The AAPS Journal

, 11:590 | Cite as

Activation of Pregnane X Receptor (PXR) and Constitutive Androstane Receptor (CAR) by Herbal Medicines

  • Thomas K. H. ChangEmail author
Review Article Theme: Natural Products as Therapeutic Modulators


Pregnane X receptor (PXR) and constitutive androstane receptor (CAR) are transcription factors that control the expression of a broad array of genes involved not only in transcellular transport and biotransformation of many drugs, other xenochemicals, and endogenous substances, such as bile acid, bilirubin, and certain vitamins, but also in various physiological/pathophysiological processes such as lipid metabolism, glucose homeostasis, and inflammation. Ligands of PXR and CAR are chemicals of diverse structures, including naturally occurring compounds present in herbal medicines. The overall aim of this article is to provide an overview of our current understanding of the role of herbal medicines as modulators of PXR and CAR.

Key words

constitutive androstane receptor herbal medicine pregnane X receptor 



This work was supported by the Canadian Institutes of Health Research (Grant MOP-84581) and Michael Smith Foundation for Health Research (a Senior Scholar Award to T.K.H.C.).


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© American Association of Pharmaceutical Scientists 2009

Authors and Affiliations

  1. 1.Faculty of Pharmaceutical SciencesThe University of British ColumbiaVancouverCanada

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