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学科主题: 物理化学
题名: nrestinal bacterial metabolite of naturally occurring 20(S)-protopanaxatriol ginsenosides is the inhibitor of CYP3A——a new biotransformation way with potential for clinical drug-druginteraction
作者: Yang L(杨凌) ;  Liu Y(刘勇)
会议名称: The 26th Symposium for Biomembrane-Drug Interaction
会议日期: 2004-11-25
出版日期: 2004-11-25
会议地点: 日本
通讯作者: 杨凌
ISSN: 0031-6903
部门归属: 十八室
主办者: 日本药学会
摘要: The intestinal bacterial metabolites of ginsenosides are really responsible for the main pharmacological activities of ginseng. The purpose of this study was to find whether intestinal bacterial metabolites of ginsenosides possess influences on hepatic metabolic enzymes and to predict the potential for ginseng-prescription drug interactions. Utilizing the probe reaction of CYP3A activity, testosterone 6β-hydroxylation, the effects of derivatives of 20(S)-protopanaxadiol and 20(S)-protopanaxatriol families on CYP3A activity in liver microsomes and cDNA-expressed human CYP3A4 were assayed. Our results showed that either in rat and human liver microsomes or in cDNA-expressed CYP3A4, ginsenosides exhibited a similar inhibition profile for testosterone 6β-hydroxylation activity. Ginsenosides from 20(S)-protopanaxadiol and 20(S)-protopanaxatriol family including Rb1, Rb2, Rc, Compound-K, Re, and Rg1 were no inhibitory effect, whereas the intestinal bacterial metabolite of 20(S)-protopanaxatriol ginsenosides, 20(S)-protopanaxatriol (Ppt), exhibited strong competitively inhibitory activity against CYP3A activity in human and rat liver microsomes and in cDNA-expressed CYP3A4. This finding demonstrates that naturally occurring ginsenosides have no inhibitory effects on CYP3A activities, yet their intestinal bacterial metabolite possesses the potential for inhibitory effects on CYP3A activities. It suggests that ginseng-derived products might result in significant ginseng-drug interactions via their intestinal bacterial metabolite.
语种: 中文
内容类型: 会议论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/111644
Appears in Collections:中国科学院大连化学物理研究所_会议论文

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Recommended Citation:
Yang L,Liu Y. nrestinal bacterial metabolite of naturally occurring 20(S)-protopanaxatriol ginsenosides is the inhibitor of CYP3A——a new biotransformation way with potential for clinical drug-druginteraction[C]. 见:The 26th Symposium for Biomembrane-Drug Interaction. 日本. 2004-11-25.
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