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题名: Intestinal bacterial metabolite of naturally occurring 20(S)-protopanaxatriol ginsenosides is the inhibitor of CYP3A - A new biotransformation way with potential for clinical drug-drug interaction
作者: Yang, L;  Liu, Y
关键词: ginseng-drug interaction ;  intestinal bacterial metabolite ;  ginsenoside ;  CYP3A
刊名: YAKUGAKU ZASSHI-JOURNAL OF THE PHARMACEUTICAL SOCIETY OF JAPAN
发表日期: 2004
卷: 124, 页:57-60
收录类别: SCI ;  ISTP
文章类型: Article
WOS标题词: Science & Technology ;  Life Sciences & Biomedicine
类目[WOS]: Pharmacology & Pharmacy
研究领域[WOS]: Pharmacology & Pharmacy
英文摘要: 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 6beta-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 6 13 -hydroxylation activity. Ginsenosides from 20(S)-protopanaxadiol and 20(S)-protopanaxatriol family including Rb-1, Rb-2, Rc, Compound-K, Re, and Rg(1) 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.
关键词[WOS]: GINSENG SAPONINS ;  RAT ;  ABSORPTION ;  EXCRETION
语种: 英语
WOS记录号: WOS:000225267900015
Citation statistics: 
内容类型: 期刊论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/139593
Appears in Collections:中国科学院大连化学物理研究所_期刊论文

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作者单位: 1.Chinese Acad Sci, Dalian Inst Chem Phys, Lab Pharmaceut Resource Discovery, Dalian 116023, Peoples R China

Recommended Citation:
Yang, L,Liu, Y. Intestinal bacterial metabolite of naturally occurring 20(S)-protopanaxatriol ginsenosides is the inhibitor of CYP3A - A new biotransformation way with potential for clinical drug-drug interaction[J]. YAKUGAKU ZASSHI-JOURNAL OF THE PHARMACEUTICAL SOCIETY OF JAPAN,2004,124:57-60.
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