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 0.94μM. AS-183 also inhibit...

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Bibliographic Details
Published in:Journal of antibiotics 1993/08/25, Vol.46(8), pp.1196-1202
Main Authors: KURODA, KAZUTOSHI, YOSHIDA, MAYUMI, UOSAKI, YOUICHI, ANDO, KATSUHIKO, KAWAMOTO, ISAO, OISHI, EIKO, ONUMA, HIROKI, YAMADA, KOJI, MATSUDA, YUZURU
Format: Article
Language:English
Subjects:
Animals
Biological and medical sciences
Enzyme Inhibitors - isolation & purification
Enzyme Inhibitors - metabolism
Enzyme Inhibitors - pharmacology
Fermentation
Furans - isolation & purification
Furans - pharmacology
General and cellular metabolism. Vitamins
Male
Medical sciences
Mitosporic Fungi - metabolism
Pharmacology. Drug treatments
Rabbits
Sterol O-Acyltransferase - antagonists & inhibitors
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Summary: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 0.94μM. AS-183 also inhibited cholesterol ester formation in HepG2, CaCo2, and THP-1 cells with IC50 values of 18.1, 25.5, and 34.5μM, respectively.
ISSN:0021-8820
1881-1469
DOI:10.7164/antibiotics.46.1196