부산대학교 도서관

ABSTRACTFerroquine (FQ; SSR97193), a ferrocene-containing 4-aminoquinoline derivate, has potent in vitroefficacy against chloroquine (CQ)-resistant Plasmodium falciparumand CQ-sensitive P. vivax. In the current study, ex vivoFQ activity was tested in multidrug-resistant P. falciparumand P. vivaxfield isolates using a schizont maturation assay. Although FQ showed excellent activity against CQ-sensitive and -resistant P. falciparumand P. vivax(median 50% inhibitory concentrations [IC50s], 9.6 nM and 18.8 nM, respectively), there was significant cross-susceptibility with the quinoline-based drugs chloroquine, amodiaquine, and piperaquine (for P. falciparum, r= 0.546 to 0.700, P< 0.001; for P. vivax, r= 0.677 to 0.821, P< 0.001). The observed ex vivocross-susceptibility is likely to reflect similar mechanisms of drug uptake/efflux and modes of drug action of this drug class. However, the potent activity of FQ against resistant isolates of both P. falciparumand P. vivaxhighlights a promising role for FQ as a lead antimalarial against CQ-resistant Plasmodiumand a useful partner drug for artemisinin-based combination therapy.