The Lipid-lowering Activity Of 2-(4-methoxyphenoxy) Propionic Acid

Hyperlipidemia is the main cause of atherosclerosis, which may lead to cerebral stroke, coronary heart disease, myocardial infarction, and a series of other cardiovascular disease. Because hyperlipidemia has caused serious threat to human health and life, it has very important significance to find effective and reliable cholesterol-lowering drugs.2-(4-methoxy phenoxy) propionic acid(HMPP) was first found in coffee beans, and it has been approved as one kind of food additives by FDA in the 1980 s. Having been consumed for decades of years, HMPP did not show any adverse reaction to people, which may prove this compound’s high safety. Containing the functional groups of bert cholesterol-lowering drugs, HMPP may have effect in reducing blood lipid concentration. So in this paper the effect of HMPP on the hyperlipidemia of was studied. The main contents are as follows:1. R-HMPP and S-HMPP were synthesized by L-ethyl lactate, D-ethyl lactate, p-toluene sulfonyl chloride and the methoxy phenol and the synthesis conditions were optimized. The experimental results show that with the dichloromethane as solvent, the optical purity of the product is highest, and the e.e value of the product is 98.15%.2. The resolution of HMPP catalyzed by lipase Novozym-435 was studied, and the results show that: when HMPP ethyl ester and R- phenethylamine were reacted as substrate at 30 ℃ in tertiary, the effect of resolution is best and the e.e value is 63.34%.3. In this paper the effects of SMPP on the mice hyperlipidemia was investigated, and the expression level of PPAR-α、LPL、FATP、HMGCOAR、SREBP2、CYP7A1、LDLR were detected by RT-PCR. The result showed that compared with HFCON group, SMPP reduced serum TC, TG, LDL level and increased HDL level significantly, which may be determined by upregulating the expression of PPAR-α and then increase the expression level of LPL、FATP、HMGCOAR、SREBP2、CYP7A1、LDLR, which play an important role in keep the balance of lipid in the mice.