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  • 标题:Human ACAT-1 and ACAT-2 Inhibitory Activities of Pentacyclic Triterpenes from the Leaves of Lycopus lucidus T URCZ .
  • 本地全文:下载
  • 作者:Woo Song Lee ; Kyung-Ran Im ; Yong-Dae Park
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:2006
  • 卷号:29
  • 期号:2
  • 页码:382-384
  • DOI:10.1248/bpb.29.382
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:

    Acyl-CoA: cholesterol acyltransferase (ACAT) catalyzes the acylation of cholesterol to cholesteryl ester with long chain fatty acids and ACAT inhibition is a useful strategy for treating hypercholesterolemia or atherosclerosis. Pentacyclic triterpenes, ursolic acid (1), oleanolic acid (2), and betulinic acid (3) were isolated from the methanol extracts of the leaves of Lycopus lucidus T URCZ . by bioassay-guided fractionation. The structures of compounds 1—3 were elucidated by their spectroscopic data analysis. Among them, betulinic acid (3) exhibited more potent human ACAT-1 and ACAT-2 inhibitory activities with IC50 values of 16.2±0.6 and 28.8±1.3 μ M , respectively.

  • 关键词:Lycopus lucidus ; acyl-CoA: cholesterol acytransferase (ACAT); pentacyclic triterpene; atherosclerosis
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