Inhibition of the different phosphodiesterase isoforms of rat heart cytosol by free fatty acids

J Cardiovasc Pharmacol. 1993 Apr;21(4):522-9. doi: 10.1097/00005344-199304000-00003.

Abstract

The sensitivity of the various phosphodiesterase (PDE) isoforms present in the cytosolic compartment of rat heart to the main fatty acids of the saturated, n-3 and n-6 families was assessed. High-performance liquid chromatography (HPLC) on a Mono Q ion-exchange column resolved four separate cyclic nucleotide phosphodiesterase activities: a calmodulin-activated fraction, a cyclic GMP-stimulated fraction, a cyclic AMP-specific rolipram-sensitive fraction, and a cyclic GMP-inhibited fraction. Polyunsaturated fatty acids (PUFA) were more potent inhibitors than saturated fatty acids whatever the considered PDE isoform. Although all PDE isoforms were affected, the cyclic GMP-stimulated isoform was the most sensitive to the inhibitory effect of PUFAs. The possible influences of free fatty acids (FFA) on cardiac contractility through PDE inhibition are discussed.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Chromatography, High Pressure Liquid
  • Chromatography, Ion Exchange
  • Cytosol / drug effects
  • Cytosol / enzymology
  • Fatty Acids, Nonesterified / pharmacology*
  • Fatty Acids, Unsaturated / pharmacology
  • Heart / drug effects*
  • Isoenzymes
  • Male
  • Myocardium / enzymology*
  • Phosphodiesterase Inhibitors / pharmacology*
  • Phosphoric Diester Hydrolases / metabolism
  • Rats
  • Rats, Sprague-Dawley

Substances

  • Fatty Acids, Nonesterified
  • Fatty Acids, Unsaturated
  • Isoenzymes
  • Phosphodiesterase Inhibitors
  • Phosphoric Diester Hydrolases