Antitrypanosomal cyclic polyketide peroxides from the Australian marine sponge Plakortis sp

J Nat Prod. 2010 Apr 23;73(4):716-9. doi: 10.1021/np900535z.

Abstract

Bioassay-guided fractionation of the crude extract from the Australian marine sponge Plakortis sp. led to the isolation of two new cyclic polyketide peroxides, 11,12-didehydro-13-oxo-plakortide Q (1) and 10-carboxy-11,12,13,14-tetranor-plakortide Q (2). Antitrypanosomal studies showed that compound 1 had an IC(50) value of 49 nM against Trypanosoma brucei brucei, and compound 2, where a carboxylic acid is present in the side chain, had a 20-fold reduction of activity. 11,12-Didehydro-13-oxo-plakortide Q (1) is the most active peroxide isolated so far against T. b. brucei, and it indicates the potential therapeutic value of this class of compounds.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Australia
  • Dioxanes / chemistry
  • Dioxanes / isolation & purification*
  • Dioxanes / pharmacology*
  • Humans
  • Marine Biology
  • Molecular Structure
  • Plakortis / chemistry*
  • Trypanocidal Agents / chemistry
  • Trypanocidal Agents / isolation & purification*
  • Trypanocidal Agents / pharmacology*
  • Trypanosoma brucei brucei / drug effects*

Substances

  • 10-carboxy-11,12,13,14-tetranor-plakortide Q
  • 11,12-didehydro-13-oxo-plakortide Q
  • Dioxanes
  • Trypanocidal Agents