BACKGROUND The in vitro activity against Leishmania spp. of a novel group of compounds, phenalenone derivatives, is described in this study. Previous studies have shown that some phenalenones present leishmanicidal activity, and induce a decrease in the mitochondrial membrane potential in L. amazonensis parasites, so in order to elucidate the evidence of programmed cell death occurring inside the promastigote stage, different assays were performed in two different species of Leishmania. METHODS We focused on the determination of the programmed cell death evidence by detecting the characteristic features of the apoptosis-like process, such as phosphatidylserine exposure, mitochondrial membrane potential, and chromatin condensation among others. RESULTS The results showed that four molecules activated the apoptosis-like process in the parasite. All the signals observed were indicative of the death process that the parasites were undergoing. CONCLUSIONS The present results highlight the potential use of phenalenone derivatives against Leishmania species and further studies should be undertaken to establish them as novel leishmanicidal therapeutic agents.

中文翻译：

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1H-苯酚-1-酮衍生物对利什曼原虫的体外活性。以及程序性细胞死亡的证据。

背景技术针对利什曼原虫的体外活性。这项研究描述了一组新的化合物，菲尔烯酮衍生物。先前的研究表明，某些非那农酮具有杀菌作用，并导致亚马逊线虫寄生虫的线粒体膜电位降低，因此，为了阐明在前鞭毛体阶段发生程序性细胞死亡的证据，在两种不同的方法中进行了不同的测定利什曼原虫的种类。方法我们着重于通过检测凋亡样过程的特征性特征来确定程序性细胞死亡证据，例如磷脂酰丝氨酸暴露，线粒体膜电位和染色质浓缩等。结果结果表明，四个分子激活了该寄生虫的凋亡样过程。观察到的所有信号均表明该寄生虫正在经历死亡过程。结论目前的结果强调了苯乙烯酮衍生物对利什曼原虫物种的潜在用途，应进行进一步的研究以将其确立为新型利什曼杀菌剂。