title: Haplofungins, novel inositol phosphorylceramide synthase inhibitors, from Lauriomyces bellulus SANK 26899 I. Taxonomy, fermentation, isolation and biological activities.
abstract: In the course of screening for antifungal agents, we have discovered eight novel compounds, haplofungin A, B, C, D, E, F, G and H, from a culture broth of the fungus strain Lauriomyces bellulus SANK 26899. Haplofungins are composed of an arabinonic acid moiety linked through an ester to a modified long alkyl chain and show potent inhibitory activities against fungal inositol phosphorylceramide (IPC) synthase. Haplofungin A inhibited the activity of IPC synthase from Saccharomyces cerevisiae with an IC(50) value of 0.0015 microg ml(-1). This inhibitor also suppressed the growth of Candida glabrata at the MIC value of 0.5 microg ml(-1).
authors: Exploratory Research Laboratories I, Daiichi Sankyo Co. Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo, Japan. ohnuki.takashi.eh@daiichisankyo.co.jp
authors: Takashi
authors: T
authors: Ohnuki
authors: Tatsuya
authors: T
authors: Yano
authors: Yasunori
authors: Y
authors: Ono
authors: Shiho
authors: S
authors: Kozuma
authors: Toshihiro
authors: T
authors: Suzuki
authors: Yasumasa
authors: Y
authors: Ogawa
authors: Toshio
authors: T
authors: Takatsu
mesh_terms: D000935:Antifungal Agents / Q000737:chemistry / Q000302:isolation & purification / Q000378:metabolism / Q000494:pharmacology*; D001203:Ascomycota / Q000145:classification / Q000254:growth & development / Q000302:isolation & purification / Q000378:metabolism*; D041221:Candida glabrata / Q000187:drug effects / Q000201:enzymology; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D005231:Fatty Acids, Unsaturated / Q000737:chemistry / Q000302:isolation & purification / Q000378:metabolism / Q000494:pharmacology*; D005285:Fermentation; D006602:Hexosyltransferases / Q000037:antagonists & inhibitors*; D006801:Humans; D008826:Microbial Sensitivity Tests; D012441:Saccharomyces cerevisiae / Q000187:drug effects / Q000201:enzymology; D012988:Soil Microbiology; D013329:Structure-Activity Relationship
chemical_list: D000935:Antifungal Agents; D004791:Enzyme Inhibitors; D005231:Fatty Acids, Unsaturated; D006602:Hexosyltransferases; C088714:phosphatidylinositol-ceramide phosphoinositol transferase