Antiprotozoal activity of ferroquine
Document type :
Article dans une revue scientifique
PMID :
Permalink :
Title :
Antiprotozoal activity of ferroquine
Author(s) :
Pomel, S. [Auteur]
Biomolécules : Conception, Isolement, Synthèse [BioCIS]
Biot, Christophe [Auteur]
Unité de Glycobiologie Structurale et Fonctionnelle (UGSF) - UMR 8576
Unité de Glycobiologie Structurale et Fonctionnelle - UMR 8576 [UGSF]
Bories, C [Auteur]
Biomolécules : Conception, Isolement, Synthèse [BioCIS]
Loiseau, P.M. [Auteur]
Biomolécules : Conception, Isolement, Synthèse [BioCIS]
Biomolécules : Conception, Isolement, Synthèse [BioCIS]
Biot, Christophe [Auteur]

Unité de Glycobiologie Structurale et Fonctionnelle (UGSF) - UMR 8576
Unité de Glycobiologie Structurale et Fonctionnelle - UMR 8576 [UGSF]
Bories, C [Auteur]
Biomolécules : Conception, Isolement, Synthèse [BioCIS]
Loiseau, P.M. [Auteur]
Biomolécules : Conception, Isolement, Synthèse [BioCIS]
Journal title :
Parasitology research
Abbreviated title :
Parasitol. Res.
Volume number :
112
Pages :
665-669
Publication date :
2013-02
ISSN :
1432-1955
HAL domain(s) :
Chimie/Chimie théorique et/ou physique
English abstract : [en]
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 ...
Show more >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.Show less >
Show more >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.Show less >
Language :
Anglais
Audience :
Non spécifiée
Administrative institution(s) :
CNRS
Université de Lille
Université de Lille
Research team(s) :
Chemical Glycobiology
Submission date :
2020-02-12T15:11:06Z
2021-05-07T06:50:37Z
2021-05-07T06:50:37Z