title: Clonoamide, a new inhibitor of sterol O-acyltransferase, produced by Clonostachys sp. BF-0131.
abstract: A new compound designated as clonoamide was isolated from a culture broth of the fungus Clonostachys sp. BF-0131 by solvent extraction, Diaion HP20 column chromatography, octadecylsilyl column chromatography and preparative HPLC as an inhibitor of sterol O-acyltransferase (SOAT). The structure of clonoamide was elucidated as 2-oxo-9E,11E-tridecandienyl acetamide by various spectral analyses including NMR. The compound inhibited SOAT1 and SOAT2 isozymes with IC50 values of 39 and 110 μm, respectively, in a cell-based assay using SOAT1- and SOAT2-expressing Chinese hamster ovary cells.
authors.affiliation: Graduate School of Pharmaceutical Sciences, Kitasato University, Tokyo, Japan.
authors.forename: Keisuke
authors.initials: K
authors.lastname: Kobayashi
authors.affiliation: School of Pharmaceutical Sciences, Kitasato University, Tokyo, Japan.
authors.forename: Nobuaki
authors.initials: N
authors.lastname: Tsukasaki
authors.affiliation: Graduate School of Pharmaceutical Sciences, Kitasato University, Tokyo, Japan.|School of Pharmaceutical Sciences, Kitasato University, Tokyo, Japan.
authors.forename: Ryuji
authors.initials: R
authors.lastname: Uchida
authors.affiliation: Graduate School of Pharmaceutical Sciences, Kitasato University, Tokyo, Japan.|Chugai Pharmaceutical Co., Ltd, Tokyo, Japan.
authors.forename: Yuichi
authors.initials: Y
authors.lastname: Yamaguchi
authors.affiliation: Graduate School of Pharmaceutical Sciences, Kitasato University, Tokyo, Japan.|School of Pharmaceutical Sciences, Kitasato University, Tokyo, Japan.
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Tomoda
mesh_terms: D000081:Acetamides / Q000737:chemistry* / Q000378:metabolism; D000818:Animals; D000890:Anti-Infective Agents / Q000494:pharmacology; D016466:CHO Cells; D002522:Chlorocebus aethiops; D006224:Cricetinae; D003412:Cricetulus; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D005285:Fermentation; D005658:Fungi / Q000737:chemistry*; D007527:Isoenzymes / Q000037:antagonists & inhibitors; D017737:Macrophages, Peritoneal / Q000187:drug effects / Q000201:enzymology; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D008826:Microbial Sensitivity Tests; D008861:Microsomes / Q000187:drug effects / Q000201:enzymology; D002785:Sterol O-Acyltransferase / Q000037:antagonists & inhibitors*
chemical_list: D000081:Acetamides; D000890:Anti-Infective Agents; D004791:Enzyme Inhibitors; D007527:Isoenzymes; C000604587:clonoamide; D002785:Sterol O-Acyltransferase