2,3,22,23-tetrahydroxyl-2,6,10,15,19,23-hexamethyl-6,10,14,18-tetracosatetraene, an acyclic triterpenoid isolated from the seeds of Alpinia katsumadai, Inhibits acyl-CoA : cholesterol acyltransferase activity.

作者: Soon-Yong Choi , Moon Hee Lee , Jung Ho Choi , Young Kook Kim

DOI: 10.1248/BPB.B12-00617

关键词:

摘要: In order to isolate a cholesterol-lowering compound from Alpinia katsumadai, an inhibitor for acyl-CoA : cholesterol acyltransferase (ACAT), enzyme responsible the ester formation in liver, was purified, its chemical structure determined, and vivo vitro inhibition activities were performed. high fat diet mouse model, we discovered that ethanol extract of katsumadai reduced plasma cholesterol, triglyceride, low density lipoprotein (LDL) levels. An acyclic triterpenoid showing ACAT inhibitory activity isolated seeds A. katsumadai. By NMR spectroscopic analysis (1)H-NMR, (13)C-NMR, (1)H-(1)H correlation spectroscopy, heteronuclear multiple bond connectivity (HMBC), hetero multiquantum coherence (HMQC) nuclear Overhauser effect, 2,3,22,23-tetrahydroxyl-2,6,10,15,19,23-hexamethyl-6,10,14,18-tetracosatetraene (1), elucidated. The found be rat liver microsomes with IC(50) values 47.9 µM. It also decreased cholesteryl 26 µM human hepatocyte HepG2 cell. experimental study revealed has hypolipemic effect mice, activity, potential novel therapeutic approach treatment hyperlipidemia atherosclerosis.

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