8-Propyl-6H-[1,3]dioxolo[4,5-g]chromen-6-one: A new coumarin with monoamine oxidase B inhibitory activity and possible anti-parkinsonian effects
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Title: | 8-Propyl-6H-[1,3]dioxolo[4,5-g]chromen-6-one: A new coumarin with monoamine oxidase B inhibitory activity and possible anti-parkinsonian effects |
Author: | Pilar Olaya, María del Vergel, Nadezdha Esperanza López, Jose Luis Viña Castelao, María Dolores |
Affiliation: | 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 |
Subject: | Parkinson’s disease | Monoamine oxidase B | Coumarin | Mice | Reserpine | Levodopa | Carbidopa | |
Date of Issue: | 2020 |
Publisher: | Universidade de São Paulo |
Citation: | OLAYA, María del Pilar et al. 8-Propyl-6H-[1,3]dioxolo[4,5-g]chromen-6-one: A new coumarin with monoamine oxidase B inhibitory activity and possible anti-parkinsonian effects. Braz. J. Pharm. Sci. [online]. 2020, vol.56 [cited 2020-04-23], e17609. Available from: <http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502020000100508&lng=en&nrm=iso>. Epub Mar 16, 2020. ISSN 2175-9790. https://doi.org/10.1590/s2175-97902019000317609 |
Abstract: | Parkinson’s disease is a common neurodegenerative disorder. In this study, the monoamine oxidase inhibitory activity and potential anti-parkinsonian effects of 8-propyl-6H-[1,3]dioxolo[4,5-g]chromen-6-one (FCS303), a new synthetic coumarin, were evaluated. To do this, we used the reserpine model of Parkinson’s disease, an assay of levodopa/carbidopa potentiation, the catalepsy model of haloperidol, and an in vitro assay against monoamine oxidase (MAO) activity. Additionally, lipid peroxidation and protein carbonyl group quantification was performed in mice brain homogenates previously treated with haloperidol. FCS303 inhibited monoamine oxidase B (MAO-B) with an IC50 of 5.46 ± 0.36 µM; however, there was no effect on monoamine oxidase A (MAO-A). The oral administration of FCS303 led to a significant reversal of hypokinesia in the reserpine model (at 24 h, doses of 100 and 200 mg/kg) and in the levodopa/carbidopa potentiation assay (at 2 and 24 h, dose of 200 mg/kg). In addition, FCS303 (100 mg/kg) showed anti-cataleptic activity against haloperidol. FCS303 (50 mg/kg) significantly decreased lipid peroxidation and protein carbonyl quantification. These results suggest that FCS303 could present anti-parkinsonian activity related to MAO-B inhibitory activity. |
Publisher version: | https://doi.org/10.1590/s2175-97902019000317609 |
URI: | http://hdl.handle.net/10347/21693 |
DOI: | 10.1590/s2175-97902019000317609 |
ISSN: | 1984-8250 |
E-ISSN: | 2175-9790 |
Rights: | This is an open-access article distributed under the terms of the Creative Commons Attribution License |
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