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Titre du document / Document title

Inhibitory effects of polyphenols on human cytochrome P450 3A4 and 2C9 activity

Auteur(s) / Author(s)

KIMURA Yuka (1) ; ITO Hideyuki (1) ; OHNISHI Ryoko (1) ; HATANO Tsutomu (1) ;

Affiliation(s) du ou des auteurs / Author(s) Affiliation(s)

(1) Division of Pharmaceutical Sciences, Okayama University, Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama, JAPON

Résumé / Abstract

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 IC50 values of 0.07 and 0.03 μM, respectively. The Ki 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.

Revue / Journal Title

Food and chemical toxicology    ISSN  0278-6915   CODEN FCTOD7 

Source / Source

2010, vol. 48, no1, pp. 429-435 [7 page(s) (article)] (1/2 p.)

Langue / Language

Anglais

Editeur / Publisher

Elsevier, Oxford, ROYAUME-UNI  (1982) (Revue)

Mots-clés anglais / English Keywords

Flavonoid

;

Enzyme

;

Phenols

;

Biological activity

;

Cytochrome P450

;

Human

;

Plant origin

;

Polyphenol

;

Apigenin

;

Mots-clés français / French Keywords

Flavonoïde

;

Enzyme

;

Phénols

;

Cytochrome CYP3A4

;

Activité biologique

;

Cytochrome P450

;

Homme

;

Origine végétale

;

Polyphénol

;

Apigénine

;

Mots-clés espagnols / Spanish Keywords

Flavonoide

;

Enzima

;

Fenoles

;

Actividad biológica

;

Citocromo P450

;

Hombre

;

Origen vegetal

;

Polifenol

;

Mots-clés d'auteur / Author Keywords

Amentoflavone

;

Apigenin

;

Cytochrome P450

;

Imperatorin

;

Polyphenols

;

Localisation / Location

INIST-CNRS, Cote INIST : 10616, 35400018929720.0630

Nº notice refdoc (ud4) : 22390596



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