The Effects of Novel AMPK Activator on Human Vascular Endothelial Cells

Abstract

Adenosine 5'-monophosphate-activated protein kinase (AMPK) is a key regulator of cellular energy homeostasis and involved in modulating several important cellular mechanism including inflammation. Here we demonstrated that a novel AMPK activator, ENERGI-F704, dose-dependently activated AMPK in human umbilical vein endothelial cells (HUVECs). The pharmacological AMPK inhibitor, compound C, abolished the phosphorylation of threonine 172 residue on AMPK induced by ENERGI-F704. Importantly, ENERGI-F704 treatment did not affect HUVECs viability at the tested concentration. It was also observed that ENERGI-F704 significantly reduced the expression of inflammation cytokine, IL-6, in the high glucose cultured HUVECs during the long culture period. Furthermore, ENERGI-F704 suppressed the high glucose induced monocytotic adhesion to HUVECs. Collectively, our data demonstrated that ENERGI-F704 is of use in the application of attenuating the high glucose induced chronic inflammation in endothelial cells. 