AimTo observe the effect of glucagon-like peptide-1 (GLP-1) receptor agonists exenatide on nuclear factor-κB (NF-κB) activity as well as the expression of its downstream inflammatory cytokins such as intercellular adhesion molecule-1 (ICAM-1) and vascular cell adhesion molecule-1 (VCAM-1) induced by high glucose in human umbilical vein endothelial cells (HUVEC) and to explore mechanism of protective effect of exenatide on vascular complication of diabetes.MethodsHUVEC were cultured in vitro and incubated under serum-free conditions with 25 mmol/L glucose for 48 hours.Exenatide at different concentrations (10－8 mol/L, 10－7 mol/L and 10－6 mol/L) was added concurrently with glucose stimulation.Meanwhile ICAM-1 and VCAM-1 in the cell culture supernatant was detected by enzyme-linked immunosorbent assay (ELISA).The expression of NF-κB p65, ICAM-1 and VCAM-1 mRNA were detected by reverse transcription-polymerase chain reaction (RT-PCR).Results25 mmol/L D-glucose significantly increased NF-κB p65 mRNA expression as well as the supernatant content and mRNA expression of ICAM-1 and VCAM-1 in HUVEC (p<0.01)， which was inhibited by different concentrations of exenatide (p<0.01)， in a dose-dependent manner.ConclusionsGLP-1 receptor agonist exenatide could improve endothelial dysfunction via inhibition of NF-κB activity and its downstream inflammatory response in vascular endothelial cells induced by high glucose in a dose-dependent manner, which could prevent and improve vascular complication of diabetes.