Evaluation of Europium and Terbium compounds as potential antimalarial drugs
摘要
The emergence of drug-resistant Plasmodium falciparum parasites warrants a need for the development of new antimalarial agents. In this study, four structurally related Europium and Terbium compounds, bis(2,2′-bipyridine)bis(hexafluoroacetylacetone)europium (III) hexafluorophosphate (EC2), bis(2,2′-bipyridine)bis(2,4-pentanedione)europium(III) hexafluorophosphate (EC3), bis(1,10-phenanthroline)bis(2,4-pentanedione)europium(III) hexafluorophosphate (EC4)) and bis(2,2′-bipyridine)bis(hexafluoroacetylacetone) Terbium (III) hexafluorophosphate (TC1)) were screened for the growth inhibitory activity of in vitro cultured P. falciparum through two complementary methods. Microscopy of Giemsa-stained blood smear for the preliminary analysis of the growth inhibitory effect of the compounds followed by fluorescence activated cell sorting (FACS) of SYBR green intercalated parasites to assess dose-dependent growth inhibition with higher sensitivity. Among the four candidates, one of the Europium based compounds, EC4 demonstrated markedly superior potency, achieving 50% inhibition or IC₅₀ at 0.98 ± 0.12 µM, a substantially lower concentrations compared to the other three compounds. These findings highlight Europium based compounds could be a novel class of promising candidates for the development of antimalarials.