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Antiproliferative and apoptotic effects of telmisartan in human colon cancer cells

Lucas D Lee1, Benjamin Mafura1, Johannes C Lauscher1

  • 1Department of General, Visceral and Vascular Surgery, Campus Benjamin Franklin, Charité-University of Medicine Berlin, Berlin D-12203, Germany.

Oncology Letters
|November 1, 2014
PubMed

Insights

Telmisartan, an antihypertensive drug, shows significant antiproliferative and apoptotic effects on human colon cancer cells. These effects are partly mediated by peroxisome proliferator-activated receptor gamma (PPARγ) activation.

Area of Science:

  • Oncology
  • Pharmacology
  • Molecular Biology

Background:

  • Telmisartan is an angiotensin I (AT1) receptor blocker used for hypertension.
  • Peroxisome proliferator-activated receptor gamma (PPARγ) activation has demonstrated antiproliferative and apoptotic effects in cancer cells.
  • Telmisartan exhibits partial PPARγ agonism, suggesting potential anticancer properties.

Purpose of the Study:

  • To investigate the antiproliferative and apoptotic effects of telmisartan in human colon cancer cells.
  • To evaluate the role of partial PPARγ activation by telmisartan in these effects.
  • To compare telmisartan's efficacy with a full PPARγ agonist, pioglitazone.

Main Methods:

  • Human colon cancer cell lines (HT-29, SW-480, SW-620) were treated with telmisartan or pioglitazone at various concentrations.
  • The effects of PPARγ blockade using GW9662 were assessed in conjunction with telmisartan and pioglitazone treatment.
  • Cell proliferation and apoptosis were measured to determine the impact of the treatments.

Main Results:

  • Telmisartan demonstrated significant antiproliferative and apoptotic effects on colon cancer cells at therapeutic concentrations, comparable to pioglitazone.
  • PPARγ blockade did not fully abolish the effects of pioglitazone but enhanced the antiproliferative and apoptotic effects of telmisartan.
  • These findings suggest that telmisartan's effects are not solely explained by PPARγ activation.

Conclusions:

  • Telmisartan possesses significant antiproliferative and apoptotic potential against human colon cancer cells.
  • The mechanism of action involves partial PPARγ activation but also includes PPARγ-independent pathways.
  • Further research is needed to elucidate the complete mechanism, including ligand-independent PPARγ activation or other independent pathways.
Keywords:
angiotensin I receptor blockerantiproliferativeapoptosiscolon cancerperoxisome proliferator-activated receptor γtelmisartan

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