Iron chelators: in vitro inhibitory effect on the liver stage of rodent and human malaria

Am J Trop Med Hyg. 1988 Sep;39(3):236-40. doi: 10.4269/ajtmh.1988.39.236.

Abstract

The activity of desferrioxamine (Desferal) and desferrithiocin (a newly developed oral iron chelator) was evaluated against the liver stage of Plasmodium yoelii and P. falciparum in the rodent and the human hepatocyte in vitro culture system. The two iron chelators were found to inhibit the liver schizogony of both the rodent and the human Plasmodium species at concentrations achievable in vivo. P. falciparum proved to be more sensitive (ic 95% below 20 micromol/l than P. yoelii (ic 95% 50-100 micromol/l). As assessed by electron microscopy, drug administration was associated with focal clarification of the cytoplasm thought to be reversible. As desferrioxamine and desferrithiocin are known to be equally active on the blood stage of rodent and human plasmodia, iron chelators are deserving of further investigation as potential alternative candidates to existing drugs for radical cure of malaria.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Animals
  • Cells, Cultured
  • Deferoxamine / pharmacology*
  • Deferoxamine / therapeutic use
  • Deferoxamine / toxicity
  • Dihydropyridines / pharmacology*
  • Dihydropyridines / therapeutic use
  • Dihydropyridines / toxicity
  • Humans
  • Iron Chelating Agents / pharmacology*
  • Iron Chelating Agents / therapeutic use
  • Iron Chelating Agents / toxicity
  • Liver / drug effects
  • Liver / parasitology
  • Liver / ultrastructure
  • Malaria / drug therapy
  • Microscopy, Electron
  • Plasmodium falciparum / drug effects*
  • Plasmodium falciparum / growth & development
  • Plasmodium yoelii / drug effects*
  • Plasmodium yoelii / growth & development
  • Rats
  • Thiazoles / pharmacology*
  • Thiazoles / therapeutic use
  • Thiazoles / toxicity

Substances

  • Dihydropyridines
  • Iron Chelating Agents
  • Thiazoles
  • Deferoxamine
  • desferrithiocin