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DOI: 10.1055/s-2005-873197
© Georg Thieme Verlag KG Stuttgart · New York
Influence of Ginsenoside Rh1 and F1 on Human Cytochrome P450 Enzymes
Publikationsverlauf
Received: May 24, 2005
Accepted: July 13, 2005
Publikationsdatum:
05. Januar 2006 (online)
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Abstract
For an oral herbal medicine, the components that can enter the systemic circulation may be the really effective components. In the present study, the effects on the human cytochrome P450 activities of ginsenoside Rb1 and two hydrolysis products of 20(S)-protopanaxatriol ginsenosides in humans, namely ginsenoside Rh1 and F1, which may reach the systemic circulation after oral administration of ginseng extract, were evaluated. Our results showed that Rb1 exhibited no marked effects on the activities of human cytochrome P450, whereas Rh1 and F1 exhibited competitive inhibition of the activity of CYP3A4 with K i values of 57.7 ± 9.6 μM and 67.8 ± 16.2 μM, respectively. F1 also exhibited a weaker inhibition of the activity of CYP2D6. Rh1 exhibited a weak stimulation rather than an inhibition of the activity of CYP2E1. The degradation of ginsenosides in the gastrointestinal tract may play an important role in the ginseng-associated drug-drug interactions, but the effects might be not due to Rh1 and F1.
Key words
Ginsenoside - hydrolysis products - systemic circulation - cytochrome P450
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Ling Yang, Ph. D.
Laboratory of Pharmaceutical Resource Discovery
Dalian Institute of Chemical Physics
The Chinese Academy of Sciences
457 Zhong-shan Road
Dalian 116023
People’s Republic of China
Telefon: +86-411-8437-9317
Fax: +86-411-8467-6961
eMail: yling@dicp.ac.cn
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