Effects of coumestrol on lipid and glucose metabolism as a farnesoid X receptor ligand

Biochem Biophys Res Commun. 2008 Aug 1;372(3):395-9. doi: 10.1016/j.bbrc.2008.04.136. Epub 2008 May 5.

Abstract

In the course of an effort to identify novel agonists of the farnesoid X receptor (FXR), coumestrol was determined to be one such ligand. Reporter and in vitro coactivator interaction assays revealed that coumestrol bound and activated FXR. Treatment of Hep G2 cells with coumestrol stimulated the expression of FXR target genes, thereby regulating the expression of target genes of the liver X receptor and hepatocyte nuclear factor-4alpha. Through these actions, coumestrol is expected to exert beneficial effects on lipid and glucose metabolism.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Apolipoproteins B / metabolism
  • Cell Line
  • Coumestrol / pharmacology*
  • DNA-Binding Proteins / agonists*
  • DNA-Binding Proteins / metabolism
  • Glucose / metabolism*
  • Humans
  • Ligands
  • Lipid Metabolism / drug effects*
  • Lipid Metabolism / genetics
  • Phytoestrogens / pharmacology*
  • Receptors, Cytoplasmic and Nuclear / agonists*
  • Receptors, Cytoplasmic and Nuclear / metabolism
  • Transcription Factors / agonists*
  • Transcription Factors / metabolism
  • Transcription, Genetic / drug effects*

Substances

  • Apolipoproteins B
  • DNA-Binding Proteins
  • Ligands
  • Phytoestrogens
  • Receptors, Cytoplasmic and Nuclear
  • Transcription Factors
  • farnesoid X-activated receptor
  • Glucose
  • Coumestrol