Antiprotozoal activity of ferroquine.

Abstract

Ferroquine (FQ, SSR97193) is a synthetic compound currently in development for the treatment of malaria. The use of a single compound to treat several parasitoses would be very convenient for multi-infected patients and also for financial considerations. In this work, the activity of FQ was investigated on three other Protista parasites: Kinetoplastidae (Leishmania and Trypanosoma) and the cosmopolite parasite Trichomonas vaginalis. FQ exhibited a significant in vitro activity on Trypanosoma brucei brucei and Trypanosoma brucei gambiense, the agents of African trypanosomiasis in a range from 0.2 to 3.1 μM. In vivo, intraperitoneally administered FQ demonstrated a weak but significant trypanocidal activity at 100 μmol/kg, which is however higher than the maximum tolerated dose. The drop of the parasitemia of the treated mice was significantly related to the amount of injected FQ. Furthermore, this organometallic compound was responsible for a delay in the appearance of bloodstream parasites at 50 μmol/kg. However, it was not able to cure infected mice. Although no synergy was identified in vitro between FQ and pentamidine, these results justify further investigations by evaluating analogues in this chemical series.

• Authors: S Pomel, C Biot, C Bories, P M Loiseau
• Journal: Parasitology research (Parasitol Res) Vol. 112 Issue 2 Pg. 665-9 (Feb 2013) ISSN: 1432-1955 [Electronic] Germany
• PMID: 23229318 (Publication Type: Journal Article)

Chemical References

• Aminoquinolines
• Antiprotozoal Agents
• Ferrous Compounds
• Metallocenes
• ferroquine

Topics

• Aminoquinolines (administration & dosage, pharmacology)
• Animals
• Antiprotozoal Agents (administration & dosage, pharmacology)
• Ferrous Compounds (administration & dosage, pharmacology)
• Leishmania (drug effects)
• Metallocenes
• Mice
• Parasitic Sensitivity Tests
• Treatment Outcome
• Trichomonas vaginalis (drug effects)
• Trypanosoma (drug effects)
• Trypanosomiasis, African (drug therapy)