Antiplasmodial activity of targeted zinc(II)-dipicolylamine complexes

  • Bioorg Med Chem. 2017 May 15;25(10):2754-2760. doi: 10.1016/j.bmc.2017.03.050.
Douglas R Rice  1 ,  María de Lourdes Betancourt Mendiola  1 ,  Claribel Murillo-Solano  2 ,  Lisa A Checkley  3 ,  Michael T Ferdig  3 ,  Juan C Pizarro  2 ,  Bradley D Smith  4
Affiliations
  • 1. Department of Chemistry and Biochemistry, 236 Nieuwland Science Hall, University of Notre Dame, Notre Dame, IN 46556, USA.
  • 2. Department of Tropical Medicine, J Bennett Johnston Building, 1430 Tulane Avenue, Tulane University, New Orleans, LA 70112, USA.
  • 3. Department of Biological Science, Galvin Life Sciences, University of Notre Dame, Notre Dame, IN 46556, USA.
  • 4. Department of Chemistry and Biochemistry, 236 Nieuwland Science Hall, University of Notre Dame, Notre Dame, IN 46556, USA. Electronic address: [email protected].
PMID: 28377170 DOI: 10.1016/j.bmc.2017.03.050
Abstract

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 600nM 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.

Keywords
Antiplasmodial drugs; Fluorescence microscopy; Malaria; Zinc dipicolylamine.
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