Delayed, oral pharmacological inhibition of calpains attenuates adverse post-infarction remodelling

Cardiovasc Res. 2017 Jul 1;113(8):950-961. doi: 10.1093/cvr/cvx073.

Abstract

Calpains activate during myocardial ischemia-reperfusion and contribute to reperfusion injury. Studies in transgenic animals with altered calpain/calpastatin system subjected to permanent ischemia suggest that calpains are also involved in post-infarction remodelling and heart failure.

Aims: To determine whether delayed oral administration of the calpain inhibitor SNJ-1945 reduces adverse myocardial remodelling and dysfunction following transient coronary occlusion.

Methods and results: Male Sprague-Dawley rats were subjected to 30 min of ischemia followed by 21 days of reperfusion and received the calpain inhibitor SNJ-1945 intraperitoneally at the onset of reperfusion (Acute group), orally starting after 24 h of reperfusion and for 14 days (Chronic group), or the combination of both treatments. Calpain-1 and calpain-2 protein content increased and correlated with higher calpain activity in control hearts. Administration of SNJ-1945 attenuated calpain activation, and reduced scar expansion, ventricular dilation and dysfunction in both acute and chronic groups. Acute treatment reduced infarct size in hearts reperfused for 24 h and inflammation measured after 3 days. Delayed, chronic oral administration of SNJ-1945 attenuated inflammation, cardiomyocyte hypertrophy and collagen infiltration in the non-infarcted myocardium at 21 days in correlation with increased levels of IĸB and reduced NF-ĸB activation. In cultured fibroblasts, SNJ-1945 attenuated TGF-β1-induced fibroblast activation.

Conclusions: Our data demonstrate for the first time that long-term calpain inhibition is possible with delayed oral treatment, attenuates adverse post-infarction remodelling, likely through prevention of NF-ĸB activation, and may be a promising therapeutic intervention to prevent adverse remodelling and heart failure in patients with acute myocardial infarction.

Keywords: Calpain; Ischemia/reperfusion; Post-infarction remodelling.

MeSH terms

  • Animals
  • Calcium-Binding Proteins / drug effects
  • Calcium-Binding Proteins / metabolism
  • Calpain / antagonists & inhibitors*
  • Calpain / metabolism
  • Carbamates / administration & dosage
  • Carbamates / pharmacology*
  • Glycoproteins / administration & dosage
  • Glycoproteins / pharmacology*
  • Heart / drug effects
  • Heart / physiopathology
  • Male
  • Myocardial Infarction / drug therapy*
  • Myocardial Infarction / metabolism
  • Myocardial Reperfusion Injury / prevention & control*
  • Myocardium / metabolism*
  • Rats, Sprague-Dawley

Substances

  • ((1S)-1-((((1S)-1-benzyl-3-cyclopropylamino-2,3-di-oxopropyl)amino)carbonyl)-3-methylbutyl)carbamic acid 5-methoxy-3-oxapentyl ester
  • Calcium-Binding Proteins
  • Carbamates
  • Glycoproteins
  • calpain inhibitors
  • calpastatin
  • Calpain