K. Kuroda et al., AS-183, A NOVEL INHIBITOR OF ACYL-COA - CHOLESTEROL ACYLTRANSFERASE PRODUCED BY SCEDOSPORIUM SP SPC-15549, Journal of antibiotics, 46(8), 1993, pp. 1196-1202
A novel compound, AS-183, which inhibits acyl-CoA: cholesterol acyltra
nsferase (ACAT), was isolated from the culture broth of a fungus, Sced
osporium sp. SPC-15549. AS-183 inhibited ACAT activity in an enzyme as
say system using rabbit liver microsomes with an IC50 value of 0.94 mu
M. 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, respecti
vely.