Guggulsterone suppresses bile acid-induced and constitutive caudal-related homeobox 2 expression in gut-derived adenocarcinoma cells

Anticancer Res. 2010 Jun;30(6):1953-60.


Background: Guggulsterone, a plant polyphenol guggulipid, has several antitumour effects and acts as an antagonist for the farnesoid X receptor. Although bile acids induce caudal-related homeobox 2 (CdX2), a transcription factor essential for intestinal development and gut tumourigenesis, the effects of guggulsterone on regulation of CdX2 in the gut are unknown.

Materials and methods: Regulation of CdX2 expression by treatment with bile acids and/or guggulsterone was analysed by immunoblot analysis in human gut-derived adenocarcinoma, Bic-1 cells. Nuclear factor-kappaB (NF-kappaB) activity and the cell cycle distribution were also examined.

Results: Chenodeoxycholic acid and deoxycholic acid increased CdX2 expression in Bic-1 cells. Guggulsterone reduced bile acid-induced and constitutive CdX2 expression at 5 microM. Guggulsterone (up to 5 microM) did not affect cell viability or the cell cycle and did not attenuate bile acid-induced or constitutive NF-kappaB activation.

Conclusion: Guggulsterone may be used as a novel drug to target CdX2 expression in certain gut adenocarcinomas.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenocarcinoma / drug therapy*
  • Adenocarcinoma / pathology
  • Antineoplastic Agents, Phytogenic / pharmacology*
  • Apoptosis / drug effects
  • Bile Acids and Salts / antagonists & inhibitors*
  • CDX2 Transcription Factor
  • Cell Cycle / drug effects
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Homeodomain Proteins / antagonists & inhibitors*
  • Humans
  • Intestinal Neoplasms / drug therapy*
  • Intestinal Neoplasms / pathology
  • NF-kappa B / antagonists & inhibitors
  • NF-kappa B / metabolism
  • Pregnenediones / pharmacology*
  • Receptors, Cytoplasmic and Nuclear / antagonists & inhibitors*


  • Antineoplastic Agents, Phytogenic
  • Bile Acids and Salts
  • CDX2 Transcription Factor
  • CDX2 protein, human
  • Homeodomain Proteins
  • NF-kappa B
  • Pregnenediones
  • Receptors, Cytoplasmic and Nuclear
  • farnesoid X-activated receptor
  • pregna-4,17-diene-3,16-dione