title: In vitro and in vivo antitrypanosomal activitiy of two microbial metabolites, KS-505a and alazopeptin.
abstract: Our on-going screening program to discover new antitrypanosomal antibiotics has been evaluating compounds isolated from soil microorganisms as well as investigating the antibiotic libraries of the Kitasato Institute for Life Sciences and BioFrontier Laboratories of Kyowa Hakko Kogyo Co., Ltd. We have now discovered two compounds, KS-505a and alazopeptin, which exhibit moderate antitrypanosomal characteristics. We report here the in vitro and in vivo antitrypanosomal activities and cytotoxicities of KS-505a and alazopeptin, compared with some commonly-used antitrypanosomal drugs. This is the first report of in vitro and in vivo antitrypanosomal activities of either KS-505a or alazopeptin.
authors.affiliation: Research Center for Tropical Diseases, Center for Basic Research, Kitasato University, Tokyo, Japan.
authors.forename: Aki
authors.initials: A
authors.lastname: Ishiyama
authors.forename: Kazuhiko
authors.initials: K
authors.lastname: Otoguro
authors.forename: Miyuki
authors.initials: M
authors.lastname: Namatame
authors.forename: Aki
authors.initials: A
authors.lastname: Nishihara
authors.forename: Toshiaki
authors.initials: T
authors.lastname: Furusawa
authors.forename: Rokuro
authors.initials: R
authors.lastname: Masuma
authors.forename: Kazuro
authors.initials: K
authors.lastname: Shiomi
authors.forename: Yoko
authors.initials: Y
authors.lastname: Takahashi
authors.forename: Michio
authors.initials: M
authors.lastname: Ichimura
authors.forename: Haruki
authors.initials: H
authors.lastname: Yamada
authors.forename: Satoshi
authors.initials: S
authors.lastname: Omura
mesh_terms: D000818:Animals; D002460:Cell Line; D004151:Dipeptides / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity; D055808:Drug Discovery; D005260:Female; D006801:Humans; D066298:In Vitro Techniques; D008757:Methylglucosides / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity; D051379:Mice; D008813:Mice, Inbred ICR; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests; D012988:Soil Microbiology; D013729:Terpenes / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity; D014344:Trypanocidal Agents / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity; D014346:Trypanosoma brucei brucei / Q000187:drug effects*; D016833:Trypanosoma brucei rhodesiense / Q000187:drug effects; D014353:Trypanosomiasis, African / Q000188:drug therapy*
chemical_list: D004151:Dipeptides; D008757:Methylglucosides; D013729:Terpenes; D014344:Trypanocidal Agents; C074362:longestin; C006439:allyl-(6-diazo-5-oxo)-norleucyl-(6-diazo-5-oxo)-norleucine