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KMID : 0370220150590020049
Yakhak Hoeji
2015 Volume.59 No. 2 p.49 ~ p.54
In vitro Assessment of Cytochrome P450 Inhibition by Red Ginseng Ginsenosides
Ryu Chang-Seon

Shin Jang-Hyun
Shin Byoung-Chan
Sim Jae-Han
Yang Hyeon-Dong
Kim Bong-Hee
Abstract
In the present study we evaluated comparative herb-drug interaction potential of red ginseng total powder, ginsenoside Rg1, and Rb1 by inhibition of CYP isoforms including CYP1A2, CYP2A6, CYP2B6, CYP2C9, CYP2C19, CYP2D6, CYP2E1 and CYP3A4 using pooled human liver microsomes (HLMs). As measured by liquid chromatography-electrospray ionization tandem mass spectrometry, red ginseng total powder inhibited significantly activities of CYP1A2, CYP2A6, CYP2B6, CYP2C9, CYP2C19, CYP2D6, CYP2E1 and testosterone 6-beta hydroxylation by CYP3A4, but the IC50 values were higher than 556 ¥ìg/ml. Activities of CYP2B6, CYP2C9, CYP2D6 and CYP3A4 were inhibited by ginsenoside Rb1. Also, activities of CYP1A2, CYP2A6, CYP2B6, CYP2C9, CYP2C19, CYP2D6 and testosterone 6-beta hydroxylation by CYP3A4 were inhibited by ginsenoside Rg1. The IC50 values of ginsenoside Rb1 and Rg1 were higher than 200 ¥ìg/ml. Based on IC50 values against CYP isoforms, ginsenosides-drug interactions by CYP inhibition may be very low in clinical situations.
KEYWORD
cytochrome P450, red ginseng, ginsenoside, drug-drug interaction
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