Time-Dependent Induction of Hepatic Cytochrome P450 Enzyme Activity and mRNA Expression by Bilobalide in Rats

Yuko Taki; Yuko Yamazaki; Fumio Shimura; Shizuo Yamada; Keizo Umegaki

Journal of Pharmacological Sciences (Jan 2009)

Time-Dependent Induction of Hepatic Cytochrome P450 Enzyme Activity and mRNA Expression by Bilobalide in Rats

Yuko Taki,
Yuko Yamazaki,
Fumio Shimura,
Shizuo Yamada,
Keizo Umegaki

Affiliations

Yuko Taki: National Institute of Health and Nutrition, 1-23-1 Toyama, Shinjuku-ku, Tokyo 162-8636, Japan; Department of Pharmacokinetics and Pharmacodynamics and Global COE Program, School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka-shi, Shizuoka 422-8526, Japan
Yuko Yamazaki: Department of Food & Nutrition, Jumonji University, 2-1-28 Sugasawa, Niiza-shi, Saitama 352-8510, Japan
Fumio Shimura: Department of Food & Nutrition, Jumonji University, 2-1-28 Sugasawa, Niiza-shi, Saitama 352-8510, Japan
Shizuo Yamada: Department of Pharmacokinetics and Pharmacodynamics and Global COE Program, School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka-shi, Shizuoka 422-8526, Japan
Keizo Umegaki: National Institute of Health and Nutrition, 1-23-1 Toyama, Shinjuku-ku, Tokyo 162-8636, Japan; Department of Food & Nutrition, Jumonji University, 2-1-28 Sugasawa, Niiza-shi, Saitama 352-8510, Japan; *Corresponding author (affiliation #1). [email protected]

Journal volume & issue: Vol. 109, no. 3
pp. 459 – 462

Abstract

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A single dose by gavage of bilobalide (30 mg/kg) was found to produce a time-dependent induction of hepatic cytochrome P450 (CYP) enzyme activity and protein expression in rats. An RT-PCR study further showed that mRNA expression of CYP2B was maximal at 6 h. Plasma and liver bilobalide concentration in rats following administration of Ginkgo biloba extract equivalent to bilobalide of approximately 40 mg/kg showed a similar response to that exhibited by mRNA expression. These findings suggest that bilobalide markedly induced hepatic CYPs, but the induction could be mitigated due to rapid elimination from the liver. Keywords:: bilobalide, cytochrome P450 (CYP) induction, herb–drug interaction

Published in Journal of Pharmacological Sciences

ISSN: 1347-8613 (Print)
Publisher: Elsevier
Country of publisher: Japan
LCC subjects: Medicine: Therapeutics. Pharmacology
Website: http://www.journals.elsevier.com/journal-of-pharmacological-sciences

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