Olprinone, a PDE3 inhibitor, modulates the inflammation associated with myocardial ischemia-reperfusion injury in rats

Eur J Pharmacol. 2011 Jan 15;650(2-3):612-20. doi: 10.1016/j.ejphar.2010.10.043. Epub 2010 Oct 27.

Abstract

Coronary ischemia and subsequent reperfusion result in deleterious effects, one of the principal ones being vascular and myocardial inflammation. Olprinone hydrochloride, a specific phosphodiesterase III inhibitor, has anti-inflammatory effects in addition to its inotropic and vasodilator effects. The purpose of this study was to examine the beneficial effects of olprinone on myocardial ischemia-reperfusion injury. Myocardial ischemia-reperfusion injury was caused by clamping the LAD (left anterior descending) coronary artery for 25 min followed by a release of the clamp allowing reperfusion for 1 h. Olprinone i.p. (0.2 mg/kg, i.p.) was administrated 15 min after ischemia. The olprinone administration significantly reduced the: (1) histological evidence of myocardial injury, (2) pro-inflammatory cytokines: tumor necrosis factor-α (TNF-α) and Interleukin-1β (IL-1β), (3) adhesion molecules: Inter-Cellular Adhesion Molecule 1 (ICAM-1) and P-Selectin, (4) nitrotyrosine formation, (5) nuclear factor kappa-B (NF-κB) expression, (6) Poly (ADP-ribose) (PAR) formation, and (7) apoptosis (Bax, Bcl-2, Fas-L and terminal deoxynucleotidyl transferase-mediated UTP end labeling (TUNEL). Based on these findings this study provides the evidence that treatment with olprinone ameliorated the inflammatory process associated with myocardial ischemia-reperfusion in rats and suggests that this drug may have potential in the treatment of various ischemia and reperfusion diseases.

MeSH terms

  • Animals
  • Apoptosis / drug effects
  • Imidazoles / pharmacology
  • Imidazoles / therapeutic use*
  • Inflammation / metabolism
  • Inflammation / prevention & control
  • Intercellular Adhesion Molecule-1 / metabolism
  • Interleukin-1beta / metabolism
  • Male
  • Myocardial Reperfusion Injury / drug therapy*
  • Myocardial Reperfusion Injury / metabolism
  • Myocardial Reperfusion Injury / pathology
  • NF-kappa B / metabolism
  • P-Selectin / metabolism
  • Phosphodiesterase 3 Inhibitors / pharmacology
  • Phosphodiesterase 3 Inhibitors / therapeutic use*
  • Poly Adenosine Diphosphate Ribose / metabolism
  • Pyridones / pharmacology
  • Pyridones / therapeutic use*
  • Rats
  • Rats, Wistar
  • Tumor Necrosis Factor-alpha / metabolism

Substances

  • Imidazoles
  • Interleukin-1beta
  • NF-kappa B
  • P-Selectin
  • Phosphodiesterase 3 Inhibitors
  • Pyridones
  • Tumor Necrosis Factor-alpha
  • Intercellular Adhesion Molecule-1
  • Poly Adenosine Diphosphate Ribose
  • olprinone