Time-dependent induction of hepatic cytochrome P450 enzyme activity and mRNA expression by bilobalide in rats.
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.
Taki
Yuko
Y
National Institute of Health and Nutrition, Japan.
Yamazaki
Yuko
Y
Shimura
Fumio
F
Yamada
Shizuo
S
Umegaki
Keizo
K
D000818:Animals; D003517:Cyclopentanes / Q000302:isolation & purification / Q000493:pharmacokinetics / Q000494:pharmacology*; D003577:Cytochrome P-450 Enzyme System / Q000187:drug effects* / Q000378:metabolism; D004790:Enzyme Induction / Q000187:drug effects; D005663:Furans / Q000302:isolation & purification / Q000493:pharmacokinetics / Q000494:pharmacology*; D005786:Gene Expression Regulation / Q000187:drug effects; D020441:Ginkgo biloba / Q000737:chemistry; D046934:Ginkgolides / Q000302:isolation & purification / Q000493:pharmacokinetics / Q000494:pharmacology*; D008099:Liver / Q000201:enzymology / Q000378:metabolism; D008297:Male; D010936:Plant Extracts / Q000493:pharmacokinetics / Q000494:pharmacology; D012333:RNA, Messenger / Q000187:drug effects / Q000378:metabolism; D051381:Rats; D017208:Rats, Wistar; D020133:Reverse Transcriptase Polymerase Chain Reaction; D013997:Time Factors
D003517:Cyclopentanes; D005663:Furans; D046934:Ginkgolides; D010936:Plant Extracts; D012333:RNA, Messenger; D003577:Cytochrome P-450 Enzyme System; C073710:bilobalide