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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...
Autores principales: | , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Instituto Nacional de Salud
2019
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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. |
format | Online Article Text |
id | pubmed-7357371 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2019 |
publisher | Instituto Nacional de Salud |
record_format | MEDLINE/PubMed |
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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