Differentiation and growth inhibition mediated via the RXR:PPARgamma heterodimer in colon cancer

Cancer Lett. 2006 Aug 28;240(2):225-33. doi: 10.1016/j.canlet.2005.09.010. Epub 2005 Nov 3.

Abstract

This study evaluated the anti-tumor efficacy of combining the RXR agonist, bexarotene, with the PPARgamma agonist, rosiglitazone, in colon cancer. Moser, a human colon cancer cell line, was treated with bexarotene and rosiglitazone alone or in combination and the effect on growth and differentiation were examined. The data demonstrated that the bexarotene/rosiglitazone combination produced greater efficacy in growth inhibition than either single agent. Furthermore, combination treatment acted cooperatively to decrease COX-2 expression and PGE2 synthesis while increasing expression of the differentiation marker, CEA. These findings were confirmed in vivo in a Moser xenograft tumor model. Collectively, our data suggest a potential role for utilizing a combination regimen of a RXR and PPARgamma agonist in the treatment of colon cancer.

MeSH terms

  • Animals
  • Anticarcinogenic Agents / pharmacology
  • Bexarotene
  • Cell Differentiation*
  • Cell Proliferation*
  • Colonic Neoplasms / drug therapy
  • Colonic Neoplasms / metabolism*
  • Colonic Neoplasms / pathology*
  • Cyclooxygenase 2 / metabolism
  • Fibrinolytic Agents / pharmacology
  • Humans
  • Male
  • Membrane Proteins / metabolism
  • Mice
  • Mice, Nude
  • PPAR gamma / agonists
  • PPAR gamma / metabolism*
  • Prostaglandin D2 / metabolism
  • Retinoid X Receptors / agonists
  • Retinoid X Receptors / metabolism*
  • Rosiglitazone
  • Tetrahydronaphthalenes / pharmacology
  • Thiazolidinediones / pharmacology
  • Transplantation, Heterologous
  • Tumor Cells, Cultured

Substances

  • Anticarcinogenic Agents
  • Fibrinolytic Agents
  • Membrane Proteins
  • PPAR gamma
  • Retinoid X Receptors
  • Tetrahydronaphthalenes
  • Thiazolidinediones
  • Rosiglitazone
  • Bexarotene
  • Cyclooxygenase 2
  • PTGS2 protein, human
  • Prostaglandin D2