Glycogen Synthase Kinase 3β Inhibition Improves Myocardial Angiogenesis and Perfusion in a Swine Model of Metabolic Syndrome

J Am Heart Assoc. 2016 Jul 12;5(7):e003694. doi: 10.1161/JAHA.116.003694.

Abstract

Background: Inhibition of glycogen synthase kinase 3β (GSK-3β) has been reported to be cardioprotective during stressful conditions.

Methods and results: Pigs were fed a high-fat diet for 4 weeks to develop metabolic syndrome, then underwent placement of an ameroid constrictor to their left circumflex artery to induce chronic myocardial ischemia. Two weeks later, animals received either: no drug (high cholesterol control group [HCC]) or a GSK-3β inhibitor (GSK-3β inhibited group [GSK-3βI]), which were continued for 5 weeks, followed by myocardial tissue harvest. Coronary blood flow and vessel density were significantly increased in the GSK-3βI group compared to the HCC group. Expression levels of the following proteins were greater in the GSK-3βI group compared to the HCC group: vascular endothelial growth factor receptor 1 , vascular endothelial cadherin, γ-catenin, β-catenin, protein kinase B, phosphorylated forkhead box O1, and superoxide dismutase 2.

Conclusions: In the setting of metabolic syndrome, inhibition of GSK-3β increases blood flow and vessel density in chronically ischemic myocardium. We identified several angiogenic, cell survival, and differentiation pathways that include β-catenin signaling and AKT/FOXO1, through which GSK-3β appears to improve vessel density and blood flow. These results may provide a potential mechanism for medical therapy of patients suffering from coronary artery disease and metabolic syndrome.

Keywords: angiogenesis; cardiovascular diseases; diabetes mellitus; hypercholesterolemia; obesity.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Cadherins / drug effects
  • Cadherins / metabolism
  • Chronic Disease
  • Coronary Circulation / drug effects
  • Coronary Vessels / drug effects*
  • Coronary Vessels / pathology
  • Diet, High-Fat
  • Disease Models, Animal
  • Forkhead Box Protein O1 / drug effects
  • Forkhead Box Protein O1 / metabolism
  • Glycogen Synthase Kinase 3 beta / antagonists & inhibitors*
  • Heart / drug effects*
  • Indoles / pharmacology*
  • Maleimides / pharmacology*
  • Metabolic Syndrome / metabolism*
  • Myocardial Ischemia / metabolism*
  • Myocardial Ischemia / pathology
  • Myocardium / pathology*
  • Neovascularization, Physiologic / drug effects*
  • Proto-Oncogene Proteins c-akt / drug effects
  • Proto-Oncogene Proteins c-akt / metabolism
  • Superoxide Dismutase / drug effects
  • Superoxide Dismutase / metabolism
  • Sus scrofa
  • Swine
  • Vascular Endothelial Growth Factor Receptor-1 / drug effects
  • Vascular Endothelial Growth Factor Receptor-1 / metabolism
  • beta Catenin / drug effects
  • beta Catenin / metabolism
  • gamma Catenin / drug effects
  • gamma Catenin / metabolism

Substances

  • 3-(4-fluorophenylethylamino)-1-methyl-4-(2-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
  • Cadherins
  • Forkhead Box Protein O1
  • Indoles
  • Maleimides
  • beta Catenin
  • gamma Catenin
  • Superoxide Dismutase
  • superoxide dismutase 2
  • Vascular Endothelial Growth Factor Receptor-1
  • Glycogen Synthase Kinase 3 beta
  • Proto-Oncogene Proteins c-akt