Author/Authors :
Wu, Qiong Jilin University - School of Life Sciences - National Engineering Laboratory of AIDS Vaccine, China , Li, Jian-zhuo Jilin University - School of Life Sciences - Key Laboratory Molecular Enzymology and Engineering of Ministry of Education, China , Zhao, Tian-yi Jilin University - School of Life Sciences - National Engineering Laboratory of AIDS Vaccine, China , Li, Tian-bao Jilin University - School of Life Sciences - National Engineering Laboratory of AIDS Vaccine, China , Wang, Jia-xin Jilin University - School of Life Sciences - Key Laboratory Molecular Enzymology and Engineering of Ministry of Education, China , Sui, Yuan Jilin University - School of Life Sciences - National Engineering Laboratory of AIDS Vaccine, China , Ma, Jun-feng Jilin University - School of Life Sciences - National Engineering Laboratory of AIDS Vaccine, China , Li, Wan-nan Jilin University - School of Life Sciences - Key Laboratory Molecular Enzymology and Engineering of Ministry of Education, China , Gao, Xue-feng Jilin University - School of Life Sciences - National Engineering Laboratory of AIDS Vaccine, China , Xing, Shu Jilin University - School of Life Sciences - National Engineering Laboratory of AIDS Vaccine, China , Fu, Xue-qi Jilin University - School of Life Sciences - Key Laboratory Molecular Enzymology and Engineering of Ministry of Education, China
Abstract :
The inhibition of 3-hydroxy-3-methylglutaryl CoA reductase (HMGCR) is considered able to decrease serum cholesterol levels and dramatically reduce the risk for cardiovascular and cerebrovascular diseases. The statins, competitive inhibitors of HMGCR, have been employed to control hypercholesterolemia. But their side effects, especially their safety of long-term administration have attracted great attention. Therefore, there is still an urgent requirement for the development of safer inhibitors of HMGCR with less serious side effects. In this study, we cloned and purified the catalytic domain of human HMGCR (△HMGCR), and applied the method of Ultra Performance Liquid Chromatography (UPLC) to assay △HMGCR activity and screen its inhibitors from natural products. The results indicated that EGCG can inhibit △HMGCR in the presence of some glycerol in vitro and can decrease cellular total cholesterol in HepG2 cells. As a consequence, it is promising to put EGCG into the development of hypolipidemic health product.
Keywords :
HMGCR , EGCG , UPLC , inhibitor , glycerol
