title: Amidepsines, inhibitors of diacylglycerol acyltransferase produced by Humicola sp. FO-2942. I. Production, isolation and biological properties.
abstract: Humicola sp. FO-2942, a soil isolate, was found to produce a series of new inhibitors of diacylglycerol acyltransferase (DGAT). Three active compounds, designated amidepsines A, B and C, were isolated from the fermentation broth of the producing strain by solvent extraction, silica gel column chromatography, ODS column chromatography and HPLC. Amidepsines inhibit DGAT activity with IC50 values of 10.2 approximately 51.6 microM in an enzyme assay system using rat liver microsomes. Amidepsines also showed specific inhibition of triacylglycerol formation in intact Raji cells, indicating that they inhibit DGAT activity in living cells.
authors.affiliation: Research Center for Biological Function, Kitasato Institute, Tokyo, Japan.
authors.forename: H
authors.initials: H
authors.lastname: Tomoda
authors.forename: M
authors.initials: M
authors.lastname: Ito
authors.forename: N
authors.initials: N
authors.lastname: Tabata
authors.forename: R
authors.initials: R
authors.lastname: Masuma
authors.forename: Y
authors.initials: Y
authors.lastname: Yamaguchi
authors.forename: S
authors.initials: S
authors.lastname: Omura
mesh_terms: D000217:Acyltransferases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D000818:Animals; D051048:Diacylglycerol O-Acyltransferase; D005285:Fermentation; D005658:Fungi; D062385:Hydroxybenzoates / Q000302:isolation & purification* / Q000494:pharmacology*; D008297:Male; D008826:Microbial Sensitivity Tests; D008862:Microsomes, Liver / Q000187:drug effects / Q000201:enzymology; D015394:Molecular Structure; D051381:Rats
chemical_list: D062385:Hydroxybenzoates; C096617:amidepsine A; C096618:amidepsine B; C096619:amidepsine C; D000217:Acyltransferases; D051048:Diacylglycerol O-Acyltransferase