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Coumarin analogue 3-methyl-7H-furo[3,2-g]chromen-7-one as a possible antiparkinsonian agent

INTRODUCTION: Parkinson’s disease is the second most common neurodegenerative disease. Monoamine oxidase B inhibitors are used in the treatment of this disease concomitantly with levodopa or as monotherapy. Several substituted coumarins have shown activity as inhibitors of monoamine oxidase B. OBJEC...

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Autores principales: Olaya, María del Pilar, Vergel, Nadezdha Esperanza, López, José Luis, Viña, María Dolores, Guerrero, Mario Francisco
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Instituto Nacional de Salud 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7357371/
https://www.ncbi.nlm.nih.gov/pubmed/31584763
http://dx.doi.org/10.7705/biomedica.4299
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author Olaya, María del Pilar
Vergel, Nadezdha Esperanza
López, José Luis
Viña, María Dolores
Guerrero, Mario Francisco
author_facet Olaya, María del Pilar
Vergel, Nadezdha Esperanza
López, José Luis
Viña, María Dolores
Guerrero, Mario Francisco
author_sort Olaya, María del Pilar
collection PubMed
description INTRODUCTION: Parkinson’s disease is the second most common neurodegenerative disease. Monoamine oxidase B inhibitors are used in the treatment of this disease concomitantly with levodopa or as monotherapy. Several substituted coumarins have shown activity as inhibitors of monoamine oxidase B. OBJECTIVE: To evaluate the possible antiparkinsonian effects of the coumarin analogue FCS005 (3-methyl-7H-furo[3,2-g]chromen-7-one) in mouse models, as well as its inhibitory activity towards monoamine oxidases (MAO) and its antioxidant activity. MATERIALS AND METHODS: FCS005 was synthesized and the reversal of hypokinesia was evaluated in the reserpine and levodopa models. Moreover, in the haloperidol model, its anticataleptic effects were evaluated. Additionally, the monoamine oxidase inhibitory activity and antioxidant activity of FCS005 were evaluated using in vitro and ex vivo studies, respectively. RESULTS: FCS005 (100 mg/kg) caused the reversal of hypokinesia in the reserpine and levodopa models. This furocoumarin also presented anti-cataleptic effects at the same dose. Besides, it showed selective inhibitory activity towards the MAO-B isoform and antioxidant activity. CONCLUSION: These results attribute interesting properties to the compound FCS005. It is important to continue research on this molecule considering that it could be a potential antiparkinsonian agent.
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spelling pubmed-73573712020-07-20 Coumarin analogue 3-methyl-7H-furo[3,2-g]chromen-7-one as a possible antiparkinsonian agent Olaya, María del Pilar Vergel, Nadezdha Esperanza López, José Luis Viña, María Dolores Guerrero, Mario Francisco Biomedica Articulo Original INTRODUCTION: Parkinson’s disease is the second most common neurodegenerative disease. Monoamine oxidase B inhibitors are used in the treatment of this disease concomitantly with levodopa or as monotherapy. Several substituted coumarins have shown activity as inhibitors of monoamine oxidase B. OBJECTIVE: To evaluate the possible antiparkinsonian effects of the coumarin analogue FCS005 (3-methyl-7H-furo[3,2-g]chromen-7-one) in mouse models, as well as its inhibitory activity towards monoamine oxidases (MAO) and its antioxidant activity. MATERIALS AND METHODS: FCS005 was synthesized and the reversal of hypokinesia was evaluated in the reserpine and levodopa models. Moreover, in the haloperidol model, its anticataleptic effects were evaluated. Additionally, the monoamine oxidase inhibitory activity and antioxidant activity of FCS005 were evaluated using in vitro and ex vivo studies, respectively. RESULTS: FCS005 (100 mg/kg) caused the reversal of hypokinesia in the reserpine and levodopa models. This furocoumarin also presented anti-cataleptic effects at the same dose. Besides, it showed selective inhibitory activity towards the MAO-B isoform and antioxidant activity. CONCLUSION: These results attribute interesting properties to the compound FCS005. It is important to continue research on this molecule considering that it could be a potential antiparkinsonian agent. Instituto Nacional de Salud 2019-09-01 /pmc/articles/PMC7357371/ /pubmed/31584763 http://dx.doi.org/10.7705/biomedica.4299 Text en https://creativecommons.org/licenses/by/4.0/ This is an open-access article distributed under the terms of the Creative Commons Attribution License
spellingShingle Articulo Original
Olaya, María del Pilar
Vergel, Nadezdha Esperanza
López, José Luis
Viña, María Dolores
Guerrero, Mario Francisco
Coumarin analogue 3-methyl-7H-furo[3,2-g]chromen-7-one as a possible antiparkinsonian agent
title Coumarin analogue 3-methyl-7H-furo[3,2-g]chromen-7-one as a possible antiparkinsonian agent
title_full Coumarin analogue 3-methyl-7H-furo[3,2-g]chromen-7-one as a possible antiparkinsonian agent
title_fullStr Coumarin analogue 3-methyl-7H-furo[3,2-g]chromen-7-one as a possible antiparkinsonian agent
title_full_unstemmed Coumarin analogue 3-methyl-7H-furo[3,2-g]chromen-7-one as a possible antiparkinsonian agent
title_short Coumarin analogue 3-methyl-7H-furo[3,2-g]chromen-7-one as a possible antiparkinsonian agent
title_sort coumarin analogue 3-methyl-7h-furo[3,2-g]chromen-7-one as a possible antiparkinsonian agent
topic Articulo Original
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7357371/
https://www.ncbi.nlm.nih.gov/pubmed/31584763
http://dx.doi.org/10.7705/biomedica.4299
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