Recombinant Human Alpha-1 Antitrypsin-Fc Fusion Protein Reduces Mouse Myocardial Inflammatory Injury After Ischemia-Reperfusion Independent of Elastase Inhibition

J Cardiovasc Pharmacol. 2016 Jul;68(1):27-32. doi: 10.1097/FJC.0000000000000383.

Abstract

Background: Alpha-1-antitrypsin (AAT) is an abundant plasma protein with neutrophil elastase-inhibiting activity, and AAT is available as a plasma-derived therapeutic (pAAT). In experimental myocardial infarction, pAAT reduced acute inflammatory injury because of ischemia-reperfusion. The aim of the present study was to assess the properties of a recombinant protein composed of human AAT fused to the human immunoglobulin (Ig) G1 Fc fragment (rhAAT-Fc) in experimental myocardial infarction.

Methods: Ten-week-old CD1 male mice underwent transient occlusion (30 minutes) of the left anterior coronary artery. rhAAT-Fc (2 mg/kg) or pAAT (60 mg/kg) were administered upon reperfusion. We used human plasma-derived Ig (2 mg/kg) or a matching volume of NaCl 0.9% as control solutions. After 24 hours, infarct size and caspase-1 activity were quantified. The left ventricular ejection fraction (LVEF) was measured by echocardiography at 24 hours and 7 days. A variant of rhAAT-Fc lacking elastase inhibition activity, rhAAT-Fc, was also tested.

Results: The rhAAT-Fc induced a significant reduction in infarct size (P < 0.01 vs. all controls, P > 0.05 vs. pAAT). Caspase-1 activity was reduced to the same degree with rhAAT-Fc and pAAT (-70%; P < 0.05; P > 0.05 rhAAT-Fc vs. pAAT). The effects on infarct size after a single administration were reflected by preservation of LVEF at 24 hours and 7 days (all P < 0.05). rhAAT-Fc without elastase inhibiting activity, rhAAT-Fc, conferred comparable effects on infarct size, caspase-1 activity, and LVEF (P > 0.2 vs. rhAAT-Fc).

Conclusions: The pAAT and recombinant human AAT-Fc reduce the acute myocardial inflammatory injury after ischemia-reperfusion in the mouse leading to preservation of viable myocardium and systolic function, independent on the effects on neutrophil elastase.

MeSH terms

  • Animals
  • Cardiovascular Agents / pharmacology*
  • Caspase 1 / metabolism
  • Disease Models, Animal
  • Humans
  • Immunoglobulin Fc Fragments / pharmacology*
  • Leukocyte Elastase / antagonists & inhibitors
  • Leukocyte Elastase / metabolism
  • Male
  • Mice
  • Myocardial Infarction / metabolism
  • Myocardial Infarction / pathology
  • Myocardial Infarction / physiopathology
  • Myocardial Infarction / prevention & control*
  • Myocardial Reperfusion Injury / metabolism
  • Myocardial Reperfusion Injury / pathology
  • Myocardial Reperfusion Injury / physiopathology
  • Myocardial Reperfusion Injury / prevention & control*
  • Myocarditis / metabolism
  • Myocarditis / pathology
  • Myocarditis / physiopathology
  • Myocarditis / prevention & control*
  • Myocardium / metabolism
  • Myocardium / pathology
  • Recombinant Fusion Proteins / pharmacology
  • Stroke Volume / drug effects
  • Time Factors
  • Tissue Survival
  • Ventricular Function, Left / drug effects
  • alpha 1-Antitrypsin / pharmacology*

Substances

  • Cardiovascular Agents
  • Immunoglobulin Fc Fragments
  • Recombinant Fusion Proteins
  • SERPINA1 protein, human
  • alpha 1-Antitrypsin
  • Leukocyte Elastase
  • Caspase 1