title: Anti-Candida metabolites from endophytic fungi.
abstract: Submerged cultures of some 1500 Ascomycota and Basidiomycota isolated from their fruit-bodies or as soil-borne, coprophilous or endophytic fungi were screened for activity against Candida albicans and a range of other pathogenic and saprotrophic fungi. Considerably more Ascomycota (11-16%) than Basidiomycota (3.5%) produced metabolites with activity against C. albicans. From five species of endophytes, six bioactive compounds were isolated and identified, viz. cerulenin (1), arundifungin (2), sphaeropsidin A (3), 5-(1,3-butadiene-1-yl)-3-(propene-1-yl)-2-(5H)-furanone (4), ascosteroside A (formerly called ascosteroside; 5) and a derivative of 5, ascosteroside B (6). 1, 3 and 5 were isolated from fungi belonging to different orders than previously described producers. Antifungal activities of 2 and 4-6 in the agar diffusion test were comparable with those of amphotericin B. Compound 6 exhibited a similar antifungal activity as 5 but its cytotoxicity towards Hep G2 cells was considerably lower. This study points to endophytic fungi related to hemibiotrophic or latent plant pathogens as an important source of bio- and chemodiversity.
authors.affiliation: Department of Biotechnology, University of Kaiserslautern, Erwin-Schrödinger-Strasse 56, D-67663 Kaiserslautern, Germany.
authors.forename: Roland W S
authors.initials: RW
authors.lastname: Weber
authors.forename: Reinhard
authors.initials: R
authors.lastname: Kappe
authors.forename: Thomas
authors.initials: T
authors.lastname: Paululat
authors.forename: Eva
authors.initials: E
authors.lastname: Mösker
authors.forename: Heidrun
authors.initials: H
authors.lastname: Anke
mesh_terms: D000935:Antifungal Agents / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D002176:Candida albicans / Q000187:drug effects*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D002569:Cerulenin / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D004224:Diterpenes / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D005658:Fungi / Q000737:chemistry / Q000378:metabolism*; D006027:Glycosides / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D006367:HeLa Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D014315:Triterpenes / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology
chemical_list: D000935:Antifungal Agents; D004224:Diterpenes; D006027:Glycosides; D014315:Triterpenes; C458839:arundifungin; C100703:ascosteroside; D002569:Cerulenin