六氮杂三萘对利什曼原虫属的体外活性
In vitro activities of hexaazatrinaphthylenes against Leishmania spp.
作者信息
López-Arencibia Atteneri, García-Velázquez Daniel, Martín-Navarro Carmen M, Sifaoui Ines, Reyes-Batlle María, Lorenzo-Morales Jacob, Gutiérrez-Ravelo Ángel, Piñero José E
机构信息
University Institute of Tropical Diseases and Public Health of the Canary Islands, University of La Laguna, Tenerife, Canary Islands, Spain
Instituto Universitario de Bio-Orgánica Antonio González, Departamento de Química Orgánica, Universidad de La Laguna, Tenerife, Spain.
出版信息
Antimicrob Agents Chemother. 2015 May;59(5):2867-74. doi: 10.1128/AAC.00226-15. Epub 2015 Mar 9.
The in vitro activity of a novel group of compounds, hexaazatrinaphthylene derivatives, against two species of Leishmania is described in this study. These compounds showed a significant dose-dependent inhibition effect on the proliferation of the parasites, with 50% inhibitory concentrations (IC(50)s) ranging from 1.23 to 25.05 μM against the promastigote stage and 0.5 to 0.7 μM against intracellular amastigotes. Also, a cytotoxicity assay was carried out to in order to evaluate the possible toxic effects of these compounds. Moreover, different assays were performed to determine the type of cell death induced after incubation with these compounds. The obtained results highlight the potential use of hexaazatrinaphthylene derivatives against Leishmania species, and further studies should be undertaken to establish them as novel leishmanicidal therapeutic agents.
本研究描述了一组新型化合物——六氮杂三亚萘衍生物对两种利什曼原虫的体外活性。这些化合物对寄生虫的增殖表现出显著的剂量依赖性抑制作用，对前鞭毛体阶段的50%抑制浓度（IC50）范围为1.23至25.05 μM，对细胞内无鞭毛体的IC50为0.5至0.7 μM。此外，还进行了细胞毒性试验以评估这些化合物可能的毒性作用。而且，进行了不同的试验以确定与这些化合物孵育后诱导的细胞死亡类型。所得结果突出了六氮杂三亚萘衍生物对利什曼原虫的潜在应用价值，应进一步开展研究以将它们确立为新型抗利什曼原虫治疗药物。
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