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Research ArticleArticle

The Chinese Herbal Medicine Sophora flavescens Activates Pregnane X Receptor

Laiyou Wang, Feng Li, Jie Lu, Guodong Li, Dan Li, Xiao-bo Zhong, Grace L. Guo and Xiaochao Ma
Drug Metabolism and Disposition December 2010, 38 (12) 2226-2231; DOI: https://doi.org/10.1124/dmd.110.035253
Laiyou Wang
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Feng Li
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Jie Lu
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Guodong Li
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Dan Li
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Xiao-bo Zhong
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Grace L. Guo
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Xiaochao Ma
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Abstract

Sophora flavescens (SF) is an herbal medicine widely used for the treatment of viral hepatitis, cancer, viral myocarditis, gastrointestinal hemorrhage, and skin diseases. It was recently reported that SF up-regulates CYP3A expression. The mechanism of SF-induced CYP3A expression is unknown. In the current study, we tested the hypothesis that SF-induced CYP3A expression is mediated by the activation of pregnane X receptor (PXR). We used two cell lines, DPX2 and HepaRG, to investigate the role of PXR in SF-induced CYP3A expression. The DPX2 cell line is derived from HepG2 cells with the stable transfection of human PXR and a luciferase reporter gene linked with a human PXR response element identified in the CYP3A4 gene promoter. In DPX2 cells, SF activated PXR in a concentration-dependent manner. We used a metabolomic approach to identify the chemical constituents in SF, which were further analyzed for their effect on PXR activation and CYP3A regulation. One chemical in SF, N-methylcytisine, was identified as an individual chemical that activated PXR. HepaRG is a highly differentiated hepatoma cell line that mimics human hepatocytes. In HepaRG cells, N-methylcytisine significantly induced CYP3A4 expression, and this induction was suppressed by the PXR antagonist sulforaphane. These results suggest that SF induces CYP3A expression via the activation of PXR.

Footnotes

  • This work was supported by the National Institutes of Health National Center for Research Resources [Grant COBRE 5P20-RR021940].

  • Article, publication date, and citation information can be found at http://dmd.aspetjournals.org.

    doi:10.1124/dmd.110.035253.

  • Embedded Image The online version of this article (available at http://dmd.aspetjournals.org) contains supplemental material.

  • ABBREVIATIONS:

    SF
    Sophora flavescens
    P450
    cytochrome P450
    CAR
    constitutive androstane receptor
    PXR
    pregnane X receptor
    SCB
    Schisandrae chinensis Baill
    GUF
    Glycyrrhizae uralensis Fisch
    qPCR
    quantitative real-time polymerase chain reaction
    UPLC
    ultraperformance liquid chromatography
    TOFMS
    time-of-flight mass spectrometry
    PCA
    principal-component analysis
    OPLS-DA
    orthogonal projection to latent structures-discriminant analysis.

  • Received July 2, 2010.
  • Accepted August 23, 2010.
  • Copyright © 2010 by The American Society for Pharmacology and Experimental Therapeutics
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Drug Metabolism and Disposition: 38 (12)
Drug Metabolism and Disposition
Vol. 38, Issue 12
1 Dec 2010
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Research ArticleArticle

The Chinese Herbal Medicine Sophora flavescens Activates Pregnane X Receptor

Laiyou Wang, Feng Li, Jie Lu, Guodong Li, Dan Li, Xiao-bo Zhong, Grace L. Guo and Xiaochao Ma
Drug Metabolism and Disposition December 1, 2010, 38 (12) 2226-2231; DOI: https://doi.org/10.1124/dmd.110.035253

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Research ArticleArticle

The Chinese Herbal Medicine Sophora flavescens Activates Pregnane X Receptor

Laiyou Wang, Feng Li, Jie Lu, Guodong Li, Dan Li, Xiao-bo Zhong, Grace L. Guo and Xiaochao Ma
Drug Metabolism and Disposition December 1, 2010, 38 (12) 2226-2231; DOI: https://doi.org/10.1124/dmd.110.035253
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