Faculdade de Farmácia/CEF, Universidade de Coimbra, Azinhaga de Santa Comba, 3030-548 Coimbra, Portugal.
Exp Parasitol. 2012 Mar;130(3):223-31. doi: 10.1016/j.exppara.2011.12.012. Epub 2012 Jan 2.
In order to contribute for the search of new drugs for leishmaniasis, we study the susceptibility of Leishmania infantum, Leishmania tropica and Leishmania major to Cymbopogon citratus essential oil and major compounds, mrycene and citral. C. citratus and citral were the most active inhibiting L. infantum, L. tropica and L. major growth at IC(50) concentrations ranging from 25 to 52 μg/ml and from 34 to 42 μg/ml, respectively. L. infantum promastigotes exposed to essential oil and citral underwent considerable ultrastructural alterations, namely mitochondrial and kinetoplast swelling, autophagosomal structures, disruption of nuclear membrane and nuclear chromatin condensation. C. citratus essential oil and citral promoted the leishmanicidal effect by triggering a programmed cell death. In fact, the leishmanicidal activity was mediated via apoptosis as evidenced by externalization of phosphatidylserine, loss of mitochondrial membrane potential, and cell-cycle arrest at the G(0)/G(1) phase. Taken together, ours findings lead us to propose that citral was responsible for anti-Leishmania activity of the C. citratus and both may represent a valuable source for therapeutic control of leishmaniasis.
为了寻找治疗利什曼病的新药，我们研究了香茅精油及其主要成分月桂烯和柠檬醛对婴儿利什曼原虫、热带利什曼原虫和利什曼原虫的敏感性。香茅精油和柠檬醛对 L. infantum、L. tropica 和 L. major 的生长抑制作用最强，IC50 浓度分别为 25 至 52μg/ml 和 34 至 42μg/ml。暴露于精油和柠檬醛的 L. infantum 前鞭毛体经历了相当大的超微结构改变，即线粒体和动基体肿胀、自噬体结构、核膜破裂和核染色质浓缩。香茅精油和柠檬醛通过触发程序性细胞死亡来促进杀利什曼原虫作用。事实上，杀利什曼原虫活性是通过凋亡介导的，这可以通过磷脂酰丝氨酸的外化、线粒体膜电位的丧失以及细胞周期在 G0/G1 期的停滞来证明。综上所述，我们的研究结果表明柠檬醛是香茅抗利什曼原虫活性的原因，两者都可能是治疗利什曼病的有价值的来源。
