PPARdelta activation normalizes cardiac substrate metabolism and reduces right ventricular hypertrophy in congestive heart failure

J Cardiovasc Pharmacol. 2007 Jul;50(1):25-34. doi: 10.1097/FJC.0b013e31804b4163.

Abstract

Previously, it was shown that selective deletion of peroxisome proliferator activated receptor delta (PPARdelta) in the heart resulted in a cardiac lipotoxicity, hypertrophy, and heart failure. The aim of the present study was to determine the effects of chronic and selective pharmacological activation of PPARdelta in a model of congestive heart failure. PPARdelta-specific agonist treatment (GW610742X at 30 and 100 mg/kg/day for 6-9 weeks) was initiated immediately postmyocardial infarction (MI) in Sprague-Dawley rats. Magnetic resonance imaging/spectroscopy was used to assess cardiac function and energetics. A 1-(13)C glucose clamp was performed to assess relative cardiac carbohydrate versus fat oxidation. Additionally, cardiac hemodynamics and reverse-transcription polymerase chain reaction gene expression analysis was performed. MI rats had significantly reduced left ventricle (LV) ejection fractions and whole heart phosphocreatine/adenosine triphosphate ratio compared with Sham animals (reduction of 43% and 14%, respectively). However, GW610742X treatment had no effect on either parameter. In contrast, the decrease in relative fat oxidation rate observed in both LV and right ventricle (RV) following MI (decrease of 58% and 54%, respectively) was normalized in a dose-dependent manner following treatment with GW610742X. These metabolic changes were associated with an increase in lipid transport/metabolism target gene expression (eg, CD36, CPT1, UCP3). Although there was no difference between groups in LV weight or infarct size measured upon necropsy, there was a dramatic reduction in RV hypertrophy and lung congestion (decrease of 22-48%, P<0.01) with treatment which was associated with a >7-fold decrease (P<0.05) in aterial natriuretic peptide gene expression in RV. Diuretic effects were not observed with GW610742X. In conclusion, chronic treatment with a selective PPARdelta agonist normalizes cardiac substrate metabolism and reduces RV hypertrophy and pulmonary congestion consistent with improvement in congestive heart failure.

MeSH terms

  • Animals
  • Biological Transport
  • Diuresis / drug effects
  • Dose-Response Relationship, Drug
  • Energy Metabolism
  • Gene Expression / drug effects
  • Heart Failure / drug therapy*
  • Heart Failure / etiology
  • Heart Failure / physiopathology
  • Hypertrophy, Right Ventricular / drug therapy*
  • Hypertrophy, Right Ventricular / etiology
  • Hypertrophy, Right Ventricular / physiopathology
  • Lipids / blood
  • Magnetic Resonance Spectroscopy
  • Male
  • Myocardial Infarction / complications
  • Oxidation-Reduction
  • PPAR delta / agonists*
  • PPAR delta / metabolism
  • Pulmonary Edema / drug therapy
  • Pulmonary Edema / etiology
  • Rats
  • Rats, Sprague-Dawley
  • Reverse Transcriptase Polymerase Chain Reaction
  • Ventricular Function, Left / drug effects

Substances

  • Lipids
  • PPAR delta