In vitro and in vivo antitrypanosomal activitiy of two microbial metabolites, KS-505a and alazopeptin.
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.
Ishiyama
Aki
A
Research Center for Tropical Diseases, Center for Basic Research, Kitasato University, Tokyo, Japan.
Otoguro
Kazuhiko
K
Namatame
Miyuki
M
Nishihara
Aki
A
Furusawa
Toshiaki
T
Masuma
Rokuro
R
Shiomi
Kazuro
K
Takahashi
Yoko
Y
Ichimura
Michio
M
Yamada
Haruki
H
Omura
Satoshi
S
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*
D004151:Dipeptides; D008757:Methylglucosides; D013729:Terpenes; D014344:Trypanocidal Agents; C074362:longestin; C006439:allyl-(6-diazo-5-oxo)-norleucyl-(6-diazo-5-oxo)-norleucine