The peroxisome proliferator-activated receptor alpha activator fenofibrate inhibits endothelin-1-induced cardiac fibroblast proliferation

J Cardiovasc Pharmacol. 2004 Nov:44 Suppl 1:S279-82. doi: 10.1097/01.fjc.0000166274.24797.0e.

Abstract

Endothelin-1 has been known to promote tissue fibrosis. We previously reported in our animal experiments that a peroxisome proliferator-activated receptor alpha (PPARalpha) inhibited cardiac fibrosis with suppression of endothelin-1 production, and it was also reported that PPARalpha activation suppressed the production of c-jun, which is a component of activator protein-1. The objective of this study is to clarify on the in vitro level that PPARalpha activators inhibited cardiac fibroblast proliferation via their suppressive action on c-jun expression. We investigated the effects of the PPARalpha activator fenofibrate (10 microM) on DNA synthesis in neonatal rat cardiac fibroblasts by [H]thymidine incorporation. The [H]thymidine incorporation in cardiac fibroblasts showed an increase of 1.1-fold by endothelin-1 (10(-8) M) stimulation. Fenofibrate treatment showed significant inhibition of [3H]thymidine incorporation in both endothelin-1-stimulated and non-stimulated fibroblasts. Additionally, we also evaluated mRNA expressions of c-jun and c-fos in the fibroblasts by the reverse transcription-polymerase chain reaction method. Fenofibrate treatment markedly reduced c-jun mRNA expression, whereas it did not affect c-fos mRNA expression. In conclusion, we demonstrated that the PPARalpha activator fenofibrate inhibited endothelin-1-induced proliferation of cardiac fibroblasts and also inhibited non-stimulated proliferation. This inhibition of proliferation may be caused by up-regulation of p27 by suppressing c-jun expression.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Animals, Newborn
  • Cell Proliferation / drug effects*
  • Cells, Cultured
  • DNA Replication / drug effects
  • Down-Regulation
  • Endothelin-1 / metabolism*
  • Fenofibrate / pharmacology*
  • Fibroblasts / drug effects*
  • Fibroblasts / metabolism
  • Heart Ventricles / drug effects
  • Heart Ventricles / metabolism
  • Hypolipidemic Agents / pharmacology*
  • PPAR alpha / agonists*
  • PPAR alpha / metabolism
  • Proto-Oncogene Proteins c-fos / genetics
  • Proto-Oncogene Proteins c-fos / metabolism
  • Proto-Oncogene Proteins c-jun / genetics
  • Proto-Oncogene Proteins c-jun / metabolism
  • RNA, Messenger / metabolism
  • Rats
  • Rats, Sprague-Dawley

Substances

  • Endothelin-1
  • Hypolipidemic Agents
  • PPAR alpha
  • Proto-Oncogene Proteins c-fos
  • Proto-Oncogene Proteins c-jun
  • RNA, Messenger
  • Fenofibrate