Koniordou, Markela; Patterson, Stephen; Wyllie, Susan; Seifert, Karin; (2017) 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. Antimicrobial agents and chemotherapy, 61 (3). e01228-e01216. ISSN 0066-4804 DOI: https://doi.org/10.1128/AAC.01228-16
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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.
Item Type | Article |
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Faculty and Department | Faculty of Infectious and Tropical Diseases > Department of Infection Biology > Dept of Immunology and Infection (-2019) |
Research Centre | Antimicrobial Resistance Centre (AMR) |
PubMed ID | 28069646 |
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