Snapshot Profiling of the Antileishmanial Potency of Lead Compounds and Drug Candidates against Intracellular Leishmania donovani Amastigotes, with a Focus on Human-Derived Host Cells
Copyright policy )Snapshot Profiling of the Antileishmanial Potency of Lead Compounds and Drug Candidates against Intracellular Leishmania donovani Amastigotes, with a Focus on Human-Derived Host Cells
ABSTRACT This study characterized the in vitro potencies of antileishmanial agents against intracellular Leishmania donovani amastigotes in primary human macrophages, obtained with or without CD14-positive monocyte enrichment, phorbol 12-myristate 13-acetate (PMA)-differentiated THP-1 cells, and mouse peritoneal exudate macrophages (PEMs). Host cell-dependent potency was confirmed for pentavalent and trivalent antimony. Fexinidazole was inactive against intracellular amastigotes across the host cell panel. Fexinidazole sulfone, ( R )-PA-824, ( S )-PA-824, and VL-2098 displayed similar potency in all of the host cells tested.
- London School of Hygiene & Tropical Medicine United Kingdom
- University of Dundee United Kingdom
- University of London United Kingdom
- Faculty of Infectious and Tropical Diseases London School of Hygiene and Tropical Medicine United Kingdom
Antimony, Mice, Knockout, host cell, Macrophages, Primary Cell Culture, Antiprotozoal Agents, 610, Cell Differentiation, Stereoisomerism, 540, Monocytes, Cell Line, Inhibitory Concentration 50, Mice, Nitroimidazoles, Host-Pathogen Interactions, Animals, Humans, Tetradecanoylphorbol Acetate, drug potency, Leishmania donovani
Antimony, Mice, Knockout, host cell, Macrophages, Primary Cell Culture, Antiprotozoal Agents, 610, Cell Differentiation, Stereoisomerism, 540, Monocytes, Cell Line, Inhibitory Concentration 50, Mice, Nitroimidazoles, Host-Pathogen Interactions, Animals, Humans, Tetradecanoylphorbol Acetate, drug potency, Leishmania donovani
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