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1-(2-羟基亚苄基)氨基硫脲对马媾疫锥虫的体外杀锥虫活性

Ex vivo trypanocidal activity of 1-(2-hydroxybenzylidene)thiosemicarbazide against Trypanosoma equiperdum.

作者信息

Parra N, Jaume M, Boscán K, Hernández A, Mijares A, González M, Alvarado Y, Restrepo J

机构信息

Laboratory of Parasites Physiology. Instituto Venezolano de Investigaciones Científicas, Caracas, Venezuela.

Laboratory of Research in Sustainable New Materials Synthesis. Centro de Investigación y Tecnología de Materiales. Instituto Venezolano de Investigaciones Científicas, Maracaibo, Venezuela.

出版信息

Vet Parasitol. 2017 Oct 15;245:163-167. doi: 10.1016/j.vetpar.2017.06.012. Epub 2017 Jul 8.

Abstract

Trypanosoma equiperdum is the causative agent of dourine, a venereal disease in horses and donkeys. This parasite has a widely distribution, is found in Africa, Asia, Southern and Eastern Europe, Russia, Mexico and Venezuela. The T. equiperdum is morphologically indistinguishable to other Trypanozoon species, however differs from other mammalian trypanosomes due to the fact that it is primarily a tissue parasite, generating cutaneous plaques, swelling of genitalia and neurological signs. The aim of this study was to evaluate the trypanocidal effectiveness of a set of derivatives of thiosemicarbazones on a T. equiperdum ex vivo culture. All compounds appeared to have trypanocidal activity, however one of them shown better solubility and a dose-dependent effect. The median inhibitory concentration (IC) was 1.2μM. The selected compound exhibits a greater inhibitory activity than diminazene aceturate, a common drug for animal trypanosomosis treatment.

摘要

马媾疫锥虫是马和驴的一种性传播疾病——马媾疫的病原体。这种寄生虫分布广泛,在非洲、亚洲、南欧和东欧、俄罗斯、墨西哥和委内瑞拉都有发现。马媾疫锥虫在形态上与其他锥虫属物种无法区分,但与其他哺乳动物锥虫不同,因为它主要是一种组织寄生虫,会产生皮肤斑块、生殖器肿胀和神经症状。本研究的目的是评估一组缩氨基硫脲衍生物对马媾疫锥虫体外培养物的杀锥虫效果。所有化合物似乎都具有杀锥虫活性,然而其中一种表现出更好的溶解性和剂量依赖性效应。半数抑制浓度(IC)为1.2μM。所选化合物表现出比乙酰氨基阿苯达唑(一种治疗动物锥虫病的常用药物)更强的抑制活性。

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