α-Glucosidase inhibition by prenylated and lavandulyl compounds from Sophora flavescens roots and in silico analysis.
Int J Biol Macromol
; 102: 960-969, 2017 Sep.
Article
em En
| MEDLINE
| ID: mdl-28455256
ABSTRACT
The enzyme α-glucosidase is a good drug target for the treatment of diabetes mellitus. Four minor flavonoids (1-4) from roots of Sophora flavescens showed the inhibitory activity, with IC50 values ranging from 11.0±0.3 to 50.6±1.3µM, toward α-glucosidase. An enzyme kinetics analysis of them revealed that the compounds 1 and 4 were non-competitive, and compounds 2 and 3 were un-competitive inhibitors. For molecular docking, 3-dimensional structure of α-glucosidase was built by homology modeling. As the result, four compounds 1-4 were confirmed to interact into common binding site of α-glucosidase. In addition, all of the four prenylated and lavandulyl compounds (1-4) were abundant in an ethyl acetate fraction separated from a methanol extract, and the potential inhibitor (3) was extracted best using tetrahydrofuran.
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Base de dados:
MEDLINE
Assunto principal:
Terpenos
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Simulação por Computador
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Extratos Vegetais
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Raízes de Plantas
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Sophora
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Alfa-Glucosidases
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Prenilação
Idioma:
En
Ano de publicação:
2017
Tipo de documento:
Article