The inhibition of CYP1A2, CYP2C9, and CYP2D6 by pterostilbene in human liver microsomes.
Pharmazie
; 76(4): 155-158, 2021 04 01.
Article
em En
| MEDLINE
| ID: mdl-33849700
ABSTRACT
This study used human liver microsomes to assess pterostilbene's effect on the metabolic activity of cytochrome P450 (CYP) 1A2, CYP2C9, and CYP2D6. The metabolism of their substrates (phenacetin, tolbutamide, and dextromethorphan) was assayed by quantifying their relevant metabolites by HPLC. The IC50 value was used to express the strength of inhibition, and the value of a volume per dose index (VDI) was used to indicate the metabolic ability of the enzyme. In this study, pterostilbene inhibited CYP1A2, CYP2C9, and CYP2D6's metabolic activities in vitro. CYP2C9's activity was most significantly inhibited by pterostilbene; its IC50 value was 0.12±0.04 µM. The IC50 value of CYP1A2 and CYP2D6 was 56.3±10.4 µM and 62.33±11.4 µM, respectively. The finding that suggests that pterostilbene has the potential to interact with CYP2C9 substrates in vivo. These results warrant clinical studies to assess the in vivo significance of these interactions.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Estilbenos
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Inibidores do Citocromo P-450 CYP1A2
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Inibidores do Citocromo P-450 CYP2C9
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Inibidores do Citocromo P-450 CYP2D6
Idioma:
En
Ano de publicação:
2021
Tipo de documento:
Article