Natural phosphodiesterase-4 (PDE4) inhibitors from Crotalaria ferruginea.
Fitoterapia
; 94: 177-82, 2014 Apr.
Article
em En
| MEDLINE
| ID: mdl-24594242
ABSTRACT
Bioassay-guided fractionation of the ethanol extract of the Chinese folk medicine Crotalaria ferruginea led to the isolation of a new isoflavonoid, 4'-hydroxy-2'-methylalpinum-isoflavone (1), and eight known analogs (2-9). Their structures were elucidated by spectroscopic analysis. Compounds 1, 2, 5, and 8 showed inhibitory activities against phosphodiesterase-4 (PDE4), a therapeutic target of asthma, with IC50 values ranging from 2.57 to 8.94 µM. The possible action mechanism and the structure-activity relationship (SAR) of the active isoflavonoids were explored by using molecular docking and molecular dynamics (MD) simulation methods. Our study herein may explain the anti-inflammatory function of this plant in Chinese folk medicine.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Extratos Vegetais
/
Crotalaria
/
Inibidores da Fosfodiesterase 4
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Isoflavonas
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Anti-Inflamatórios
Tipo de estudo:
Diagnostic_studies
Idioma:
En
Revista:
Fitoterapia
Ano de publicação:
2014
Tipo de documento:
Article
País de afiliação:
China