The Inhibitory Effect of Intestinal Bacterial Metabolite of Ginsenosides on CYP3A Activity

DOI Web Site Web Site PubMed 被引用文献1件 参考文献46件
  • Liu Yong
    Laboratory of Pharmaceutical Resource Discovery, Dalian Institute of Chemical Physics, Chinese Academy of Sciences Graduate School of the Chinese Academy of Sciences
  • Li Wei
    Laboratory of Pharmaceutical Resource Discovery, Dalian Institute of Chemical Physics, Chinese Academy of Sciences Graduate School of the Chinese Academy of Sciences
  • Li Peng
    Laboratory of Pharmaceutical Resource Discovery, Dalian Institute of Chemical Physics, Chinese Academy of Sciences
  • Deng Mai-Cun
    Laboratory of Pharmaceutical Resource Discovery, Dalian Institute of Chemical Physics, Chinese Academy of Sciences
  • Yang Sheng-Li
    Laboratory of Pharmaceutical Resource Discovery, Dalian Institute of Chemical Physics, Chinese Academy of Sciences
  • Yang Ling
    Laboratory of Pharmaceutical Resource Discovery, Dalian Institute of Chemical Physics, Chinese Academy of Sciences

書誌事項

タイトル別名
  • Inhibitory Effect of Intestinal Bacterial Metabolite of Ginsenosides on CYP3A Activity
公開日
2004
資源種別
journal article
DOI
  • 10.1248/bpb.27.1555
公開者
公益社団法人 日本薬学会

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説明

The intestinal bacterial metabolites of ginsenosides are responsible for the main pharmacological activities of ginseng. The purpose of this study was to find whether these metabolites influence 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 rat liver microsomes were assayed. Our results showed that ginsenosides from the 20(S)-protopanaxadiol and 20(S)-protopanaxatriol family including Rb1, Rb2, Rc, Compound-K, Re, and Rg1 had no inhibitory effect, whereas Rg2, 20(S)-panaxatriol and 20(S)-protopanaxatriol exhibited competitive inhibitory activity against CYP3A activity in these microsomes with the inhibition constants (Ki) of 86.4±0.8 μM, 1.7±0.1 μM, and 3.2±0.2 μM, respectively. This finding demonstrates that differences in their chemical structure might influence the effects of ginsenosides on CYP3A activity and that ginseng-derived products might have potential for significant ginseng–drug interactions.

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