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萘醌衍生物环氧-α-拉帕醌的杀利什曼原虫活性证据。

Evidences for leishmanicidal activity of the naphthoquinone derivative epoxy-α-lapachone.

作者信息

Souza-Silva Franklin, do Nascimento Samara Braga, Bourguignon Saulo Cabral, Pereira Bernardo Acácio Santini, Carneiro Paula Fernandes, da Silva Wellington Seguis, Alves Carlos Roberto, de Pinho Rosa Teixeira

机构信息

Fundação Oswaldo Cruz, Instituto Oswaldo Cruz, Laboratório de Biologia Molecular e Doenças Endêmicas, Av. Brasil, 4365, Maguinhos, CEP 21040-360, Rio de Janeiro, Brazil.

Instituto de Biologia, Pós-Graduação em Ciências e Biotecnologia, Universidade Federal Fluminense, Outeiro de São João Baptista s/n - Centro, Niterói, CEP 24020-150 Rio de Janeiro, Brazil.

出版信息

Exp Parasitol. 2014 Dec;147:81-4. doi: 10.1016/j.exppara.2014.10.002. Epub 2014 Oct 13.

DOI:10.1016/j.exppara.2014.10.002
PMID:25307687
Abstract

In this work, we analyze the leishmanicidal effects of epoxy-α-lapachone on Leishmania (Viannia) braziliensis and Leishmania (Leishmania) amazonensis. Promasigotes and amastigotes (inhabiting human macrophages) from both species were assayed to verify the compound's activity over the distinct morphological stages. The incubation with epoxy-α-lapachone led to a significant decrease in the numbers of promastigotes from both species in the cultures, in a dose-and time-dependent fashion. The survival of amastigotes inhabiting human macrophages was also drastically affected by the compound, as shown by the variations in the endocytic index. Our results indicate that the epoxy-α-lapachone has an antiparasitic effect over Leishmania in both morphological stages and may potentially affect a range of species in two distinct subgenera of this parasite.

摘要

在本研究中,我们分析了环氧-α-拉帕醌对巴西利什曼原虫(维阿尼亚种)和亚马逊利什曼原虫(利什曼原虫属)的杀利什曼原虫作用。对这两个物种的前鞭毛体和无鞭毛体(寄生于人类巨噬细胞中)进行了检测,以验证该化合物在不同形态阶段的活性。用环氧-α-拉帕醌孵育导致培养物中两个物种的前鞭毛体数量显著减少,呈剂量和时间依赖性。如内吞指数的变化所示,寄生于人类巨噬细胞中的无鞭毛体的存活也受到该化合物的显著影响。我们的结果表明,环氧-α-拉帕醌在两个形态阶段均对利什曼原虫具有抗寄生虫作用,并且可能潜在地影响该寄生虫两个不同亚属中的一系列物种。

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