title: In Vitro Antitrypanosomal Activity of the Secondary Metabolites from the Mutant Strain IU-3 of the Insect Pathogenic Fungus Ophiocordyceps coccidiicola NBRC 100683.
abstract: During the search for new antitrypanosomal drug leads, four antitrypanosomal compounds, of three depsipeptides and one nortriterpenoid, were isolated from cultures of the mutant strain IU-3 of the insect pathogenic fungus Ophiocordyceps coccidiicola NBRC 100683. Their structures were identified by the analysis of high resolution-electron ionization (HR-EI)-MS and HR-FAB-MS, and (1)H- and (13)C-NMR spectra, including extensive two dimensional (2D)-heteronuclear NMR experiments, and comparison with literature data for destruxin A (1), destruxin B (2), destruxin E chlorohydrin (3) and helvolic acid (4). Compounds 1-4 showed in vitro antitrypanosomal activity against Trypanosoma brucei brucei GUTat3.1 with IC50 values of 0.33, 0.16, 0.061 and 5.08 µg/mL, respectively.
authors.affiliation: Faculty of Pharmaceutical Sciences, Tokushima Bunri University.
authors.forename: Momoko
authors.initials: M
authors.lastname: Ganaha
authors.forename: Kento
authors.initials: K
authors.lastname: Yoshii
authors.forename: Yuuta
authors.initials: Y
authors.lastname: Ōtsuki
authors.forename: Miki
authors.initials: M
authors.lastname: Iguchi
authors.forename: Yasuko
authors.initials: Y
authors.lastname: Okamoto
authors.forename: Kanako
authors.initials: K
authors.lastname: Iseki
authors.forename: Sayaka
authors.initials: S
authors.lastname: Ban
authors.forename: Aki
authors.initials: A
authors.lastname: Ishiyama
authors.forename: Rei
authors.initials: R
authors.lastname: Hokari
authors.forename: Masato
authors.initials: M
authors.lastname: Iwatsuki
authors.forename: Kazuhiko
authors.initials: K
authors.lastname: Otoguro
authors.forename: Satoshi
authors.initials: S
authors.lastname: Ōmura
authors.forename: Toshihiro
authors.initials: T
authors.lastname: Hashimoto
authors.forename: Masaaki
authors.initials: M
authors.lastname: Noji
authors.forename: Akemi
authors.initials: A
authors.lastname: Umeyama
mesh_terms: D000981:Antiprotozoal Agents / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D001203:Ascomycota / Q000737:chemistry* / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D008968:Molecular Conformation; D021261:Parasitic Sensitivity Tests; D013329:Structure-Activity Relationship; D014346:Trypanosoma brucei brucei / Q000187:drug effects*
chemical_list: D000981:Antiprotozoal Agents