Protective effects of 7-difluoromethyl-5,4'-dimethoxygenistein against human aorta endothelial injury caused by lysophosphatidyl choline.

7-Difluoromethyl-5,4'-dimethoxygenistein (DFMG) is an active new derivative of genistein (GEN). It has shown effective protection in vascular endothelial injury. To further investigate its potential protective effects and its mechanism probably related to atherosclerosis, in present study, human aorta endothelial cells (HAECs) were chosen and treated with various concentrations of lysophosphatidyl choline (LPC) to establish an experimental model. Results showed that 10.0 μmol/l of LPC was optimal for inducing HAEC injury. DFMG pretreatment was able to prevent HAEC injury induced by LPC and restore cell viability in a concentration-dependent manner. The protective efficacy of DFMG (10.0 μmol/l) was significantly greater than that of GEN (10.0 μmol/l) and vitamin E (50.0 μmol/l). The mechanisms underlying the protective effects of DFMG are related to the activation of the antioxidant enzymes superoxide dismutase (SOD) and glutathione peroxidase and to the clearance of intracellular reactive oxygen species. DFMG inhibits the apoptosis of HAECs mediated by LPC involving the blockage of the mitochondrial apoptotic pathway.