Activation of pregnane X receptor (PXR) and constitutive androstane receptor (CAR) by herbal medicines

AAPS J. 2009 Sep;11(3):590-601. doi: 10.1208/s12248-009-9135-y. Epub 2009 Aug 18.


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.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Constitutive Androstane Receptor
  • Herbal Medicine*
  • Humans
  • Plants / classification
  • Pregnane X Receptor
  • Rats
  • Receptors, Cytoplasmic and Nuclear / agonists*
  • Receptors, Steroid / agonists*


  • Constitutive Androstane Receptor
  • Pregnane X Receptor
  • Receptors, Cytoplasmic and Nuclear
  • Receptors, Steroid