Syntesis Of 7-Difluoromethylyl-5, 4'-Di-substituted-alkoxyl Isoflavone Compounds And Determination Of Their Protective Activities For Vascular Endotheliium Injury By Oxidative Stress

Genistein(5,7,4'-trihydroxyl isoflavone) , a typical phytoestrogen, is a isoflavone extracted from soy mainly. Genistein(GEN) possess a broad range of pharmacological properties including anti-oxidant, anti-cancer and anti-inflammatory properties. However, most of their activities were low because flavonoids were not or little absorbed in intestines. Therefore, we may take GEN as lead compound in order to design various target compounds.It is known that the introduction of the CHF₂ group into organic molecules often changes their physiological, physical and chemical properties dramatically. Besides, extension or bifurcation of hydrocarbon chain may effect their bioactivity.Vascular endothelium injury is considered to be initial in the development of atherosaderosis (AS). Eendothelium injury may lead to endothelial cells(EEC) apoptosis, which han major potential implication in atherosaderotic plague development and stability. Moreever, EEC apoptosis will aggravate other vascular disease in patients with diabetes or hypertension. So, EEC apoptosis is considered to play key role in vascular disease.The expremental research has demonstrated that genistein possess the protective effect of vascular endothelium damage and suppress endothelial cell apoptosis by oxidative stress. It is reported that the adhesion between endothelial cell and mononuclear cell or leucocyte is pristine feature and key procedure of atherosclerosis which is mediate by adhesion molecule. Vascular endothelial cell is impairment by oxidation induction and many adhesion molecules are expressed on cell surface, majority of them are E-selectin, ICAM-1, p-selectin and VCAM-1. The endothelial cell and the mononuclear cell synthesis and the release tumor necrosis factor - alpha (TNF- alpha) and the interleukin- 6 (IL - 6) participating in the immunity function which with organism inflammation, the organization damages, can affect the function of lymphocyte, adjusting inflammation process. The...