Effect of scopoletin on monoamine oxidases and brain amines.
Neurochem Int
; 93: 113-7, 2016 Feb.
Article
em En
| MEDLINE
| ID: mdl-26796202
ABSTRACT
Naturally, occurring compounds with MAO inhibitory property may provide promising lead molecules against neurodegenerative disorders. We report MAO inhibitory activity of a naturally occurring coumarin (validated chemical scaffold as MAO inhibitors), scopoletin. It selectively (and reversibly) inhibits human (Ki = 20.7 µM) and mouse (Ki = 22 µM) MAO-B, â¼3.5 times more selective towards MAO-B than MAO-A. Docking studies revealed its molecular recognition and explained the selectivity mechanism towards MAO isoforms. Scopoletin occupied the hydrophobic aromatic pockets showing favorable interactions for MAO-B; experimental Ki agreed with the predicted Ki. In vivo, scopoletin (80 mg/kg, i.p.) treatment significantly increases dopamine level and decreases its metabolite DOPAC in striatum. Overall, scopoletin is a partially selective MAO-B inhibitor that increases brain dopamine level.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Escopoletina
/
Encéfalo
/
Aminas
/
Monoaminoxidase
Limite:
Animals
Idioma:
En
Revista:
Neurochem Int
Ano de publicação:
2016
Tipo de documento:
Article
País de afiliação:
Índia