Liraglutide prevents β-cell apoptosis via inactivation of NOX2 and its related signaling pathway

J Diabetes Complications. 2019 Apr;33(4):267-277. doi: 10.1016/j.jdiacomp.2018.12.013. Epub 2019 Jan 2.

Abstract

Aims: High glucose (HG)-induced pancreatic β-cell apoptosis may be a major contributor to the progression of diabetes mellitus (DM). NADPH oxidase (NOX2) has been considered a crucial regulator in β-cell apoptosis. This study was designed to evaluate the impact of GLP-1 receptor agonist (GLP-1Ra) liraglutide on pancreatic β-cell apoptosis in diabetes and the underlying mechanisms involved.

Methods: The diabetic rat models induced by streptozotocin (STZ) and a high fat diet (HFD) received 12 weeks of liraglutide treatment. Hyperglycemic clamp test was carried out to evaluate β-cell function in vivo. Flow cytometry analysis was used to measure apoptosis rates in vitro. DCFH-DA method was used to detected ROS level in vivo and in vitro.

Results: Liraglutide significantly improved islet function and morphology in diabetic rats and decreased cell apoptosis rates. Thr183/Thr185 p-JNK1/2 and NOX2 levels reduced in diabetic rats and HG-induced INS-1 cell following liraglutide treatment. In addition, liraglutide upregulated the phosphorylation of AMPKα (p-AMPKα), which prevented NOX2 activation and alleviated HG-induced β-cell apoptosis.

Conclusion: The p-AMPKα/NOX2/JNK1/2 pathway is essential for liraglutide to attenuate HG-induced β-cell apoptosis, which further proves that GLP-1Ras may become promising therapeutics for diabetes mellitus.

Keywords: Apoptosis; GLP-1; Liraglutide; NOX2; β-Cells.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Apoptosis / drug effects*
  • Cells, Cultured
  • Cytoprotection / drug effects
  • Diabetes Mellitus, Experimental / chemically induced
  • Diabetes Mellitus, Experimental / drug therapy
  • Diabetes Mellitus, Experimental / metabolism
  • Diabetes Mellitus, Experimental / pathology*
  • Down-Regulation / drug effects
  • Insulin-Secreting Cells / drug effects*
  • Insulin-Secreting Cells / physiology
  • Liraglutide / pharmacology*
  • Liraglutide / therapeutic use
  • Male
  • Mice
  • NADPH Oxidase 2 / metabolism*
  • Rats
  • Rats, Sprague-Dawley
  • Signal Transduction / drug effects
  • Streptozocin

Substances

  • Streptozocin
  • Liraglutide
  • NADPH Oxidase 2