title: Epigallocatechin-3-gallate (EGCG) inhibits 3-hydroxy-3-methylglutaryl-CoA reductase in the presence of glycerol.
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.
authors.affiliation: National Engineering Laboratory of AIDS Vaccine, School of Life Sciences, Jilin University, Changchun, PR China.
authors.forename: Qiong
authors.initials: Q
authors.lastname: Wu
authors.affiliation: Key Laboratory Molecular Enzymology and Engineering of Ministry of Education, School of Life Sciences, Jilin University, Changchun, PR China.
authors.forename: Jian-zhuo
authors.initials: JZ
authors.lastname: Li
authors.affiliation: National Engineering Laboratory of AIDS Vaccine, School of Life Sciences, Jilin University, Changchun, PR China.
authors.forename: Tian-yi
authors.initials: TY
authors.lastname: Zhao
authors.affiliation: National Engineering Laboratory of AIDS Vaccine, School of Life Sciences, Jilin University, Changchun, PR China.
authors.forename: Tian-bao
authors.initials: TB
authors.lastname: Li
authors.affiliation: Key Laboratory Molecular Enzymology and Engineering of Ministry of Education, School of Life Sciences, Jilin University, Changchun, PR China.
authors.forename: Jia-xin
authors.initials: JX
authors.lastname: Wang
authors.affiliation: National Engineering Laboratory of AIDS Vaccine, School of Life Sciences, Jilin University, Changchun, PR China.
authors.forename: Yuan
authors.initials: Y
authors.lastname: Sui
authors.forename: Jun-feng
authors.initials: JF
authors.lastname: Ma
authors.forename: Wan-nan
authors.initials: WN
authors.lastname: Li
authors.forename: Xue-feng
authors.initials: XF
authors.lastname: Gao
authors.forename: Shu
authors.initials: S
authors.lastname: Xing
authors.forename: Xue-qi
authors.initials: XQ
authors.lastname: Fu
mesh_terms: D002392:Catechin / Q000031:analogs & derivatives* / Q000494:pharmacology; D005990:Glycerol / Q000494:pharmacology*; D056945:Hep G2 Cells; D006801:Humans; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors / Q000494:pharmacology*
chemical_list: D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors; D002392:Catechin; C045651:epigallocatechin gallate; D005990:Glycerol