Antiplasmodial activity of targeted zinc(II)-dipicolylamine complexes

作者：Rice Douglas R; Mendiola Maria de Lourdes Betancourt; Murillo Solano Claribel; Checkley Lisa A; Ferdig Michael T; Pizarro Juan C; Smith Bradley D^*

来源：Bioorganic & Medicinal Chemistry, 2017, 25(10): 2754-2760.

DOI：10.1016/j.bmc.2017.03.050

• Malaria
• Antiplasmodial drugs
• Zinc dipicolylamine
• Fluorescence microscopy

This study measured the antiplasmodial activity of nine zinc-dipicolylamine (ZnDPA) complexes against three strains of Plasmodium falciparum, the causative parasite of malaria. Growth inhibition assays showed significant activity against all tested strains, with 50% inhibitory concentrations between 5 and 600 nM and almost no toxic effect against host cells including healthy red blood cells. Fluorescence microscopy studies with a green-fluorescent ZnDPA probe showed selective targeting of infected red blood cells. The results suggest that ZnDPA coordination complexes are promising antiplasmodial agents with potential for targeted malaria treatment.

• 出版日期2017-5-15