AS-183, a novel inhibitor of acyl-CoA: cholesterol acyltransferase produced by Scedosporium sp. SPC-15549.
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 microM. 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 microM, respectively.
Kuroda
K
K
Tokyo Research Laboratories, Kyowa Hakko Kogyo Co., Ltd., Japan.
Yoshida
M
M
Uosaki
Y
Y
Ando
K
K
Kawamoto
I
I
Oishi
E
E
Onuma
H
H
Yamada
K
K
Matsuda
Y
Y
D000818:Animals; D004791:Enzyme Inhibitors / Q000302:isolation & purification / Q000378:metabolism / Q000494:pharmacology; D005285:Fermentation; D005663:Furans / Q000302:isolation & purification* / Q000494:pharmacology; D008297:Male; D003904:Mitosporic Fungi / Q000378:metabolism*; D011817:Rabbits; D002785:Sterol O-Acyltransferase / Q000037:antagonists & inhibitors*
D004791:Enzyme Inhibitors; D005663:Furans; C083647:2,4-dimethyl-2-hydroxy-5-(1,3,5,7-tetramethylnonyl)-3(2H)furanone; D002785:Sterol O-Acyltransferase