先导化合物和候选药物对细胞内杜氏利什曼原虫无鞭毛体的抗利什曼活性的快照分析，重点关注人源宿主细胞。
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.
作者信息
Koniordou Markela, Patterson Stephen, Wyllie Susan, Seifert Karin
机构信息
Faculty of Infectious and Tropical Diseases, London School of Hygiene and Tropical Medicine, London, United Kingdom.
School of Life Sciences, University of Dundee, Dundee, United Kingdom.
出版信息
Antimicrob Agents Chemother. 2017 Feb 23;61(3). doi: 10.1128/AAC.01228-16. Print 2017 Mar.
Abstract
This study characterized the potencies of antileishmanial agents against intracellular 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, ()-PA-824, ()-PA-824, and VL-2098 displayed similar potency in all of the host cells tested.
摘要
本研究表征了抗利什曼原虫药物对原代人巨噬细胞内无鞭毛体的效力，这些原代人巨噬细胞通过有无CD14阳性单核细胞富集获得，佛波醇12-肉豆蔻酸酯13-乙酸酯（PMA）分化的THP-1细胞，以及小鼠腹腔渗出巨噬细胞（PEMs）。证实了五价和三价锑的宿主细胞依赖性效力。非昔硝唑对整个宿主细胞组中的细胞内无鞭毛体无活性。非昔硝唑砜、()-PA-824、()-PA-824和VL-2098在所有测试的宿主细胞中显示出相似的效力。
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