Trimucrin, an Arg-Gly-Asp containing disintegrin, attenuates myocardial ischemia-reperfusion injury in murine by inhibiting platelet function

Eur J Pharmacol. 2017 Oct 15:813:24-32. doi: 10.1016/j.ejphar.2017.07.039. Epub 2017 Jul 21.

Abstract

Trimucrin, a novel small-mass Arg-Gly-Asp (RGD)-containing disintegrin, has been demonstrated to possess anti-platelet and anti-inflammatory effect through blockade of platelet αIIbβ3 and phagocyte αvβ3 integrin. In this study, we found that the platelet-rich plasma prepared from trimucrin-treated rats platelet aggregation was diminished in response to adenosine diphosphate (ADP). We tried to determine whether trimucrin is cardioprotective in rats subjected to myocardial ischemia-reperfusion (I-R) injury. The left anterior descending coronary artery of anesthetized rats was subjected to 1h occlusion and 3h reperfusion. The animals received intravenous trimucrin or saline, and the severities of I-R-induced arrhythmia and infarction were compared. Trimucrin significantly reduced I-R-induced arrhythmias and reduced mortality, as well as infarct volume, troponin-I levels, creatine kinase, and lactate dehydrogenase activity in carotid blood compared with vehicle-treated animals during the same period. Trimucrin also improved cardiac function and survival rates after I-R injury. In addition, trimucrin concentration-dependently inhibited platelet adhesion on collagen- and fibrinogen-coated surfaces without affecting platelet counts. Trimucrin also significantly reduced neutrophil infiltration into heart tissues after I-R compared with controls. Furthermore, trimucrin treatment caused significant downregulation of Bax, Caspase-3 apoptotic proteins and upregulation of anti-apoptotic Bcl-2 protein. These results demonstrate that trimucrin exerts cardioprotective property against myocardial I-R injury mediated through antiplatele, anti-inflammatory, anti-apoptotic mechanism, as well as improvements in cardiac function.

Keywords: Anti-inflammation; Cardioprotection; Ischemia; Platelet function; Reperfusion; Trimucrin.

MeSH terms

  • Animals
  • Apoptosis / drug effects
  • Blood Platelets / drug effects*
  • Blood Platelets / physiology*
  • Cardiotonic Agents / chemistry
  • Cardiotonic Agents / pharmacology
  • Cardiotonic Agents / therapeutic use
  • Disintegrins / chemistry*
  • Hemodynamics / drug effects
  • Male
  • Mice
  • Myocardial Reperfusion Injury / drug therapy*
  • Myocardial Reperfusion Injury / pathology
  • Myocardial Reperfusion Injury / physiopathology*
  • Myocardium / pathology
  • Oligopeptides*
  • Peptides / chemistry
  • Peptides / pharmacology*
  • Peptides / therapeutic use
  • Platelet Adhesiveness / drug effects
  • Rats
  • Rats, Sprague-Dawley

Substances

  • Cardiotonic Agents
  • Disintegrins
  • Oligopeptides
  • Peptides
  • trimucrin
  • arginyl-glycyl-aspartic acid