AS-183, A NOVEL INHIBITOR OF ACYL-COA - CHOLESTEROL ACYLTRANSFERASE PRODUCED BY SCEDOSPORIUM SP SPC-15549

被引:24
作者
KURODA, K
YOSHIDA, M
UOSAKI, Y
ANDO, K
KAWAMOTO, I
OISHI, E
ONUMA, H
YAMADA, K
MATSUDA, Y
机构
[1] KYOWA HAKKO KOGYO CO LTD,TOKYO RES LABS,3-6-6 ASAHIMACHI,MACHIDA,TOKYO 194,JAPAN
[2] KYOWA HAKKO KOGYO CO LTD,PHARMACEUT RES LABS,NAGAIZUMI,SHIZUOKA 411,JAPAN
关键词
D O I
10.7164/antibiotics.46.1196
中图分类号
Q81 [生物工程学(生物技术)]; Q93 [微生物学];
学科分类号
071005 ; 0836 ; 090102 ; 100705 ;
摘要
A novel compound, AS-183, which inhibits acyl-CoA: cholesterol acyltransferase (ACAT), was isolated from the culture broth of a fungus, Scedosporium sp. SPC-15549. AS-183 inhibited ACAT activity in an enzyme assay system using rabbit liver microsomes with an IC50 value of 0.94 muM. AS-183 also inhibited cholesterol ester formation in HepG2, CaCo2, and THP-1 cells with IC50 values of 18.1, 25.5, and 34.5 muM, respectively.
引用
收藏
页码:1196 / 1202
页数:7
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