Exendin-4 directly improves endothelial dysfunction in isolated aortas from obese rats through the cAMP or AMPK-eNOS pathways

Diabetes Res Clin Pract. 2012 Sep;97(3):453-60. doi: 10.1016/j.diabres.2012.04.001. Epub 2012 May 5.

Abstract

Aims: To determine whether exendin-4 might directly improve endothelial dysfunction in aorta isolated from high-fat diet-induced obese rats.

Methods: Wistar rats were randomly divided into control and obesity (OB) groups and fed. Vascular segments of obese rats were incubated in organ bath in the presence or absence of exendin-4. Nitric oxide (NO) production and nuclear transcription factor kappa B expression in vascular rings were measured. The aortic rings of the obese rats were then incubated in an organ bath with exendin-4 in the presence or absence of the following inhibitors: the AMPK, the adenylate cyclase and the NO synthase inhibitor.

Results: The maximum endothelium-dependent vasodilatation (EDV) value was severely reduced in the OB group. Exendin-4 treatment significantly increased the NO level, improved endothelium-dependent vasodilatation and reduced expression of NF-κB in the obese group. The beneficial effect of exendin-4 on EDV in obese rats was partly attenuated in the presence of the specific inhibitors.

Conclusion: Exendin-4 directly improves impaired EDV of aortae from obese rats. The beneficial effect of exendin-4 appears to be mediated in part via stimulation of cAMP/AMPK-related signalling pathways and enhancement of endothelial nitric oxide synthase activity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenylate Kinase / metabolism*
  • Adenylate Kinase / physiology
  • Animals
  • Aorta / drug effects*
  • Aorta / pathology
  • Aorta / physiopathology
  • Cells, Cultured
  • Cyclic AMP / metabolism*
  • Cyclic AMP / physiology
  • Drug Evaluation, Preclinical
  • Endothelium, Vascular / drug effects*
  • Endothelium, Vascular / physiopathology
  • Exenatide
  • Hypoglycemic Agents / pharmacology
  • Male
  • Nitric Oxide Synthase Type III / metabolism*
  • Nitric Oxide Synthase Type III / physiology
  • Obesity / complications
  • Obesity / pathology*
  • Obesity / physiopathology
  • Organ Culture Techniques
  • Peptides / pharmacology*
  • Rats
  • Rats, Wistar
  • Signal Transduction / drug effects
  • Signal Transduction / physiology
  • Venoms / pharmacology*

Substances

  • Hypoglycemic Agents
  • Peptides
  • Venoms
  • Exenatide
  • Cyclic AMP
  • Nitric Oxide Synthase Type III
  • Nos3 protein, rat
  • Adenylate Kinase