A tea catechin, epigallocatechin-3-gallate, is a unique modulator of the farnesoid X receptor

Guodong Li, Wenwei Lin, Juan J. Araya, Taosheng Chen, Barbara N. Timmermann, Grace L. Guo

Research output: Contribution to journalArticlepeer-review

51 Scopus citations


Farnesoid X receptor (FXR) is a ligand-activated nuclear receptor and serves as a key regulator to maintain health of the liver and intestine. Bile acids are endogenous ligands of FXR, and there are increasing efforts to identify FXR modulators to serve as biological probes and/or pharmaceutical agents. Natural FXR ligands isolated from plants may serve as models to synthesize novel FXR modulators. In this study, we demonstrated that epigallocatechin-3-gallate (EGCG), a major tea catechin, specifically and dose-dependently activates FXR. In addition, EGCG induced FXR target gene expression in vitro. Surprisingly, in a co-activator (SRC2) recruitment assay, we found that EGCG does not recruit SRC2 to FXR, but it dose-dependently inhibits recruitment of SRC2 to FXR (IC 50, 1μM) by GW6064, which is a potent FXR synthetic ligand. In addition, EGCG suppressed FXR target gene expression induced by either GW4064 or chenodeoxycholic acid in vitro. Furthermore, wild-type and FXR knockout mice treated with an acute dose of EGCG had induced mRNA expression in a subset of FXR target genes in the intestine but not in the liver. In conclusion, EGCG is a unique modulator of FXR in the intestine and may serve as an important model for future development of FXR modulators.

Original languageEnglish (US)
Pages (from-to)268-274
Number of pages7
JournalToxicology and Applied Pharmacology
Issue number2
StatePublished - Jan 15 2012
Externally publishedYes

All Science Journal Classification (ASJC) codes

  • Toxicology
  • Pharmacology


  • Epigallocatechin-3-gallate
  • Farnesoid X receptor
  • Mice
  • Modulator
  • Nuclear receptor
  • Tea catechin


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