AimTo observe the effect of ibrolipim on the expresstion of endothelin-1 (ET-1) and von Willebrand factor (vWF) in cultured human umbilical vein endothelial cells induced by high glucose, and to investigate its molecular mechanism.MethodsHuman umbilical vein endothelial cell-12 (HUVEC-12) were cultured respectively under normal glucose level (5.5 mmol/L), high glucose level (33.3 mmol/L), and high glucose level with ibrolipim treatment.HUVEC-12 activity or injury was assayed by methyl thiazolyl tetrazolium (MTT).The ET-1 concentrations were evaluated by radioimmunoassay.The expression of vWF in the conditioned media was tested by enzyme-linked immunosorbent assay (ELISA).Endothelial dysfunction was identified by the expression of ET-1 and vWF through reverse transcription polymerase chain reaction (RT-PCR).The protein content of ET-1 and vWF were evaluated by cell immunofluorescence.ResultsHigh glucose condition significantly weakened cell viability, and increased the expression of ET-1 and vWF.Ibrolipim treatment significantly attenuated these alterations of endothelial dysfunction.The low er con-cen trations (2, 4, 8 μmol/L) of ibrolipim improved cell viability, down-regulated the expression of ET-1 and vWF, and attenuated the cytotoxicity, however, higher concentration (16, 32 μmol/L) of ibrolipim aggravated the damage of HUVEC-12 cultured under high glucose level.ConclusionIbrolipim at low concentration can inhibit high glucose-induced endothelial dysfunction of cultured HUVEC-12, which may be related to the alternation of ET-1 and vWF expression.