Antiprotozoal activity of ferroquine
Type de document :
Article dans une revue scientifique
PMID :
URL permanente :
Titre :
Antiprotozoal activity of ferroquine
Auteur(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]
Titre de la revue :
Parasitology research
Nom court de la revue :
Parasitol. Res.
Numéro :
112
Pagination :
665-669
Date de publication :
2013-02
ISSN :
1432-1955
Discipline(s) HAL :
Chimie/Chimie théorique et/ou physique
Résumé en anglais : [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 ...
Lire la suite >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.Lire moins >
Lire la suite >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.Lire moins >
Langue :
Anglais
Audience :
Non spécifiée
Établissement(s) :
CNRS
Université de Lille
Université de Lille
Équipe(s) de recherche :
Chemical Glycobiology
Date de dépôt :
2020-02-12T15:11:06Z
2021-05-07T06:50:37Z
2021-05-07T06:50:37Z