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ToxSci Advance Access originally published online on March 17, 2006
Toxicological Sciences 2006 91(2):356-364; doi:10.1093/toxsci/kfj164
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© The Author 2006. Published by Oxford University Press on behalf of the Society of Toxicology. All rights reserved. For Permissions, please email: journals.permissions@oxfordjournals.org

Ginsenoside Metabolites, Rather Than Naturally Occurring Ginsenosides, Lead to Inhibition of Human Cytochrome P450 Enzymes

Yong Liu*,{dagger}, Jiang-Wei Zhang*,{dagger}, Wei Li*,{dagger}, Hong Ma{ddagger}, Jie Sun§, Mai-Cun Deng* and Ling Yang*,1

* Laboratory of Pharmaceutical Resource Discovery, Dalian Institute of Chemical Physics, Chinese Academy of Sciences, Dalian 116023, People's Republic of China; {dagger} Graduate School of the Chinese Academy of Sciences, People's Republic of China; {ddagger} College of Life Sciences, Liaoning Normal University, Dalian 116029, People's Republic of China; and § The Second Affiliated Hospital of Dalian Medical University, Dalian 116027, People's Republic of China

Received November 25, 2005; accepted March 10, 2006

There is still an argument about ginseng–prescription drug interactions. To evaluate the influence on cytochrome P450 (P450) activities of ginseng in the present study, the influence on P450 activities of naturally occurring ginsenosides and their degradation products in human gut lumen was assayed by using human liver microsomes and cDNA-expressed CYP3A4. The results showed that the naturally occurring ginsenosides exhibited no inhibition or weak inhibition against human CYP3A4, CYP2D6, CYP2C9, CYP2A6, or CYP1A2 activities; however, their main intestinal metabolites demonstrated a wide range of inhibition of the P450-mediated metabolism. There was no mechanism-based inhibition found on these P450 isoforms. It is noteworthy that Compound K, protopanaxadiol (Ppd), and protopanaxatriol (Ppt) all exhibited moderate inhibition against CYP2C9 activity, and Ppd and Ppt also exhibited potent competitive inhibition against CYP3A4 activity. We suggest that after oral administration, naturally occurring ginsenosides might influence hepatic P450 activity in vivo via their intestinal metabolites.

Key Words: ginseng-drug interactions; ginsenosides; intestinal metabolites; cytochrome P450.


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