The ferroquine antimalarial conundrum: redox activation and reinvasion inhibition

Angew Chem Int Ed Engl. 2013 Jul 22;52(30):7690-3. doi: 10.1002/anie.201303690. Epub 2013 Jun 13.

Abstract

Metal health: Ferroquine is a ferrocene-based analogue of the antimalarial drug chloroquine. In addition to the primary mechanism of quinoline action, fluorescent probe studies in infected red blood cells show another mechanism is at work. It is based on the production of HO(·) in the acidic and oxidizing environment of the digestive vacuole of the malaria parasite and implies that, with ferroquine, reinvasion can be inhibited.

Keywords: bioorganometallic chemistry; ferroquine; malaria; reactive species; subcellular imaging.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aminoquinolines / therapeutic use*
  • Antimalarials / therapeutic use*
  • Erythrocytes / drug effects*
  • Erythrocytes / parasitology
  • Ferrous Compounds / therapeutic use*
  • Humans
  • Hydroxyl Radical / chemistry*
  • Malaria, Falciparum / drug therapy*
  • Malaria, Falciparum / parasitology
  • Metallocenes
  • Oxidation-Reduction
  • Plasmodium falciparum / pathogenicity*

Substances

  • Aminoquinolines
  • Antimalarials
  • Ferrous Compounds
  • Metallocenes
  • Hydroxyl Radical
  • ferroquine