Selective and potent in vitro antitrypanosomal activities of ten microbial metabolites

J Antibiot (Tokyo). 2008 Jun;61(6):372-8. doi: 10.1038/ja.2008.52.

Abstract

More than 400 compounds isolated from soil microorganisms, and catalogued in the antibiotic library of the Kitasato Institute for Life Sciences, were screened against African trypanosomes. Ten compounds were found to have selective and potent antitrypanosomal activity in vitro: aureothin, cellocidin, destomycin A, echinomycin, hedamycin, irumamycin, LL-Z 1272beta, O-methylnanaomycin A, venturicidin A and virustomycin A. Results of the in vitro assays using the GUTat 3.1 strain of Trypanosomal brucei brucei and the STIB900 strain of T. b. rhodesiense are presented. Cytotoxicity was determined using a human MRC-5 cell line. This is the first report of antitrypanosomal activities of the 10 microbial metabolites listed above.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkynes / chemistry
  • Alkynes / isolation & purification
  • Alkynes / metabolism
  • Alkynes / pharmacology
  • Animals
  • Anthraquinones / chemistry
  • Anthraquinones / isolation & purification
  • Anthraquinones / metabolism
  • Anthraquinones / pharmacology
  • Cell Line
  • Chromones / chemistry
  • Chromones / isolation & purification
  • Chromones / metabolism
  • Chromones / pharmacology
  • Echinomycin / chemistry
  • Echinomycin / isolation & purification
  • Echinomycin / metabolism
  • Echinomycin / pharmacology
  • Hygromycin B / analogs & derivatives
  • Hygromycin B / chemistry
  • Hygromycin B / isolation & purification
  • Hygromycin B / metabolism
  • Hygromycin B / pharmacology
  • Macrolides / chemistry
  • Macrolides / isolation & purification
  • Macrolides / metabolism
  • Macrolides / pharmacology
  • Naphthoquinones / chemistry
  • Naphthoquinones / isolation & purification
  • Naphthoquinones / metabolism
  • Naphthoquinones / pharmacology
  • Soil Microbiology
  • Trypanocidal Agents / chemistry
  • Trypanocidal Agents / isolation & purification*
  • Trypanocidal Agents / metabolism
  • Trypanocidal Agents / pharmacology*
  • Trypanosoma brucei brucei / drug effects*
  • Venturicidins / chemistry
  • Venturicidins / isolation & purification
  • Venturicidins / metabolism
  • Venturicidins / pharmacology

Substances

  • Alkynes
  • Anthraquinones
  • Chromones
  • Macrolides
  • Naphthoquinones
  • Trypanocidal Agents
  • Venturicidins
  • hedamycin
  • cellocidin
  • venturicidin A
  • Hygromycin B
  • Echinomycin
  • nanaomycin A
  • irumamycin
  • virustomycin A
  • aureothin
  • destomycin A