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- Title
Epigallocatechin-3-gallate (EGCG) inhibits 3-hydroxy-3-methylglutaryl-CoA reductase in the presence of glycerol.
- Authors
Qiong Wu; Jian-zhuo Li; Tian-yi Zhao; Tian-bao Li; Jia-xin Wang; Yuan Sui; Jun-feng Ma; Wan-nan Li; Xue-feng Gao; Shu Xing; Xue-qi Fu
- 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 (ΔHMGCR), and applied the method of Ultra Performance Liquid Chromatography (UPLC) to assay ΔHMGCR activity and screen its inhibitors from natural products. The results indicated that EGCG can inhibit ΔHMGCR 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.
- Subjects
EPIGALLOCATECHIN gallate; REDUCTASE inhibitors; GLYCERIN; BLOOD cholesterol; CEREBROVASCULAR disease; CARDIOVASCULAR diseases
- Publication
Pakistan Journal of Pharmaceutical Sciences, 2014, Vol 27, Issue 6, p1905
- ISSN
1011-601X
- Publication type
Article