be developed for them to reach their targets. This review aims at analyzing the historical seminal advances that shaped the development of the protein/peptide delivery field, along with the emerging technologies on the lead of the current landscape. Particularly, focus is made on technologies with a potential for transmucosal systemic delivery of protein/peptide drugs, followed by approaches for the delivery of antigens as new vaccination strategies, and formulations of biological drugs in oncology, with special emphasis on mAbs. Finally, a discussion of the key challenges the field is facing, along with an overview of prospective advances are provided
2022-03-21T08:47:06Z
2022-03-21T08:47:06Z
2021
journal article
Advanced Drug Delivery Reviews 176 (2021) 113899. https://doi.org/10.1016/j.addr.2021.113899
http://hdl.handle.net/10347/27687
10.1016/j.addr.2021.113899
0169-409X
eng
https://doi.org/10.1016/j.addr.2021.113899
info:eu-repo/grantAgreement/AEI/Plan Estatal de Investigación Científica y Técnica y de Innovación 2017-2020/SAF2017-86634-R/ES/NANO-INMUNOTERAPIAS INTEGRADAS DIRIGIDAS A DIANAS INTRACELULARES RELEVANTES EN CANCER
http://creativecommons.org/licenses/by-nc-nd/4.0/
open access
©2021 The Authors. Published by Elsevier B.V. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/)
Elsevier
oai:minerva.usc.es:10347/329752024-03-21T09:21:42Zcom_10347_2989com_10347_2889com_10347_227com_10347_2904com_10347_2890com_10347_2888com_10347_2908col_10347_9764col_10347_12265col_10347_15764
Vancomycin-loaded methylcellulose aerogel scaffolds for advanced bone tissue engineering
Iglesias Mejuto, Ana
Magariños Ferro, Beatriz
Ferreira Gonçalves, Tânia
Starbird Pérez, Ricardo
Álvarez Lorenzo, Carmen Isabel
Reis, Catarina Pinto
Ardao Palacios, Inés
García González, Carlos Alberto
Universidade de Santiago de Compostela. Centro de Investigación en Medicina Molecular e Enfermidades Crónicas
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Universidade de Santiago de Compostela. Departamento de Microbioloxía e Parasitoloxía
3D-printing
Aerogels
Supercritical sterilization
Vancomycin
Scaffolds grafting combined with local delivery of antibiotics at the injury site may promote bone regeneration along with prevention of infections. In this work, a processing strategy combining the 3D-printing of polysaccharide-based inks with supercritical (sc)CO2 technology was employed to manufacture drug-loaded, nanostructured, and personalized-to-patient aerogels for the first time. Methylcellulose (MC) was employed as graft matrix endowed with nanohydroxyapatite (nHA) to confer bioactivity as required in bone tissue engineering (BTE). MC-nHA aerogels were obtained through the 3D-printing of hydrogel-based scaffolds followed by scCO2 drying. Aerogels were loaded with vancomycin (VAN), an antibiotic employed in the management of bone infections. Textural properties and printing fidelity of scaffolds were studied as well as VAN release, long-term bioactivity, and pre-osteoblasts mineralization. In vitro cell studies and in vivo Artemia salina tests were carried out to evaluate the potential toxicity of the antibiotic-loaded aerogels. Aerogels efficacy in inhibiting bacterial growth was assessed by antimicrobial tests with Staphylococcus aureus. Textural stability of the aerogels after 7 months of storage was also evaluated. Obtained results showed that the scaffolds promoted the intended two-in-one effect (bone repair and infection management simultaneously) in a personalized way, regulating formulation design, drug dose, and porosity
2024-03-04T15:49:20Z
2024-03-04T15:49:20Z
2024
journal article
Carbohydrate Polymers, Volume 324, 2024, 121536
0144-8617
http://hdl.handle.net/10347/32975
10.1016/j.carbpol.2023.121536
eng
https://doi.org/10.1016/j.carbpol.2023.121536
http://creativecommons.org/licenses/by/4.0/
open access
© 2023 The Authors. Published by Elsevier Ltd. This is an open access article under the CC BY license (http://creativecommons.org/licenses/by/4.0/)
Atribución 4.0 Internacional
Elsevier
oai:minerva.usc.es:10347/329862024-03-21T09:21:42Zcom_10347_2989com_10347_2889com_10347_227com_10347_2899com_10347_2890com_10347_2888com_10347_2904com_10347_2912col_10347_9764col_10347_13398col_10347_12265col_10347_13405
Edoxaban treatment in a post-infarction experimental model
Martínez-Fernández, Javier
Almengló Buzón, Cristina
Babarro, Borja
Iglesias Rey, Ramón
García-Caballero Parada, Tomás
Fernández, Ángel L.
Souto Bayarri, José Miguel
González Juanatey, José Ramón
Álvarez Castro, Ezequiel
Universidade de Santiago de Compostela. Centro de Investigación en Medicina Molecular e Enfermidades Crónicas
Universidade de Santiago de Compostela. Departamento de Ciencias Morfolóxicas
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Universidade de Santiago de Compostela. Departamento de Psiquiatría, Radioloxía, Saúde Pública, Enfermaría e Medicina
Edoxaban
Acute myocardial infarction experimental model
Cardiac remodelling after infarction
Cardiac magnetic resonance imaging
Post-infarction anticoagulant treatment
Background
The sequelae of myocardial infarction (MI) require specific pharmacological therapy to minimise the post-MI remodelling, which in many cases evolves into cardiovascular complications. The aim of this study was to analyse the effect of edoxaban, an oral anticoagulant, on cardiac recovery in a rat model of permanent coronary artery ligation.
Methods
An experimental method to assess the post-MI remodelling in rats for 4 weeks, based on cardiac magnetic resonance imaging (MRI) and final histological analysis of the hearts was performed. The influence of daily oral treatment with edoxaban (20 mg/kg/day) for 28 days post-MI was analysed in comparison to vehicle.
Results
In our model, edoxaban was shown to be safe and bleeding was observed in 1 of 10 animals. General physical recovery of the treated animals was shown by higher body weight recovery compared with non-treated animals (38.6 ± 2.9 vs. 29.9 ± 3.1 g, respectively, after 28 days). There was not a pronounced effect of edoxaban in post-MI cardiac remodelling, but mitigated fibrosis was observed by the reduced expression of vascular endothelial growth factor and tumour growth factor β1 in the peri-infarct zone.
Conclusions
Our analysis provided the experimental basis to support the feasibility of MRI to study cardiac function and characterise myocardial scarring in a rat model. Overall data suggested the safety of edoxaban in the model, and compared to placebo, it showed a better post-MI recovery, probably by reducing fibrosis of the heart. Further research on mid-term cardiac recovery with edoxaban after MI is justified.
2024-03-05T09:31:54Z
2024-03-05T09:31:54Z
2024
journal article
European Journal of Pharmacology Volume 962, 5 January 2024, 176216
0014-2999
http://hdl.handle.net/10347/32986
10.1016/j.ejphar.2023.176216
eng
http://creativecommons.org/licenses/by-nc-nd/4.0/
open access
© 2023 The Authors. Published by Elsevier B.V. This is an open access article under the CC BY-NC-ND license
Attribution-NonCommercial-NoDerivatives 4.0 Internacional
Elsevier
oai:minerva.usc.es:10347/290142023-07-10T06:21:40Zcom_10347_2903com_10347_2890com_10347_2888com_10347_227com_10347_2904col_10347_12018col_10347_12265
Lactoferrin-loaded nanostructured lipid carriers (NLCs) as a new formulation for optimized ocular drug delivery
Varela Fernández, Rubén
García Otero, Xurxo
Díaz Tomé, Victoria
Regueiro Lorenzo, Uxía
López López, María Teresa
González Barcia, Miguel
Lema Gesto, María Isabel
Otero Espinar, Francisco Javier
Universidade de Santiago de Compostela. Departamento de Cirurxía e Especialidades Médico-Cirúrxicas
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Nanostructured lipid carriers (NLC)
Double emulsification-solvent evaporation method
Lactoferrin
Ocular drug delivery
Topical ophthalmic administration
Keratoconus
Nanostructured lipid carriers (NLC) are novel lipidic nanosystems that provide significant improvements in terms of high drug loading capacity and controlled drug release. The purpose of the present work was based on the design, development, and physicochemical characterization of lactoferrin-loaded NLCs as a new therapeutic alternative for the keratoconus treatment. Lactoferrin-loaded NLCs were successfully prepared by a double emulsion/solvent evaporation method. The resultant NLC were assessed in terms of particle size, size distribution, surface charge, morphology, encapsulation efficiency (EE), loading capacity (LC), stability, cytotoxicity, in vitro release, and ocular surface retention. Resulting data showed a size of 119.45 ± 11.44 nm, a 0.151 ± 0.045 PDI value and a surface charge of −17.50 ± 2.53 mV. Besides, high EE and LC values were obtained (up to 75%). The in vitro release study demonstrated a lactoferrin controlled release pattern. NLCs were also stable, non-toxic and show mucoadhesive properties. Thus, a consistent preclinical base was obtained, where NLC may be considered as a potential controlled release novel drug delivery system of lactoferrin for the keratoconus treatment
2022-08-05T07:24:55Z
2022-08-05T07:24:55Z
2022
journal article
European Journal of Pharmaceutics and Biopharmaceutics 172 (2022) 144-156
http://hdl.handle.net/10347/29014
10.1016/j.ejpb.2022.02.010
0939-6411
eng
https://doi.org/10.1016/j.ejpb.2022.02.010
info:eu-repo/grantAgreement/AEI/Plan Estatal de Investigación Científica y Técnica y de Innovación 2017-2020/RTI2018-099597-B-100/ES/DESARROLLO DE SISTEMAS BIODEGRADABLES INTRAOCULARES DE ANTIVEGF PARA EL TRATAMIENTO DE LA DEGENERACION MACULAR ASOCIADA A LA EDAD Y A RETINOPATIA DIABETICA
http://creativecommons.org/licenses/by/4.0/
open access
2022 The Author(s). Published by Elsevier B.V. This is an open access article under the CC BY license (https://creativecommons.org/licenses/by/4.0/)
Atribución 4.0 Internacional
Elsevier
oai:minerva.usc.es:10347/247382021-03-13T03:01:54Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Dual-Targeted Hyaluronic Acid/Albumin Micelle-Like Nanoparticles for the Vectorization of Doxorubicin
Curcio, Manuela
Díaz Gómez, Luis Antonio
Cirillo, Giuseppe
Nicoletta, Fiore Pasquale
Leggio, Antonella
Lemma, Francesca
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Hyaluronic acid
Human serum albumin
Polysaccharide-protein conjugate
Micelle-like nanoparticles
Redox-responsive
Active targeting
Cancer therapy
Drug targeting of tumor cells is one of the great challenges in cancer therapy; nanoparticles based on natural polymers represent valuable tools to achieve this aim. The ability to respond to environmental signals from the pathological site (e.g., altered redox potential), together with the specific interaction with membrane receptors overexpressed on cancer cells membrane (e.g., CD44 receptors), represent the main features of actively targeted nanoparticles. In this work, redox-responsive micelle-like nanoparticles were prepared by self-assembling of a hyaluronic acid–human serum albumin conjugate containing cystamine moieties acting as a functional spacer. The conjugation procedure consisted of a reductive amination step of hyaluronic acid followed by condensation with albumin. After self-assembling, nanoparticles with a mean size of 70 nm and able to be destabilized in reducing media were obtained. Doxorubicin-loaded nanoparticles modulated drug release rate in response to different redox conditions. Finally, the viability and uptake experiments on healthy (BALB-3T3) and metastatic cancer (MDA-MB-231) cells proved the potential applicability of the proposed system as a drug vector in cancer therapy
2021-03-12T14:24:58Z
2021-03-12T14:24:58Z
2021
journal article
Pharmaceutics 2021, 13(3), 304; https://doi.org/10.3390/pharmaceutics13030304
http://hdl.handle.net/10347/24738
10.3390/pharmaceutics13030304
1999-4923
eng
https://doi.org/10.3390/pharmaceutics13030304
http://creativecommons.org/licenses/by/4.0/
open access
© 2021 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/)
Atribución 4.0 Internacional
MDPI
oai:minerva.usc.es:10347/300002023-07-10T06:11:36Zcom_10347_2989com_10347_2889com_10347_227com_10347_2988com_10347_2955com_10347_2893com_10347_2888com_10347_2904com_10347_2890col_10347_9764col_10347_11762col_10347_12262col_10347_12265
Mannose-modified hyaluronic acid nanocapsules for the targeting of tumor-associated macrophages
Fernández Mariño, Iago
Anfray, Clément
Crecente Campo, José
Maeda, Akihiro
Ummarino, Aldo
Teijeiro Valiño, Carmen
Blanco Martínez, Darío
Mpambani, Francis
Poul, Laurence
Devalliere, Julie
Germain, Matthieu
Correa Chinea, Juan Francisco
Fernández Villamarín, Marcos
Allavena, Paola
Fernández Megía, Eduardo
Alonso Fernández, María José
Torres Andón, Fernando
Universidade de Santiago de Compostela. Centro de Investigación en Medicina Molecular e Enfermidades Crónicas
Universidade de Santiago de Compostela. Centro de Investigación en Química Biolóxica e Materiais Moleculares
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Universidade de Santiago de Compostela. Departamento de Química Orgánica
Cancer
Hyaluronic acid
Mannose
Polymeric nanocapsules
Nanoprimer
Tumor-associated macrophages
Tumor-associated macrophages (TAMs), a class of immune cells that play a key role in tumor immunosuppression, are recognized as important targets to improve cancer prognosis and treatment. Consequently, the engineering of drug delivery nanocarriers that can reach TAMs has acquired special relevance. This work describes the development and biological evaluation of a panel of hyaluronic acid (HA) nanocapsules (NCs), with different compositions and prepared by different techniques, designed to target macrophages. The results showed that plain HA NCs did not significantly influence the polarization of M0 and M2-like macrophages towards an M1-like pro-inflammatory phenotype; however, the chemical functionalization of HA with mannose (HA-Man) led to a significant increase of NCs uptake by M2 macrophages in vitro and to an improved biodistribution in a MN/MNCA1 fibrosarcoma mouse model with high infiltration of TAMs. These functionalized HA-Man NCs showed a higher accumulation in the tumor compared to non-modified HA NCs. Finally, the pre-administration of the liposomal liver occupying agent Nanoprimer™ further increased the accumulation of the HA-Man NCs in the tumor. This work highlights the promise shown by the HA-Man NCs to target TAMs and thus provides new options for the development of nanomedicine and immunotherapy-based cancer treatments
2023-01-24T12:53:54Z
2023-01-24T12:53:54Z
2022
journal article
Fernández-Mariño, I., Anfray, C., Crecente-Campo, J. et al. Mannose-modified hyaluronic acid nanocapsules for the targeting of tumor-associated macrophages. Drug Deliv. and Transl. Res. (2022). https://doi.org/10.1007/s13346-022-01265-9
2190-393X
http://hdl.handle.net/10347/30000
10.1007/s13346-022-01265-9
2190-3948
eng
https://doi.org/10.1007/s13346-022-01265-9
Info:eu-repo/grantAgreement/EC/H2020/ERA NET EuroNanoMed GA N 723770
http://creativecommons.org/licenses/by/4.0/
open access
© 2022 The Authors. This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons licence, and indicate if changes were made. The images or other third party material in this article are included in the article's Creative Commons licence, unless indicated otherwise in a credit line to the material. If material is not included in the article's Creative Commons licence and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this licence, visit http://creativecommons.org/licenses/by/4.0/
Atribución 4.0 Internacional
Springer
oai:minerva.usc.es:10347/214142020-04-16T02:00:19Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227com_10347_2912col_10347_12265col_10347_13405
Glucosinolate-Degradation Products as Co-Adjuvant Therapy on Prostate Cancer in Vitro
Núñez Iglesias, María Jesús
Novío Mallón, Silvia
García Santiago, Carlota
Pérez Muñuzuri, Elena
Soengas Fernández, María del Pilar
Cartea González, María Elena
Velasco Pazos, Pablo
Freire-Garabal Núñez, Manuel
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Universidade de Santiago de Compostela. Departamento de Psiquiatría, Radioloxía, Saúde Pública, Enfermaría e Medicina
Chemoprevention
Docetaxel
Drug-sensitization
Isothiocyanates
Prostate cancer
Synergism
Glucosinolate-degradation products (GS-degradation products) are believed to be responsible for the anticancer effects of cruciferous vegetables. Furthermore, they could improve the efficacy and reduce side-effects of chemotherapy. The aim of the present study was to determine the cytotoxic effects of GS-degradation products on androgen-insensitive human prostate cancer (AIPC) PC-3 and DU 145 cells and investigate their ability to sensitize such cells to chemotherapeutic drug Docetaxel (DOCE). Cells were cultured under growing concentrations of allyl-isothiocyanate (AITC), sulforaphane (SFN), 4-pentenyl-isothiocyanate (4PI), iberin (IB), indole-3-carbinol (I3C), or phenethyl-isothiocyanate (PEITC) in absence or presence of DOCE. The anti-tumor effects of these compounds were analyzed using the trypan blue exclusion, apoptosis, invasion and RT-qPCR assays and confocal microscopy. We observed that AITC, SFN, IB, and/or PEITC induced a dose- and time-dependent cytotoxic effect on PC-3 and DU 145 cells, which was mediated, at least, by apoptosis and cell cycle arrest. Likewise, we showed that these GS-degradation products sensitized both cell lines to DOCE by synergic mechanisms. Taken together, our results indicate that GS-degradation products can be promising compounds as co-adjuvant therapy in prostate cancer.
2020-04-15T12:53:58Z
2020-04-15T12:53:58Z
2019
journal article
Núñez-Iglesias, M. J., Novío, S., García, C., Pérez-Muñuzuri, E., Soengas, P., Cartea, E., . . . Freire-Garabal, M. (2019). Glucosinolate-degradation products as co-adjuvant therapy on prostate cancer in vitro. International Journal of Molecular Sciences, 20(20), 4977. doi:10.3390/ijms20204977
http://hdl.handle.net/10347/21414
10.3390/ijms20204977
1422-0067
eng
https://doi.org/10.3390/ijms20204977
https://creativecommons.org/licenses/by/4.0/
open access
© 2019 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/)
MDPI
oai:minerva.usc.es:10347/326232024-02-10T01:03:26Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Synthesis and in vitro study of nitro- and methoxy-2-phenylbenzofurans as human Monoamine Oxidase inhibitors
Delogu, Giovanna Lucia
Kumar, Amit
Gatto, Gianluca
Bustelo Paz, Fernando
Saavedra, Lucía M
Rodríguez Franco, María Isabel
Laguna-Francia, Reyes
Viña, Dolores
Universidade de Santiago de Compostela. Centro de Investigación en Medicina Molecular e Enfermidades Crónicas
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
2-Phenylbenzofurans
Monoamine Oxidase Inhibitors
Docking studies
A new series of 2-phenylbenzofuran derivatives were designed and synthesized to
determine relevant structural features for the MAO inhibitory activity and selectivity. Methoxy substituents were introduced in the 2-phenyl ring, whereas the benzofuran moiety was not
substituted or substituted at the positions 5 or 7 with a nitro group. Substitution patterns on
both the phenyl ring and the benzofuran moiety determine the affinity for MAO-A or MAO-B.
The 2-(3-methoxyphenyl)-5-nitrobenzofuran 9 was the most potent MAO-B inhibitor (IC50 =
0.024 μM) identified in this series, whereas 7-nitro-2-phenylbenzofuran 7 was the most
potent MAO-A inhibitor (IC50 = 0.168 μM), both acting as reversible inhibitors. The number
and position of the methoxyl groups on the 2-phenyl ring, have an important influence on
the inhibitory activity. Molecular docking studies confirmed the experimental results and
highlighted the importance of key residues in enzyme inhibition.
2024-02-09T08:33:54Z
2024-02-09T08:33:54Z
2021-01-05
journal article
Delogu, G.L.; Kumar, A.; Gatto, G.; Bustelo, F.; Saavedra, L.M.; Rodríguez-Franco, M.I.; Laguna, R.; Viña, D. Synthesis and in vitro study of nitro- and methoxy-2-phenylbenzofurans as human monoamine oxidase inhibitors. Bioorg. Chem. 2021;107:104616
1090-2120
0045-2068
http://hdl.handle.net/10347/32623
10.1016/j.bioorg.2020.104616
eng
https://doi.org/10.1016/j.bioorg.2020.104616
info:eu-repo/grantAgreement/AEI/Plan Estatal de Investigación Científica y Técnica y de Innovación 2017-2020/RTI2018-093955-B-C21/ES/INNOVADORES COMPUESTOS NEUROGENICOS Y FOTOCONMUTABLES PARA ENFERMEDADES NEUROLOGICAS. DESARROLLO GUIADO POR UNA PLATAFORMA OMICA DE TOXICOLOGIA Y DE MECANISMOS DE ACCION/
https://creativecommons.org/licenses/by-nc-nd/4.0/deed.es
open access
© 2021 Elsevier Inc. All rights reserved
Elsevier
oai:minerva.usc.es:10347/212372020-04-08T02:01:34Zcom_10347_2989com_10347_2889com_10347_227com_10347_2904com_10347_2890com_10347_2888col_10347_9764col_10347_12265
EU-OPENSCREEN: A Novel Collaborative Approach to Facilitate Chemical Biology
Brennecke, Philip
Rasina, Dace
Aubi, Oscar
Herzog, Katja
Landskron, Johannes
Cautain, Bastien
Vicente, Francisca
Quintana, Jordi
Mestres, Jordi
Stechmann, Bahne
Ellinger, Bernhard
Brea Floriani, José Manuel
Kolanowski, Jacek L.
Pilarsk, Radosław
Orzaez, Mar
Pineda-Lucena, Antonio
Laraia, Luca
Nam, Faranak
Zielenkiewicz, Piotr
Paruch, Kamil
Hansen, Espen
Kries, Jens P. von
Neuenschwander, Martin
Specker, Edgar
Bartunek, Petr
Simova, Sarka
Lesnikowski, Zbigniew
Krauss, Stefan
Lehtiö, Lari
Bilitewski, Ursula
Brönstrup, Mark
Taskén, Kjetil
Jirgensons, Aigars
Lickert, Heiko
Clausen, Mads H.
Andersen, Jeanette H.
Vicent, Maria J.
Genilloud, Olga
Martínez, Aurora
Nazaré, Marc
Fecke, Wolfgang
Gribbon, Philip
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Universidade de Santiago de Compostela. Centro de Investigación en Medicina Molecular e Enfermidades Crónicas
Chemical biology
Screening
Medicinal chemistry
Open access
Compound library
Compound screening in biological assays and subsequent optimization of hits is indispensable for the development of new molecular research tools and drug candidates. To facilitate such discoveries, the European Research Infrastructure EU-OPENSCREEN was founded recently with the support of its member countries and the European Commission. Its distributed character harnesses complementary knowledge, expertise, and instrumentation in the discipline of chemical biology from 20 European partners, and its open working model ensures that academia and industry can readily access EU-OPENSCREEN’s compound collection, equipment, and generated data. To demonstrate the power of this collaborative approach, this perspective article highlights recent projects from EU-OPENSCREEN partner institutions. These studies yielded (1) 2-aminoquinazolin-4(3H)-ones as potential lead structures for new antimalarial drugs, (2) a novel lipodepsipeptide specifically inducing apoptosis in cells deficient for the pVHL tumor suppressor, (3) small-molecule-based ROCK inhibitors that induce definitive endoderm formation and can potentially be used for regenerative medicine, (4) potential pharmacological chaperones for inborn errors of metabolism and a familiar form of acute myeloid leukemia (AML), and (5) novel tankyrase inhibitors that entered a lead-to-candidate program. Collectively, these findings highlight the benefits of small-molecule screening, the plethora of assay designs, and the close connection between screening and medicinal chemistry within EU-OPENSCREEN.
2020-04-07T17:56:27Z
2020-04-07T17:56:27Z
2019
journal article
Brennecke, P., Rasina, D., Aubi, O., Herzog, K., Landskron, J., Cautain, B., … Gribbon, P. (2019). EU-OPENSCREEN: A Novel Collaborative Approach to Facilitate Chemical Biology. SLAS DISCOVERY: Advancing the Science of Drug Discovery, 24(3), 398–413. https://doi.org/10.1177/2472555218816276
2472-5552
http://hdl.handle.net/10347/21237
10.1177/2472555218816276
2472-5560
eng
https://doi.org/10.1177/2472555218816276
https://creativecommons.org/licenses/by-nc/4.0/
open access
© 2019 Society for Laboratory. This article is distributed under the terms of the Creative Commons Attribution-NonCommercial 4.0 License
SAGE Publications
oai:minerva.usc.es:10347/271072023-07-10T06:11:28Zcom_10347_2906com_10347_2890com_10347_2888com_10347_227com_10347_2904col_10347_15791col_10347_12265
Single and combined effects of regulated and emerging mycotoxins on viability and mitochondrial function of SH-SY5Y cells
Pérez Fuentes, Nadia
Alvariño Romero, Rebeca
Alfonso Rancaño, María Amparo
González Jartín, Jesús María
Gegunde Mosquera, Sandra
Rodríguez Vieytes, María Mercedes
Botana López, Luis Miguel
Universidade de Santiago de Compostela. Departamento de Farmacoloxía
Universidade de Santiago de Compostela. Departamento de Fisioloxía
Mycotoxin
Emerging
Cytotoxicity
Antagonistic
Apoptosis
Co-occurrence of emerging and regulated mycotoxins in contaminated samples has been widely documented, but studies about their combined toxicity are scarce. In this report, the regulated mycotoxins deoxynivalenol, fumonisin B1 and zearalenone, and the emerging ones enniatin A, enniatin B and beauvericin were tested in SH-SY5Y human neuroblastoma cells. Their individual and binary combined effects on cell viability and mitochondrial function were evaluated. The results with individual mycotoxins revealed that deoxynivalenol and emerging mycotoxins were the most damaging to neuronal cells, presenting IC50 values between 0.35 and 2.4 μM. Interestingly, non-regulated mycotoxins triggered apoptosis by affecting to mitochondrial membrane potential. However, when regulated and non-regulated mycotoxins were binary mixed, antagonistic effects were found in all cases. Finally, cow feed and milk extracts were analysed by UHPLC-MS/MS, detecting the presence of several mycotoxins included in this study. These extracts were tested in neuroblastoma cells, and damaging effects on cell viability were found. Although binary combinations of mycotoxins produced antagonistic effects, their mixture in natural matrixes induces greater effects than expected. Therefore, it would be interesting to explore the matrix influence on mycotoxin toxicity, and to continue studying the neurotoxic mechanism of action of emerging mycotoxins, as they could be a health hazard
2021-11-19T12:15:14Z
2021-11-19T12:15:14Z
2021
journal article
Food and Chemical Toxicology 154 (2021) 112308
0278-6915
http://hdl.handle.net/10347/27107
doi.org/10.1016/j.fct.2021.112308
eng
https://doi.org/10.1016/j.fct.2021.112308
info:eu-repo/grantAgreement/EC/EAPA-317-2016
info:eu-repo/grantAgreement/EC/EAPA-998-2018
info:eu-repo/grantAgreement/EC/H2020/778069-EMERTOX
http://creativecommons.org/licenses/by-nc-nd/4.0/
open access
© 2021 The Author(s). Published by Elsevier Ltd. This is an open access work under the CC BY-NC-ND 4.0 license (https://creativecommons.org/licenses/by-nc-nd/4.0/legalcode)
Attribution-NonCommercial-NoDerivatives 4.0 Internacional
Elsevier
oai:minerva.usc.es:10347/214032021-01-18T08:12:19Zcom_10347_2989com_10347_2889com_10347_227com_10347_2904com_10347_2890com_10347_2888col_10347_9764col_10347_12265
5-HT2 receptor binding, functional activity and selectivity in N-benzyltryptamines
Toro Sazo, Miguel
Brea Floriani, José Manuel
Loza García, María Isabel
Cimadevila Fondevila, Marta
Cassels, Bruce K.
Universidade de Santiago de Compostela. Centro de Investigación en Medicina Molecular e Enfermidades Crónicas
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
N-benzyltryptamines
5-HT2 receptor
The last fifteen years have seen the emergence and overflow into the drug scene of “superpotent” N-benzylated phenethylamines belonging to the “NBOMe” series, accompanied by
numerous research articles. Although N-benzyl substitution of 5-methoxytryptamine is
known to increase its affinity and potency at 5-HT2 receptors associated with psychedelic
activity, N-benzylated tryptamines have been studied much less than their phenethylamine
analogs. To further our knowledge of the activity of N-benzyltryptamines, we have synthesized a family of tryptamine derivatives and, for comparison, a few 5-methoxytryptamine
analogs with many different substitution patterns on the benzyl moiety, and subjected them
to in vitro affinity and functional activity assays vs. the human 5-HT2 receptor subtypes. In
the binding (radioligand displacement) studies some of these compounds exhibited only
modest selectivity for either 5-HT2A or 5-HT2C receptors suggesting that a few of them, with
affinities in the 10–100 nanomolar range for 5-HT2A receptors, might presumably be psychedelic. Unexpectedly, their functional (calcium mobilization) assays reflected very different
trends. All of these compounds proved to be 5-HT2C receptor full agonists while most of
them showed low efficacy at the 5-HT2A subtype. Furthermore, several showed moderateto-strong preferences for activation of the 5-HT2C subtype at nanomolar concentrations.
Thus, although some N-benzyltryptamines might be abuse-liable, others might represent
new leads for the development of therapeutics for weight loss, erectile dysfunction, drug
abuse, or schizophrenia
2020-04-14T18:32:39Z
2020-04-14T18:32:39Z
2019
journal article
Toro-Sazo M, Brea J, Loza MI, Cimadevila M, Cassels BK (2019) 5-HT2 receptor binding, functional activity and selectivity in N-benzyltryptamines. PLoS ONE 14(1): e0209804. https://doi.org/10.1371/journal.pone.0209804
http://hdl.handle.net/10347/21403
10.1371/journal.pone.0209804
1932-6203
eng
https://doi.org/10.1371/journal.pone.0209804
https://creativecommons.org/licenses/by/4.0/
open access
Copyright: © 2019 Toro-Sazo et al. This is an open access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited
PLOS
oai:minerva.usc.es:10347/262572021-05-22T02:05:10Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Ageratum conyzoides L. and Its Secondary Metabolites in the Management of Different Fungal Pathogens
Chahal, Rubal
Nanda, Arun
Küpeli Akkol, Esra
Sobarzo Sánchez, Eduardo Marcelo
Arya, Ashwani
Kaushik, Deepak
Dutt, Rohit
Bhardwaj, Rashmi
Rahman, Md. Habibur
Mittal, Vineet
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Ageratum conyzoides
Fungal pathogens
Clinical applications
Ethnomedicinal uses
Precocene
Toxicity
Ageratum conyzoides L. (Family—Asteraceae) is an annual aromatic invasive herb, mainly distributed over the tropical and subtropical regions of the world. It owns a reputed history of indigenous remedial uses, including as a wound dressing, an antimicrobial, and mouthwash as well as in treatment of dysentery, diarrhea, skin diseases, etc. In this review, the core idea is to present the antifungal potential of the selected medicinal plant and its secondary metabolites against different fungal pathogens. Additionally, toxicological studies (safety profile) conducted on the amazing plant A. conyzoides L. are discussed for the possible clinical development of this medicinal herb. Articles available from 2000 to 2020 were reviewed in detail to exhibit recent appraisals of the antifungal properties of A. conyzoides. Efforts were aimed at delivering evidences for the medicinal application of A. conyzoides by using globally recognized scientific search engines and databases so that an efficient approach for filling the lacunae in the research and development of antifungal drugs can be adopted. After analyzing the literature, it can be reported that the selected medicinal plant effectively suppressed the growth of numerous fungal species, such as Aspergillus, Alternaria, Candida, Fusarium, Phytophthora, and Pythium, owing to the presence of various secondary metabolites, particularly chromenes, terpenoids, flavonoids and coumarins. The possible mechanism of action of different secondary metabolites of the plant against fungal pathogens is also discussed briefly. However, it was found that only a few studies have been performed to demonstrate the plant’s dosage and safety profile in humans. Considered all together, A. conyzoides extract and its constituents may act as a promising biosource for the development of effective antifungal formulations for clinical use. However, in order to establish safety and efficacy, additional scientific research is required to explore chronic toxicological effects of ageratum, to determine the probability of interactions when used with different herbs, and to identify safe dosage. The particulars presented here not only bridge this gap but also furnish future research strategies for the investigators in microbiology, ethno-pharmacology, and drug discovery
2021-05-21T12:54:30Z
2021-05-21T12:54:30Z
2021
journal article
Molecules 2021, 26(10), 2933; https://doi.org/10.3390/molecules26102933
http://hdl.handle.net/10347/26257
10.3390/molecules26102933
1420-3049
eng
https://doi.org/10.3390/molecules26102933
http://creativecommons.org/licenses/by/4.0/
open access
© 2021 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/)
Atribución 4.0 Internacional
MDPI
oai:minerva.usc.es:10347/212192020-04-08T02:01:04Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Design of aerogels, cryogels and xerogels of Alginate: effect of molecular weight, gelation conditions and drying method on particles’ micromeritics
Rodríguez Dorado, Rosalía
López Iglesias, Clara
García González, Carlos Alberto
Auriemma, Giulia
Aquino, Rita P.
Gaudio, Pasquale del
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Aerogel
Alginate
Prilling
Supercritical-CO2
Cryogel
[ENG]Processing and shaping of dried gels are of interest in several fields like alginate aerogel beads used as highly porous and nanostructured particles in biomedical applications. The physicochemical properties of the alginate source, the solvent used in the gelation solution and the gel drying method are key parameters influencing the characteristics of the resulting dried gels. In this work, dried gel beads in the form of xerogels, cryogels or aerogels were prepared from alginates of different molecular weights (120 and 180 kDa) and concentrations (1.25, 1.50, 2.0 and 2.25% (w/v)) using different gelation conditions (aqueous and ethanolic CaCl2 solutions) and drying methods (supercritical drying, freeze-drying and oven drying) to obtain particles with a broad range of physicochemical and textural properties. The stability of physicochemical properties of alginate aerogels under storage conditions of 25 °C and 65% relative humidity (ICH-climatic zone II) during 1 and 3 months was studied. Results showed significant effects of the studied processing parameters on the resulting alginate dried gel properties. Stability studies showed small variations in aerogels weight and specific surface area after 3 months of storage, especially, in the case of aerogels produced with medium molecular weight alginate
2020-04-07T08:49:09Z
2020-04-07T08:49:09Z
2019
journal article
Rodríguez-Dorado, R.; López-Iglesias, C.; García-González, C.A.; Auriemma, G.; Aquino, R.P.; Del Gaudio, P. Design of Aerogels, Cryogels and Xerogels of Alginate: Effect of Molecular Weight, Gelation Conditions and Drying Method on Particles’ Micromeritics. Molecules 2019, 24, 1049
http://hdl.handle.net/10347/21219
10.3390/molecules24061049
1420-3049
eng
https://doi.org/10.3390/molecules24061049
http://creativecommons.org/licenses/by/4.0/
open access
© 2019 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/)
MDPI
oai:minerva.usc.es:10347/292272022-09-20T02:02:40Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Sublingual boosting with a novel mucoadhesive thermogelling hydrogel following parenteral CAF01 priming as a strategy against Chlamydia trachomatis
García del Rio, Lorena
Díaz Rodríguez, Patricia
Pedersen, Gabriel Kristian
Christensen, Dennis
Landin Pérez, Mariana
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Cationic adjuvant liposomes
Mucoadhesive and thermosensitive platforms
Mucosal vaccination
Polymeric networks
Prime-boost strategy
Systemic and sublingual immunization
Chlamydia trachomatis is the most prevalent sexually transmitted disease of bacterial origin. The high number of asymptomatic cases makes it difficult to stop the transmission, requiring vaccine development. Herein, a strategy is proposed to obtain local genital tract immunity against C. trachomatis through parenteral prime and sublingual boost. Subcutaneous administration of chlamydia CTH522 subunit vaccine loaded in the adjuvant CAF01 is combined with sublingual administration of CTH522 loaded in a novel thermosensitive and mucoadhesive hydrogel. Briefly, a ternary optimized hydrogel (OGEL) with desirable biological and physicochemical properties is obtained using artificial intelligence techniques. This formulation exhibits a high gel strength and a strong mucoadhesive, adhesive and cohesive nature. The thermosensitive properties of the hydrogel facilitate application under the tongue. Meanwhile the fast gelation at body temperature together with rapid antigen release should avoid CTH522 leakage by swallowing and increase the contact with sublingual tissue, thus promoting absorption. In vivo studies demonstrate that parenteral-sublingual prime-boost immunization, using CAF01 and OGEL as CTH522 vaccine carriers, shows a tendency to increase cellular (Th1/Th17) immune responses when compared to mucosal or parenteral vaccination alone. Furthermore, parenteral prime with CAF01/CTH522 followed by sublingual boosting with OGEL/CTH522 elicits a local IgA response in the genital tract
2022-09-19T07:30:47Z
2022-09-19T07:30:47Z
2022
journal article
Garcia‐del Rio, L., Diaz‐Rodriguez, P., Pedersen, G. K., Christensen, D., & Landin, M. (2022). Sublingual boosting with a novel mucoadhesive thermogelling hydrogel following parenteral CAF01 priming as a strategy against chlamydia trachomatis. Advanced Healthcare Materials, 11(11). doi:10.1002/adhm.202102508
2192-2640
http://hdl.handle.net/10347/29227
10.1002/adhm.202102508
2192-2659
eng
https://doi.org/10.1002/adhm.202102508
http://creativecommons.org/licenses/by-nc/4.0/
open access
© 2022 The Authors. Advanced Healthcare Materials published by Wiley-VCH GmbH. This is an open access article under the terms of the Creative Commons Attribution-NonCommercial License, which permits use, distribution and reproduction in any medium, provided the original work is properly cited and is not used for commercial purposes
Wiley
oai:minerva.usc.es:10347/217372021-05-20T10:42:09Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
New insights into the causes of human illness due to consumption of azaspiracid contaminated shellfish
Chevallier, Olivier P.
Graham, S. F.
Alonso, E.
Duffy, C.
Silke, J.
Campbell, K.
Botana López, Luis Miguel
Elliot, Christopher T.
Universidade de Santiago de Compostela. Departamento de Farmacia e Tecnoloxía Farmacéutica
Biochemistry
Diseases
Azaspiracid (AZA) poisoning was unknown until 1995 when shellfish harvested in Ireland caused illness
manifesting by vomiting and diarrhoea. Furtherin vivo/vitro studies showed neurotoxicity linked with AZA
exposure. However, the biological target of the toxin which will help explain such potent neurological
activity is still unknown. A region of Irish coastline was selected and shellfish were sampled and tested for
AZA using mass spectrometry. An outbreak was identified in 2010 and samples collected before and after
the contamination episode were compared for their metabolite profile using high resolution mass
spectrometry. Twenty eight ions were identified at higher concentration in the contaminated samples.
Stringent bioinformatic analysis revealed putative identifications for seven compounds including,
glutarylcarnitine, a glutaric acid metabolite. Glutaric acid, the parent compound linked with human
neurological manifestations was subjected to toxicological investigations but was found to have no specific
effect on the sodium channel (as was the case with AZA). However in combination, glutaric acid (1mM) and
azaspiracid (50nM) inhibited the activity of the sodium channel by over 50%. Glutaric acid was subsequently
detected in all shellfish employed in the study. For the first time a viable mechanism for how AZA manifests
itself as a toxin is presented.
2020-04-24T17:02:02Z
2020-04-24T17:02:02Z
2015
journal article
Chevallier, O., Graham, S., Alonso, E. et al. New insights into the causes of human illness due to consumption of azaspiracid contaminated shellfish. Sci Rep 5, 9818 (2015). https://doi.org/10.1038/srep09818
http://hdl.handle.net/10347/21737
10.1038/srep09818
2045-2322
eng
https://doi.org/10.1038/srep09818
https://creativecommons.org/licenses/by/4.0/
open access
© The Author(s) 2015. This work is licensed under a Creative Commons Attribution 4.0 International License. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in the credit line; if the material is not included under the Creative Commons license, users will need to obtain permission from the license holder in order to reproduce the material. To view a copy of this license, visit http://creativecommons.org/licenses/by/4.0/
Nature Publishing Group
oai:minerva.usc.es:10347/325112024-02-08T01:03:08Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Stability studies of starch aerogel formulations for 2 biomedical applications
Santos-Rosales, Víctor
Alvarez Rivera, Gerardo
Hillgärtner, Markus
Cifuentes, Alejandro
Itskov, Mikhail
Rege, Ameya
García González, Carlos Alberto
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Aerogels
Carbohydrates
Morphology
Peptides and proteins,
Scaffolds
This document is the unedited Author’s version of a Submitted Work that was subsequently accepted for publication in Biomacromolecules, copyright © American Chemical Society after peer review. To access the final edited and published work see https://doi.org/10.1021/acs.biomac.0c01414
Starch aerogels are attractive materials for biomedical applications because of their low density and high open porosity coupled with high surface areas. However, the lack of macropores in conventionally manufactured polysaccharide aerogels is a limitation to their use as scaffolds for regenerative medicine. Moreover, the stability under storage of polysaccharide aerogels is critical for biomedical purposes and scarcely studied so far. In this work, the induction of a new macropore population (1–2 μm) well integrated into the starch aerogel backbone was successfully achieved by the incorporation of zein as a porogen. The obtained dual-porous aerogels were evaluated in terms of composition as well as morphological, textural, and mechanical properties. Stability of aerogels upon storage mimicking the zone II (25 °C, 65% relative humidity) according to the International Council for Harmonization guideline of climatic conditions was checked after 1 and 3 months from morphological, physicochemical, and mechanical perspectives. Zein incorporation induced remarkable changes in the mechanical performance of the end aerogel products and showed a preventive effect on the morphological changes during the storage period
2024-02-07T11:39:01Z
2024-02-07T11:39:01Z
2020
journal article
Santos-Rosales V, Alvarez-Rivera G, Hillgärtner M, Cifuentes A, Itskov M, García-González CA, Rege A. (2020). Stability studies of starch aerogel formulations for biomedical applications. Biomacromlecules, 21(12), pp. 5336-5344
1525-7797
http://hdl.handle.net/10347/32511
10.1021/acs.biomac.0c01414
1526-4602
eng
https://doi.org/10.1021/acs.biomac.0c01414
open access
American Chemical Society
oai:minerva.usc.es:10347/210462020-04-02T02:01:00Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Editorial: Novel Approaches to the Neuropharmacology of Mood Disorders
Caruncho, Héctor J.
Kalynchuk, Lisa E.
Loza García, María Isabel
Olivares, Jose M.
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Antidepressant (AD)
Mood stabilizers
Major depression (MDD)
Bipolar disorder
Biomarker
2020-04-01T11:16:22Z
2020-04-01T11:16:22Z
2019
journal article
Caruncho HJ, Kalynchuk LE, Loza MI and Olivares JM (2019) Editorial: Novel Approaches to the Neuropharmacology of Mood Disorders. Front. Pharmacol. 10:589. doi: 10.3389/fphar.2019.00589
http://hdl.handle.net/10347/21046
10.3389/fphar.2019.00589
1663-9812
eng
https://doi.org/10.3389/fphar.2019.00589
https://creativecommons.org/licenses/by/4.0/
open access
Copyright © 2019 Caruncho, Kalynchuk, Loza and Olivares. This is an openaccess article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms
Frontiers Media
oai:minerva.usc.es:10347/275952023-07-10T06:11:15Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Determination of the toxicity equivalency factors for ciguatoxins using human sodium channels
Raposo García, Sandra
Louzao Ojeda, María Carmen
Fuwa, Haruhiko
Sasaki, Makoto
Vale González, María del Carmen
Botana López, Luis Miguel
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Universidade de Santiago de Compostela. Facultade de Veterinaria
Ciguatoxin
Gambierol
Gambierone
44-Methyl gambierone
Sodium channel
Ciguatoxins (CTXs) which are produced by dinoflagellates of the genus Gambierdiscus and Fukuyoa and share a ladder-shaped polyether structure, are causative compounds of one of the most frequent foodborne illness disease known as ciguatera fish poisoning (CFP). CFP was initially found in tropical and subtropical areas but nowadays the dinoflagellates producers of ciguatoxins had spread to European coasts. Therefore, this raises the need of establishing toxicity equivalency factors for the different compounds that can contribute to ciguatera fish poisoning, since biological methods have been replaced by analytical techniques. Thus, in this work, the effects of six compounds causative of ciguatera, on their main target, the human voltage-gated sodium channels have been analyzed for the first time. The results presented here led to the conclusion that the order of potency was CTX1B, CTX3B, CTX4A, gambierol, gambierone and MTX3. Furthermore, the data indicate that the activation voltage of sodium channels is more sensitive to detect ciguatoxins than their effect on the peak sodium current amplitude
2022-02-22T09:11:21Z
2022-02-22T09:11:21Z
2022
journal article
Food and Chemical Toxicology 160 (2022) 112812
http://hdl.handle.net/10347/27595
10.1016/j.fct.2022.112812
0278-6915
eng
https://doi.org/10.1016/j.fct.2022.112812
info:eu-repo/grantAgreement/AEI/Plan Estatal de Investigación Científica y Técnica y de Innovación 2017-2020/PID 2020-11262RB-C21/ES
info:eu-repo/grantAgreement/EC/H2020-EMERTOX/778069
http://creativecommons.org/licenses/by-nc-nd/4.0/
open access
© 2022 The Authors. Published by Elsevier Ltd. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/)
Attribution-NonCommercial-NoDerivatives 4.0 Internacional
Elsevier
oai:minerva.usc.es:10347/275252022-02-10T03:02:43Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Enhancement in corneal permeability of riboflavin using cyclodextrin derivates complexes as a previous step to transepithelial cross-linking
Conde Penedo, Andrea
Díaz Tomé, Victoria
Fernández Ferreiro, Anxo
González Barcia, Miguel
Otero Espinar, Francisco Javier
Universidade de Santiago de Compostela. Departamento de Farmacoloxía
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Corneal drug delivery
Cornea
Corneal epithelium
Cyclodextrin
Riboflavin
Keratoconus
Corneal cross-linking
Corneal cross-linking has been described as an effective treatment to slow the progression of keratoconus. The standard protocol entails corneal epithelial removal to allow the diffusion of riboflavin into the stroma. Although, de-epithelization can generate risks or complications that transepithelial cross-linking tries to solve or avoid. Different formulations were developed after verifying that hydroxypropyl-β-cyclodextrin (HPβCD) and sulfobuthylether-β-cyclodextrin (SBEβCD) in a 20% concentration, increased the solubility of practically insoluble in water drugs such as riboflavin from 0.12 mg/mL to 0.35 mg/mL and 0.29 mg/mL respectively. These values were higher when chitosan and arginine were added to the formulation, showing solubility of 0.78 mg/mL when HPβCD concentration was not modified. Ex vivo corneal permeability was measured after having kept in contact bovine corneas with intact epithelium for 5 h with the 0.1 mg/mL riboflavin solution, the formulations developed and a reproduced nanoemulsion from another work. Riboflavin’s permeability was increased when cyclodextrins, chitosan, and arginine were part of the formulations, compared to the control drug solution. The best permeability coefficient was reached when riboflavin was combined with 40% (w/v) HPβCD, 0.5% (w/w) arginine, and 0.5% (w/w) chitosan. After having carried out toxicity studies as bovine corneal opacity and permeability (BCOP) and Heńs Egg Test - Chorioallantoic Membrane Test (HET-CAM) it was verified that both, the active ingredients and the excipients of the different formulations were not harmful without generating irritation, loss of transparency or corneal permeability alterations. The results show the great potential of the ocular developed solution for their use in transepithelial cross-linking for keratoconus treatment
2022-02-09T11:34:43Z
2022-02-09T11:34:43Z
2021
journal article
European Journal of Pharmaceutics and Biopharmaceutics 162 (2021) 12-22
http://hdl.handle.net/10347/27525
10.1016/j.ejpb.2021.02.012
0939-6411
eng
https://doi.org/10.1016/j.ejpb.2021.02.012
http://creativecommons.org/licenses/by-nc-nd/4.0/
open access
© 2021 The Authors. Published by Elsevier B.V. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/)
Elsevier
oai:minerva.usc.es:10347/328922024-02-24T01:03:01Zcom_10347_2989com_10347_2889com_10347_227com_10347_2904com_10347_2890com_10347_2888col_10347_9764col_10347_12265
Personalized Cancer Nanomedicine: Overcoming BiologicalBarriers for Intracellular Delivery of Biopharmaceuticals
López Estévez, Ana María
Lapuhs, Philipp
Piñeiro Alonso, Laura
Alonso Fernández, María José
Piñeiro Alonso
Universidade de Santiago de Compostela. Centro de Investigación en Medicina Molecular e Enfermidades Crónicas
Universidade de Santiago de Compostela. Departamento de Farmacoloxía
Cancer
Intracellular
Monoclonal antibody
Nanotechnology
RNA
The success of personalized medicine in oncology relies on using highlyeffective and precise
therapeutic modalities such as small interfering RNA(siRNA) and monoclonal antibodies (mAbs). Unfortunately, the clinicalexploitation of these biological drugs has encountered obstacles inovercoming intricate biological barriers. Drug delivery technologies representa plausible strategy to overcome such barriers, ultimately facilitating theaccess to intracellular domains. Here, an overview of the current landscapeon how nanotechnology has dealt with protein corona phenomena as a firstand determinant biological barrier is presented. This continues with theanalysis of strategies facilitating access to the tumor, along with conceivablemethods for enhanced tumor penetration. As a final step, the cellular barriersthat nanocarriers must confront in order for their biological cargo to reachtheir target are deeply analyzed. This review concludes with a critical analysisand future perspectives of the translational advances in personalizedoncological nanomedicine
2024-02-23T14:05:32Z
2024-02-23T14:05:32Z
2023
journal article
A. M. López-Estévez, P. Lapuhs, L. Pineiro-Alonso, M. J. Alonso, Personalized Cancer Nanomedicine: Overcoming Biological Barriers for Intracellular Delivery of Biopharmaceuticals. Adv. Mater. 2023, 2309355. https://doi.org/10.1002/adma.202309355
0935-9648
http://hdl.handle.net/10347/32892
10.1002/adma.202309355
1521-4095
eng
https://doi.org/10.1002/adma.202309355
http://creativecommons.org/licenses/by-nc-nd/4.0/
open access
© 2023 The Authors. Advanced Materials published by Wiley-VCHGmbH. This is an open access article under the terms of theCreativeCommons Attribution-NonCommercial-NoDerivsLicense
Wiley
oai:minerva.usc.es:10347/219962020-05-05T02:00:56Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Improving the solubility of the antichagasic drug benznidazole through formation of inclusion complexes with cyclodextrins
Sobrinho, José Lamartine Soares
Soares, Mônica Felts de La Roca
Torres Labandeira, Santiago
Alves, Lariza Darlene Santos
Neto, Pedro José Rolim
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Benznidazole
Chagas disease
Inclusion complex and dissolution
This study describes unpublished research on improving the solubility of benznidazole by the formation of an inclusion complex. The cyclodextrins selected were αCD, βCD, γCD, HPβCD, RMβCD and SBβCD. All complexes were obtained in solution, presenting 1:1 stoichiometry according to the phase solubility diagram. The highest association constants were obtained with RMβCD and SBβCD, being selected for attainment of solid state complexes. These were characterized using XRD, SEM and dissolution test. The data obtained suggest the formation of complexes and indicate that these may provide a promising alternative way of developing solid doses of drug with suitable biopharmaceutical properties.
2020-05-04T12:16:43Z
2020-05-04T12:16:43Z
2011
journal article
Sobrinho, José Lamartine Soares, Soares, Mônica Felts de La Roca, Labandeira, Juan Jose Torres, Alves, Lariza Darlene Santos, & Rolim Neto, Pedro José. (2011). Improving the solubility of the antichagasic drug benznidazole through formation of inclusion complexes with cyclodextrins. "Química Nova", 34(9), 1534-1538
0100-4042
http://hdl.handle.net/10347/21996
10.1590/S0100-40422011000900010
1678-7064
eng
https://doi.org/10.1590/S0100-40422011000900010
https://creativecommons.org/licenses/by/4.0/deed.en
open access
This article is licensed under a Creative Commons Attribution License
Sociedade Brasileira de Química
oai:minerva.usc.es:10347/325892024-02-09T01:03:26Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Novel 2-pheynlbenzofuran derivatives as selective butyrylcholinesterase inhibitors for Alzheimer’s disease
Kumar, Amit
Pintus, Francesca
Di Petrillo, Amalia
Matos, Maria João Correia Pinto Carvalho de
Viña, Dolores
Delogu, Francesco
Era, Benedetta
Delogu, Giovanna Lucia
Fais, Antonella
Medda, Rosaria
Caria, Paola
Pieroni, Enrico
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Alzheimer's disease
Butyrylcholinesterase
2-Phenylbenzofuran
Alzheimer’s disease (AD) is a neurodegenerative disorder representing the leading cause of dementia
and is affecting nearly 44 million people worldwide. AD is characterized by a progressive decline in
acetylcholine levels in the cholinergic systems, which results in severe memory loss and cognitive
impairments. Expression levels and activity of butyrylcholinesterase (BChE) enzyme has been
noted to increase significantly in the late stages of AD, thus making it a viable drug target. A series
of hydroxylated 2-phenylbenzofurans compounds were designed, synthesized and their inhibitory
activities toward acetylcholinesterase (AChE) and BChE enzymes were evaluated. Two compounds
(15 and 17) displayed higher inhibitory activity towards BChE with IC50 values of 6.23 μM and 3.57 μM,
and a good antioxidant activity with EC50 values 14.9 μM and 16.7 μM, respectively. The same
compounds further exhibited selective inhibitory activity against BChE over AChE. Computational
studies were used to compare protein-binding pockets and evaluate the interaction fingerprints of the
compound. Molecular simulations showed a conserved protein residue interaction network between
the compounds, resulting in similar interaction energy values. Thus, combination of biochemical and
computational approaches could represent rational guidelines for further structural modification of
these hydroxy-benzofuran derivatives as future drugs for treatment of AD
2024-02-08T12:18:59Z
2024-02-08T12:18:59Z
2018
journal article
Kumar, A.; Pintus, F.; Di Petrillo, A.; Medda, R.; Caria, P.; Matos, M.J.; Viña, D.; Pieroni, E.; Delogu, F.; Era, B.; Delogu, G.L.; Fais, A. Novel 2-pheynlbenzofuran derivatives as selective butyrylcholinesterase inhibitors for Alzheimer's disease. Sci. Rep. 2018;8:4424
http://hdl.handle.net/10347/32589
10.1038/S41598-018-22747-2
2045-2322
eng
https://doi.org/10.1038/s41598-018-22747-2
http://creativecommons.org/licenses/by-nc-nd/4.0/
open access
This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. Te images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in a credit line to the material. If material is not included in the article’s Creative Commons license and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder.
Nature Research
oai:minerva.usc.es:10347/244242021-02-13T03:01:08Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Special Issue: Biopolymers in Drug Delivery and Regenerative Medicine
Starbid Pérez, Ricardo
Gaudio, Pasquale del
García González, Carlos Alberto
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
2021-02-12T11:45:00Z
2021-02-12T11:45:00Z
2021
journal article
Molecules 2021, 26(3), 568; https://doi.org/10.3390/molecules26030568
http://hdl.handle.net/10347/24424
10.3390/molecules26030568
1420-3049
eng
https://doi.org/10.3390/molecules26030568
http://creativecommons.org/licenses/by/4.0/
open access
Copyright: © 2021 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https:// creativecommons.org/licenses/by/ 4.0/)
Atribución 4.0 Internacional
MDPI
oai:minerva.usc.es:10347/293882022-11-10T03:02:44Zcom_10347_2918com_10347_2891com_10347_2888com_10347_227com_10347_2904com_10347_2890com_10347_2930col_10347_13951col_10347_12265col_10347_11711
PET study of intravitreal adalimumab pharmacokinetics in a uveitis rat model
García Otero, Xurxo
Mondelo García, Cristina
Bandín Vilar, Enrique
Gómez Lado, Noemí
Silva Rodríguez, Jesús
Rey Bretal, David
Otero Espinar, María Victoria
Adán Civera, Alfredo
González Barcia, Miguel
Fernández Ferreiro, Anxo
Aguiar Fernández, Pablo
Otero Espinar, Francisco Javier
Fernández Ferreiro, Anxo
Universidade de Santiago de Compostela. Departamento de Estatística, Análise Matemática e Optimización
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Universidade de Santiago de Compostela. Departamento de Zooloxía e Antropoloxía Física
Adalimumab
Anti-TNFα
Pharmacokinetics
Molecular imaging
Positron
Emission Tomography
Endotoxin-induced uveitis
2022-11-09T09:09:36Z
2022-11-09T09:09:36Z
2022
journal article
International Journal of Pharmaceutics 627 (2022) 122261
http://hdl.handle.net/10347/29388
10.1016/j.ijpharm.2022.122261
0378-5173
eng
https://doi.org/10.1016/j.ijpharm.2022.122261
http://creativecommons.org/licenses/by-nc-nd/4.0/
open access
Elsevier
oai:minerva.usc.es:10347/219152020-05-01T02:00:57Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
3D Printed Tablets (Printlets) with Braille and Moon Patterns for Visually Impaired Patients
Awad, Atheer
Yao, Aliya
Trenfield, Sarah J.
Goyanes Goyanes, Álvaro
Gaisford, Simon
Basit, Abdul W.
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Three-Dimensional Printing
3D Printed Drug Products
Orally Disintegrating Tablets
Personalised Medicines
Personalized Pharmaceuticals
Blindness
Visual Deprivation
Touch-Reading Compliance
Tactile Patterns
Sight Loss
Visual impairment and blindness affects 285 million people worldwide, resulting in a high public health burden. This study reports, for the first time, the use of three-dimensional (3D) printing to create orally disintegrating printlets (ODPs) suited for patients with visual impairment. Printlets were designed with Braille and Moon patterns on their surface, enabling patients to identify medications when taken out of their original packaging. Printlets with different shapes were fabricated to offer additional information, such as the medication indication or its dosing regimen. Despite the presence of the patterns, the printlets retained their original mechanical properties and dissolution characteristics, wherein all the printlets disintegrated within ~5 s, avoiding the need for water and facilitating self-administration of medications. Moreover, the readability of the printlets was verified by a blind person. Overall, this novel and practical approach should reduce medication errors and improve medication adherence in patients with visual impairment
2020-04-30T09:12:50Z
2020-04-30T09:12:50Z
2020
journal article
Awad, A.; Yao, A.; Trenfield, S.J.; Goyanes, A.; Gaisford, S.; Basit, A.W. 3D Printed Tablets (Printlets) with Braille and Moon Patterns for Visually Impaired Patients. Pharmaceutics 2020, 12, 172.
http://hdl.handle.net/10347/21915
10.3390/pharmaceutics12020172
1999-4923
eng
https://doi.org/10.3390/pharmaceutics12020172
http://creativecommons.org/licenses/by/4.0/
open access
© 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/)
MDPI
oai:minerva.usc.es:10347/211982020-09-10T08:24:09Zcom_10347_2989com_10347_2889com_10347_227com_10347_2904com_10347_2890com_10347_2888col_10347_9764col_10347_12265
New flavonoid – N,N-dibenzyl(N-methyl)amine hybrids: Multi-target-directed agents for Alzheimer´s disease endowed with neurogenic properties
Estrada Valencia, Martín
Herrera Arozamena, Clara
Pérez, Concepción
Viña Castelao, María Dolores
Morales García, José A.
Pérez Castillo, Ana
Ramos, Eva
Romero, Alejandro
Laurini, Erik
Prici, Sabrina
Rodríguez Franco, María Isabel
Universidade de Santiago de Compostela. Centro de Investigación en Medicina Molecular e Enfermidades Crónicas
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Multi-target-directed ligands
Neurogenesis
Sigma receptors
Human b-secretase
Human lipoxygenase-5
Human cholinesterases
Alzheimer’s disease
Neurodegenerative diseases
The design of multi-target directed ligands (MTDLs) is a valid approach for obtaining effective drugs for
complex pathologies. MTDLs that combine neuro-repair properties and block the first steps of neurotoxic
cascades could be the so long wanted remedies to treat neurodegenerative diseases (NDs). By linking two
privileged scaffolds with well-known activities in ND-targets, the flavonoid and the N,N-dibenzyl(N-methyl)-
amine (DBMA) fragments, new CNS-permeable flavonoid – DBMA hybrids (1–13) were obtained. They
were subjected to biological evaluation in a battery of targets involved in Alzheimer’s disease (AD) and
other NDs, namely human cholinesterases (hAChE/hBuChE), b-secretase (hBACE-1), monoamine oxidases
(hMAO-A/B), lipoxygenase-5 (hLOX-5) and sigma receptors (r1R/r2R). After a funnel-type screening, 6,7-
dimethoxychromone – DBMA (6) was highlighted due to its neurogenic properties and an interesting
MTD-profile in hAChE, hLOX-5, hBACE-1 and r1R. Molecular dynamic simulations showed the most relevant drug-protein interactions of hybrid 6, which could synergistically contribute to neuronal regeneration
and block neurodegeneration.
2020-04-06T18:10:32Z
2020-04-06T18:10:32Z
2019
journal article
Martín Estrada-Valencia, Clara Herrera-Arozamena, Concepción Pérez, Dolores Viña, José A. Morales-García, Ana Pérez-Castillo, Eva Ramos, Alejandro Romero, Erik Laurini, Sabrina Pricl & María Isabel Rodríguez-Franco (2019). New flavonoid – N,N-dibenzyl(N-methyl)amine hybrids: Multi-target-directed agents for Alzheimer's disease endowed with neurogenic properties, Journal of Enzyme Inhibition and Medicinal Chemistry, 34:1, 712-727
1475-6366
http://hdl.handle.net/10347/21198
10.1080/14756366.2019.1581184
1475-6374
eng
https://doi.org/10.1080/14756366.2019.1581184
https://creativecommons.org/licenses/by/4.0/
open access
© 2019 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited
Taylor & Francis
oai:minerva.usc.es:10347/225042020-05-25T02:00:39Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Combining DOE with neurofuzzy logic for healthy mineral nutrition of pistachio rootstocks in vitro culture
Nezami Alanagh, Esmaeil
Garoosi, Ghasem-Ali
Landín Pérez, Mariana
Gallego, Pedro Pablo
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
DOE
Micropropagation
Health shoots
Neurofuzzy logic
Pistachio rootstock
Physiological disorders
The aim of this study was to determine the effects of Murashige and Skoog (MS) salts on optimal growth of two pistachio rootstocks, P. vera cv. “Ghazvini” and “UCB1” using design of experiments (DOE) and artificial intelligence (AI) tools. MS medium with 14 macro—and micro-elements was used as base point and its concentration varied from 0 to 5 × MS concentrations. Design of experiments (DOE) software was used to generate a five-dimensional design space by categorizing MS salts into five independent factors (NH4NO3, KNO3, mesos, micros and iron), reducing the experimental design space from 3,125 to just 29 treatments. Typical plant growth parameters such as shoot quality (SQ), proliferation rate (PR), shoot length (SL), and some physiological disorders including shoot-tip necrosis (STN) and callus formation at the base of explants (BC) were evaluated for each treatment. The results were successfully modeled using neurofuzzy logic software. The model delivered new insights, by different sets of “IF–THEN” rules, pinpointing the key role of some ion interactions (SO42- × Cl−, K+ × SO42- × EDTA−, and Fe2+ × Cu2+ × NO3-) for SQ, PR, and SL, whilst physiological disorders (STN and BC) were governed mainly by independent ions as Fe2+ and EDTA−, respectively. In our opinion, the methodology and results obtained in this study is extremely useful to understand the effect of mineral nutrients on pistachio in vitro culture, through discovering new complex interactions among macro—and micro-elements which can be implemented to design new media of plant tissue culture and improve healthy plant micropropagation for any plant species
2020-05-24T17:59:49Z
2020-05-24T17:59:49Z
2018
journal article
Nezami-Alanagh E, Garoosi G-A, Landín M and Gallego PP (2018) Combining DOE With Neurofuzzy Logic for Healthy Mineral Nutrition of Pistachio Rootstocks in vitro Culture. Front. Plant Sci. 9:1474. doi: 10.3389/fpls.2018.01474
http://hdl.handle.net/10347/22504
10.3389/fpls.2018.01474
1664-462X
eng
https://doi.org/10.3389/fpls.2018.01474
https://creativecommons.org/licenses/by/4.0/
open access
Copyright © 2018 Nezami-Alanagh, Garoosi, Landín and Gallego. This is an openaccess article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms
Fontiers Media
oai:minerva.usc.es:10347/273892023-07-10T06:10:56Zcom_10347_2919com_10347_2891com_10347_2888com_10347_227com_10347_2904com_10347_2890col_10347_10699col_10347_12265
ZnO nanoparticles coated with oleic acid as additives for a polyalphaolefin lubricant
Mariño Fernández, Fátima
López Iglesias, Enriqueta
Arnosa Prieto, Ángela
González Gómez, Manuel Antonio
Piñeiro Redondo, Yolanda
Rivas Rey, José
Álvarez Lorenzo, Carmen Isabel
Fernández Pérez, Josefa
Universidade de Santiago de Compostela. Departamento de Física Aplicada
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Zinc oxide nanoparticles
Nanoparticle surface modification
Oleic acid coating
Nanolubricant
Tribological properties
Lubricant additives
In this work, ZnO nanoparticles (NPs) were successfully synthesized and coated with oleic acid (OA). The mean diameter of these NPs (ZnO-OA) was around 11.5 nm, their core was characterized by XRD and their coating by FTIR and Raman. Homogeneous dispersions at different concentrations (0.10, 0.25, 0.50, 0.75 and 1.00 wt%) of ZnO-OA in polyalphaolefin 40 (PAO40) oil were thermophysically and tribologically characterized. Both density and viscosity values increased with the concentration of NPs, reaching relative increments of 0.5% and 4.0%, respectively, for the 1 wt% nanodispersion. Tribological tests were performed at 353.15 K using an Anton Paar MCR 302 rheometer equipped with a tribological ball-on three-pins configuration testing module. Regarding the tribological behavior, the optimal concentration was 0.25 wt% of ZnO-OA (25% of reduction in the friction coefficient and 82% wear reduction in terms of cross sectional area, respect to those obtained with the neat base oil). The rolling mechanism owing to the spherical shape of the nanoadditives, transforming sliding friction into rolling friction, and the mending effect could explain the better tribological performance of nanolubricants with respect to that of neat PAO40. In addition, the presence of PAO40, ZnO-OA NPs and iron oxides was evidenced from confocal Raman microscopy on the worn surfaces obtained from tribological test with PAO40 + 0.25 wt% ZnO-OA dispersion
2022-01-25T12:13:09Z
2022-01-25T12:13:09Z
2022
journal article
Journal of Molecular Liquids 348 (2022) 118401
0167-7322
http://hdl.handle.net/10347/27389
10.1016/j.molliq.2021.118401
eng
https://doi.org/10.1016/j.molliq.2021.118401
info:eu-repo/grantAgreement/AEI/Plan Estatal de Investigación Científica y Técnica y de Innovación 2013-2016/ENE2017-86425-C2-2-R/ES/LUBRICANTES BASADOS EN NANOADITIVOS AVANZADOS PARA ENGRANAJES Y MOTORES
http://creativecommons.org/licenses/by-nc-nd/4.0/
open access
© 2021 The Author(s). Published by Elsevier B.V. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/)
Attribution-NonCommercial-NoDerivatives 4.0 Internacional
Elsevier
oai:minerva.usc.es:10347/316142024-01-09T01:02:51Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227col_10347_12265
Evaluation of the Protective Effects of Sarains on H2O2-Induced Mitochondrial Dysfunction and Oxidative Stress in SH-SY5Y Neuroblastoma Cells
Alvariño Romero, Rebeca
Alonso López, Eva
Tribalat, Marie-Aude
Gegunde Mosquera, Sandra
Thomas, Olivier P.
Botana López, Luis Miguel
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Universidade de Santiago de Compostela. Departamento de Fisioloxía
Sarains
Oxidative stress
Nrf2
mPTP
Cyclophilin D
Neuroprotection
Sarains are diamide alkaloids isolated from the
Mediterranean sponge Haliclona (Rhizoniera) sarai that have
previously shown antibacterial, insecticidal and anti-fouling
activities. In this study, we examined for the first time the
neuroprotective effects of sarains 1, 2 and A against oxidative
stress in a human neuronal model. SH-SY5Y cells were coincubated with sarains at concentrations ranging from 0.01 to
10 μM, and the well-known oxidant hydrogen peroxide at
150 μM for 6 h and the protective effects of the compounds
were evaluated. Among the sarains tested, sarain A was the
most promising compound, improving mitochondrial function
and decreasing reactive oxygen species levels in human neuroblastoma cells treated with the compound at 0.01, 0.1 and
1 μM. This compound was also able to increase the activity of
the antioxidant enzymes superoxide dismutases by inducing
the translocation of the nuclear factor E2-related factor 2
(Nrf2) to the nucleus at the lower concentrations tested (0.01
and 0.1 μM). Moreover, sarain A at 0.1 and 1 μM blocked the
mitochondrial permeability transition pore (mPTP) opening
through cyclophilin D inhibition. These results suggest that
the protective effects produced by the treatment with sarain
A are related with its ability to block the mPTP and to enhance
the Nrf2 pathway, indicating that sarain A may be a candidate
compound for further studies in neurodegenerative diseases
2023-12-20T13:15:50Z
2023-12-20T13:15:50Z
2017
journal article
Alvariño, R., Alonso, E., Tribalat, MA. et al. Evaluation of the Protective Effects of Sarains on H2O2-Induced Mitochondrial Dysfunction and Oxidative Stress in SH-SY5Y Neuroblastoma Cells. Neurotox Res 32, 368–380 (2017)
http://hdl.handle.net/10347/31614
10.1007/s12640-017-9748-3
1476-3524
eng
https://doi.org/10.1007/s12640-017-9748-3
info:eu-repo/grantAgreement/MINECO//AGL2014-58210-R/ES/EVALUACION DE LA SEGURIDAD ALIMENTARIA DE PRODUCTOS PESQUEROS ASOCIADA A LA PRESENCIA DE TOXINAS MARINAS DE NUEVA APARICION EN AGUAS EUROPEAS/
info:eu-repo/grantAgreement/MINECO//PI16%2F01830/ES/PAPEL DE LAS CICLOFILINAS Y SU RECEPTOR EMPRIM (CD147) EN LAS ENFERMEDADES ATEROSCLERÓTICAS Y SU MODULACIÓN CON COMPUESTOS DE ORIGEN MARINO/
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info:eu-repo/grantAgreement/EC/FP7/312184/EU
http://creativecommons.org/licenses/by/4.0/
open access
Atribución 4.0 Internacional
Springer
oai:minerva.usc.es:10347/290402023-07-10T06:11:15Zcom_10347_2904com_10347_2890com_10347_2888com_10347_227com_10347_2908col_10347_12265col_10347_15764
Supercritical CO2 sterilization: an effective treatment to reprocess FFP3 face masks and to reduce waste during COVID-19 pandemic
Santos Rosales, Víctor
López Iglesias, Clara
Sampedro Viana, Ana
Álvarez Lorenzo, Carmen Isabel
Ghazanfari, Samaneh
Magariños Ferro, Beatriz
García-González, Carlos A
Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
Universidade de Santiago de Compostela. Departamento de Microbioloxía e Parasitoloxía
Supercritical carbon dioxide
Sterilization
PPE reprocessing
Face mask
Bacillus pumilus
The outbreak of COVID-19 pandemic unveiled an unprecedented scarcity of personal protective equipment (PPE) available in sanitary premises and for the population worldwide. This situation fostered the development of new strategies to reuse PPE that would ensure sterility and, simultaneously, preserve the filtering properties of the materials. In addition, the reuse of PPEs by reprocessing could reduce the environmental impact of the massive single-use and disposal of these materials. Conventional sterilization techniques such as steam or dry heat, ethylene oxide, and gamma irradiation may alter the functional properties of the PPEs and/or leave toxic residues. Supercritical CO2 (scCO2)-based sterilization is herein proposed as a safe, sustainable, and rapid sterilization method for contaminated face masks while preserving their performance. The functional (bacterial filtration efficiency, breathability, splash resistance, straps elasticity) properties of the processed FFP3 face masks were evaluated after 1 and 10 cycles of sterilization. Log-6 sterilization reduction levels were obtained for face masks contaminated with Bacillus pumilus endospores at mild operating conditions (CO2 at 39 °C and 100 bar for 30 min) and with low contents of H2O2 (150 ppm). Physicochemical properties of the FFP3 face masks remained unchanged after reprocessing and differences in efficacy were not observed neither in the filtration tests, following UNE-EN 14683, nor in the integrity of FFP3 filtration after the sterilization process. The herein presented method based on scCO2 technology is the first reported protocol achieving the reprocessing of FFP3 masks up to 10 cycles while preserving their functional properties
2022-08-09T08:46:40Z
2022-08-09T08:46:40Z
2022
journal article
Science of The Total Environment 826 (2022) 154089
0048-9697
http://hdl.handle.net/10347/29040
10.1016/j.scitotenv.2022.154089
eng
https://doi.org/10.1016/j.scitotenv.2022.154089
info:eu-repo/grantAgreement/AEI/Plan Estatal de Investigación Científica y Técnica y de Innovación 2017-2020/PID2020-120010RB-I00/ES/INGENIERIA DE AEROGELES PARA APLICACIONES BIOMEDICAS AVANZADAS
http://creativecommons.org/licenses/by/4.0/
open access
© 2022 The Authors. Published by Elsevier B.V. This is an open access article under the CC BY license (http://creativecommons.org/licenses/by/4.0/)
Atribución 4.0 Internacional
Elsevier
rdf///col_10347_12265/100