Influence of Ginsenoside Rh₁ and F₁ on Human Cytochrome P450 Enzymes

 

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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.

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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

Phone: +86-411-8437-9317

Fax: +86-411-8467-6961

Email: yling@dicp.ac.cn

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