Anthracene-polyamine conjugates inhibit in vitro proliferation of intraerythrocytic Plasmodium falciparum parasites

Antimicrob Agents Chemother. 2013 Jun;57(6):2874-7. doi: 10.1128/AAC.00106-13. Epub 2013 Apr 1.

Abstract

Anthracene-polyamine conjugates inhibit the in vitro proliferation of the intraerythrocytic human malaria parasite Plasmodium falciparum, with 50% inhibitory concentrations (IC50s) in the nM to μM range. The compounds are taken up into the intraerythrocytic parasite, where they arrest the parasite cell cycle. Both the anthracene and polyamine components of the conjugates play a role in their antiplasmodial effect.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anthracenes / chemistry
  • Anthracenes / pharmacology*
  • Antimalarials / chemistry
  • Antimalarials / metabolism
  • Antimalarials / pharmacology*
  • CHO Cells
  • Cell Line, Tumor
  • Cricetulus
  • Erythrocytes / parasitology
  • Humans
  • Inhibitory Concentration 50
  • Malaria, Falciparum / parasitology
  • Parasitic Sensitivity Tests / methods
  • Plasmodium falciparum / drug effects*
  • Plasmodium falciparum / growth & development
  • Plasmodium falciparum / metabolism
  • Polyamines / chemistry
  • Polyamines / metabolism
  • Polyamines / pharmacology*

Substances

  • Anthracenes
  • Antimalarials
  • Polyamines
  • anthracene