Document Detail

Inhibitory effects of polyphenols on human cytochrome P450 3A4 and 2C9 activity.
MedLine Citation:
PMID:  19883715     Owner:  NLM     Status:  MEDLINE    
Polyphenols present in foods and supplements may contribute to human health by preventing cardiovascular diseases and cancer. Drug-food or drug-herb interactions have recently come into focus but, except for some phytochemicals, few components of food or herbs participate in such interactions. In this study, we systematically evaluated the inhibitory effects of 60 polyphenols and related compounds on human cytochrome P450 (CYP) 3A4 and CYP2C9 activity by in vitro assay to investigate whether some polyphenols induce drug interactions. In addition, the kinetics of potent CYP inhibitors was investigated by Lineweaver-Burk plot analysis. Three coumarins and 12 flavonoids significantly suppressed CYP3A4 or CYP2C9 activities. Lineweaver-Burk plot analysis indicated that apigenin and its dimer amentoflavone and imperatorin displayed a mixed type of inhibition on CYP3A4 or CYP2C9. Among the inhibitors, amentoflavone was the most potent inhibitor of CYP3A4 and CYP2C9 activities with IC(50) values of 0.07 and 0.03 microM, respectively. The K(i) value of amentoflavone was significantly lower than that of the CYP2C9 inhibition positive control sulfaphenazole. These findings suggest that some dietary polyphenols may have the potential to inhibit the metabolism of clinical drugs.
Yuka Kimura; Hideyuki Ito; Ryoko Ohnishi; Tsutomu Hatano
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2009-10-31
Journal Detail:
Title:  Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association     Volume:  48     ISSN:  1873-6351     ISO Abbreviation:  Food Chem. Toxicol.     Publication Date:  2010 Jan 
Date Detail:
Created Date:  2010-02-01     Completed Date:  2010-04-15     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  8207483     Medline TA:  Food Chem Toxicol     Country:  England    
Other Details:
Languages:  eng     Pagination:  429-35     Citation Subset:  IM    
Copyright Information:
Copyright 2009 Elsevier Ltd. All rights reserved.
Division of Pharmaceutical Sciences, Okayama University, Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama, Japan.
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MeSH Terms
Aryl Hydrocarbon Hydroxylases / antagonists & inhibitors*
Biflavonoids / chemistry,  pharmacology
Chromatography, High Pressure Liquid
Cytochrome P-450 CYP3A / antagonists & inhibitors*
Enzyme Inhibitors*
Flavonoids / pharmacology*
Magnetic Resonance Spectroscopy
Pharmaceutical Preparations / metabolism
Phenols / pharmacology*
Spectrometry, Mass, Electrospray Ionization
Reg. No./Substance:
0/Biflavonoids; 0/Enzyme Inhibitors; 0/Flavonoids; 0/Pharmaceutical Preparations; 0/Phenols; 0/polyphenols; 1617-53-4/amentoflavone; EC protein, human; EC Hydrocarbon Hydroxylases; EC protein, human; EC P-450 CYP3A

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