The DPP-4 inhibitor linagliptin counteracts stroke in the normal and diabetic mouse brain: a comparison with glimepiride

Diabetes. 2013 Apr;62(4):1289-96. doi: 10.2337/db12-0988. Epub 2012 Dec 3.

Abstract

Type 2 diabetes is a strong risk factor for stroke. Linagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor in clinical use against type 2 diabetes. The aim of this study was to determine the potential antistroke efficacy of linagliptin in type 2 diabetic mice. To understand whether efficacy was mediated by glycemia regulation, a comparison with the sulfonylurea glimepiride was done. To determine whether linagliptin-mediated efficacy was dependent on a diabetic background, experiments in nondiabetic mice were performed. Type 2 diabetes was induced by feeding the mice a high-fat diet for 32 weeks. Mice were treated with linagliptin/glimepiride for 7 weeks. Stroke was induced at 4 weeks into the treatment by transient middle cerebral artery occlusion. Blood DPP-4 activity, glucagon-like peptide-1 (GLP-1) levels, glucose, body weight, and food intake were assessed throughout the experiments. Ischemic brain damage was measured by determining stroke volume and by stereologic quantifications of surviving neurons in the striatum/cortex. We show pronounced antistroke efficacy of linagliptin in type 2 diabetic and normal mice, whereas glimepiride proved efficacious against stroke in normal mice only. These results indicate a linagliptin-mediated neuroprotection that is glucose-independent and likely involves GLP-1. The findings may provide an impetus for the development of DPP-4 inhibitors for the prevention and treatment of stroke in diabetic patients.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Diabetes Mellitus, Experimental / complications*
  • Diabetes Mellitus, Experimental / drug therapy
  • Dietary Fats / adverse effects
  • Dipeptidyl-Peptidase IV Inhibitors / therapeutic use*
  • Hypoglycemic Agents / therapeutic use*
  • Linagliptin
  • Male
  • Mice
  • Obesity / complications
  • Obesity / etiology
  • Purines / therapeutic use*
  • Quinazolines / therapeutic use*
  • Stroke / etiology
  • Stroke / prevention & control*
  • Sulfonylurea Compounds / therapeutic use*

Substances

  • Dietary Fats
  • Dipeptidyl-Peptidase IV Inhibitors
  • Hypoglycemic Agents
  • Purines
  • Quinazolines
  • Sulfonylurea Compounds
  • Linagliptin
  • glimepiride