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 hav...

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Veröffentlicht in:	Journal of antibiotics 2008-10, Vol.61 (10), p.627-632
Hauptverfasser:	Ishiyama, Aki, Otoguro, Kazuhiko, Namatame, Miyuki, Nishihara, Aki, Furusawa, Toshiaki, Masuma, Rokuro, Shiomi, Kazuro, Takahashi, Yoko, Ichimura, Michio, Yamada, Haruki, Ōmura, Satoshi
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antibiotics Bacteriology Biomedical and Life Sciences Bioorganic Chemistry Cell Line Dipeptides - chemistry Dipeptides - pharmacology Dipeptides - toxicity Drug Discovery Female Humans In Vitro Techniques Life Sciences Medicinal Chemistry Metabolites Methylglucosides - chemistry Methylglucosides - pharmacology Methylglucosides - toxicity Mice Mice, Inbred ICR Microbiology Microorganisms Molecular Structure Organic Chemistry original-article Parasitic Sensitivity Tests Soil Microbiology Soil microorganisms Terpenes - chemistry Terpenes - pharmacology Terpenes - toxicity Trypanocidal Agents - chemistry Trypanocidal Agents - pharmacology Trypanocidal Agents - toxicity Trypanosoma brucei brucei - drug effects Trypanosoma brucei rhodesiense - drug effects Trypanosomiasis, African - drug therapy
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Zusammenfassung:	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.
ISSN:	0021-8820 1881-1469
DOI:	10.1038/ja.2008.83