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学科主题物理化学
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
杨凌; 刘勇
会议名称The 26th Symposium for Biomembrane-Drug Interaction
会议日期2004-11-25
2004-11-25
会议地点日本
页码57/4
ISSN0031-6903
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
文献类型会议论文
条目标识符http://cas-ir.dicp.ac.cn/handle/321008/111644
专题中国科学院大连化学物理研究所
通讯作者杨凌
推荐引用方式
GB/T 7714
杨凌,刘勇. 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],2004:57/4.
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