7-Difluoromethyl-5, 4’-dimethoxygenistein (DFMG), prepared by the difluoromethylation and alkylation of Genistein, is a new active chemical entity. In this study, we investigated the inhibitory effect of DFMG on Lysophosphatidyl choline (LPC)-induced apoptosis of human umbilical vein endothelial cells-12 (HUVEC-12) through mitochondrial apoptosis pathway. Lysophosphatidyl choline (LPC) was used to build apoptosis model in HUVEC-12 cells. The apoptosis rate in each group was determined by using flow cytometry of ANNEXIN V/PI staining. The mean ffluorescence intensity (MFI) of mitochondria mmembrane ppotential (MMP) was determined by using flow cytometry. The expression levels of cytochrome C (CytC), p-JNK and PARP were detected by performing western blotting assay. The activities of caspase-3 and caspase-9 were detected by a colorimetric method with caspase colorimetric assay kits. As compared with the control group, DFMG notably decreased the apoptosis rate, the MFI of the MMP, and the generation of Reactive Oxygen Species (ROS) induced by LPC. In addition, DFMG had suppressive effects on the expressions of CytC, P-JNK, and PARP, as well as on the activities of caspase-3 and caspase-9 in LPC-treated HUVEC-12 cells. DFMG can antagonize LPC-induced apoptosis of HUVE-12 cells. The underlying mechanism may be involved in the inhibition of mitochondrial apoptosis pathway.
Keywords: Apoptosis, 7-Difluoromethyl-5, 4'-dimethoxygenistein, mitochondrial, Cytochrome C, Lysophosphatidyl choline.