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Research ArticleArticle

In Vitro Effect of Standardized Ginseng Extracts and Individual Ginsenosides on the Catalytic Activity of Human CYP1A1, CYP1A2, and CYP1B1

Thomas K. H. Chang, Jie Chen and Salete A. Benetton
Drug Metabolism and Disposition April 2002, 30 (4) 378-384; DOI: https://doi.org/10.1124/dmd.30.4.378
Thomas K. H. Chang
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Jie Chen
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Salete A. Benetton
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Abstract

Ginseng extract has been reported to decrease the incidence of 7,12-dimethylbenz[a]anthracene (DMBA)-initiated tumorigenesis in mice. A potential mechanism for this effect by ginseng is inhibition of DMBA-bioactivating cytochrome P450 (P450) enzymes. In the present in vitro study, we examined the effect of a standardized Panax ginseng (or Asian ginseng) extract (G115), a standardized Panax quinquefolius (or North American ginseng) extract (NAGE), and individual ginsenosides (Rb1, Rb2, Rc, Rd, Re, Rf, and Rg1) on CYP1 catalytic activities, as assessed by 7-ethoxyresorufin O-dealkylation. G115 and NAGE decreased human recombinant CYP1A1, CYP1A2, and CYP1B1 activities in a concentration-dependent manner. Except for the competitive inhibition of CYP1A1 by G115, the mode of inhibition was the mixed-type in the other cases. A striking finding was that NAGE was 45-fold more potent than G115 in inhibiting CYP1A2. Compared with G115, NAGE also preferentially inhibited 7-ethoxyresorufinO-dealkylation activity in human liver microsomes. Rb1, Rb2, Rc, Rd, Re, Rf, and Rg1, either individually or as a mixture and at the levels reflecting those found in an inhibitory concentration (100 μg/ml) of NAGE or G115, did not influence CYP1 activities. However, at a higher ginsenoside concentration (50 μg/ml), Rb1, Rb2, Rc, Rd, and Rf inhibited these activities. Overall, our in vitro findings indicate that standardized NAGE and G115 extracts, which were not treated with calf serum or subjected to acid hydrolysis, inhibited CYP1 catalytic activity in an enzyme-selective and extract-specific manner, but the effects were not due to Rb1, Rb2, Rc, Rd, Re, Rf, or Rg1.

Footnotes

  • This research was supported by National Institutes of Health Grant AT00286 (to T.K.H.C.). T.K.H.C. is the recipient of a Research Career Award in the Health Sciences from the Canadian Institutes of Health Research and the Rx&D Health Research Foundation.

  • Abbreviations used are::
    DMBA
    7,12-dimethylbenz[a]anthracene
    P450
    cytochrome P450
    G115
    Panax ginseng (Asian ginseng) extract
    NAGE
    Panax quinquefolius (North American) ginseng extract
    HPLC
    high-performance liquid chromatography
    • Received October 25, 2001.
    • Accepted December 18, 2001.
  • The American Society for Pharmacology and Experimental Therapeutics
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Drug Metabolism and Disposition: 30 (4)
Drug Metabolism and Disposition
Vol. 30, Issue 4
1 Apr 2002
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Research ArticleArticle

In Vitro Effect of Standardized Ginseng Extracts and Individual Ginsenosides on the Catalytic Activity of Human CYP1A1, CYP1A2, and CYP1B1

Thomas K. H. Chang, Jie Chen and Salete A. Benetton
Drug Metabolism and Disposition April 1, 2002, 30 (4) 378-384; DOI: https://doi.org/10.1124/dmd.30.4.378

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Research ArticleArticle

In Vitro Effect of Standardized Ginseng Extracts and Individual Ginsenosides on the Catalytic Activity of Human CYP1A1, CYP1A2, and CYP1B1

Thomas K. H. Chang, Jie Chen and Salete A. Benetton
Drug Metabolism and Disposition April 1, 2002, 30 (4) 378-384; DOI: https://doi.org/10.1124/dmd.30.4.378
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