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

Markella Koniordou, Stephen Patterson, Susan Wyllie, Karin Seifert (Lead / Corresponding author)

Research output: Contribution to journalArticle

9 Citations (Scopus)
132 Downloads (Pure)

Abstract

This study characterised in vitro potencies of anti-leishmanial 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 host cells tested.

Original languageEnglish
Article numbere01228
Pages (from-to)1-16
Number of pages16
JournalAntimicrobial Agents and Chemotherapy
Volume61
Issue number3
Early online date9 Jan 2017
DOIs
Publication statusPublished - Mar 2017

Keywords

  • drug potency
  • host cell
  • Leishmania donovani

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