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N-十二烷基-1,2-乙二胺的体外杀利什曼原虫活性。

In vitro leishmanicidal activity of N-dodecyl-1,2-ethanediamine.

机构信息

Instituto de Ciências Biomédicas, Universidade Federal de Uberlândia, Av. Pará 1720, Uberlândia, MG, Brazil.

出版信息

Biomed Pharmacother. 2012 Apr;66(3):180-6. doi: 10.1016/j.biopha.2011.10.005. Epub 2012 Jan 2.

Abstract

Polyamine biosynthesis and inhibition in parasites have been an attractive chemotherapeutic approach in the design of novel antiparasitic drugs. We study in this work the effect of N-dodecyl-1,2-ethylenediamine (NDDE) on the morphology and replication of Leishmania using macrophages cultured from the peritoneal exudate of mice infected in vitro with three species of Leishmania: Leishmania (Leishmania) amazonensis, Leishmania (Viannia) brasiliensis and Leishmania (Leishmania) chagasi. The results showed that NDDE inhibited Leishmania amastigotes multiplication into inflammatory peritoneal cells in concentrations which were not toxic to mammalian cells (0.5-1μg/mL). An intracellular disorganization of the promastigote forms was observed by transmission electron microscopy after 3 to 24h of treatment with 1μg/mL NDDE, suggesting that this compound affects the viability of the parasite by an autophagy pathway.

摘要

多胺生物合成和抑制在寄生虫中一直是设计新型抗寄生虫药物的有吸引力的化疗方法。我们在这项工作中研究了 N-十二烷基-1,2-乙二胺 (NDDE) 对用感染体外三种利什曼原虫的小鼠腹腔渗出液培养的巨噬细胞中的利什曼原虫形态和复制的影响:利什曼原虫(利什曼原虫)亚马逊、利什曼原虫(Viannia)巴西和利什曼原虫(利什曼原虫)chagasi。结果表明,NDDE 在对哺乳动物细胞无毒的浓度(0.5-1μg/mL)下抑制利什曼原虫无鞭毛体在炎症性腹腔细胞中的增殖。在用 1μg/mL NDDE 处理 3 至 24 小时后,通过透射电子显微镜观察到前鞭毛体形式的细胞内解聚,表明该化合物通过自噬途径影响寄生虫的活力。

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