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评价 (-)-古巴醇和 (-)-扁柏素对克氏锥虫的体内治疗特性。

Evaluation of the in vivo therapeutic properties of (-)-cubebin and (-)-hinokinin against Trypanosoma cruzi.

机构信息

Núcleo de Pesquisa em Ciências Exatas e Tecnológicas da Universidade de Franca, Av. Dr. Armando Salles Oliveira, 201-Cx. Postal 82-Pq. Universitário, 14404-600 Franca, SP, Brazil.

出版信息

Exp Parasitol. 2013 Apr;133(4):442-6. doi: 10.1016/j.exppara.2012.12.005. Epub 2012 Dec 27.

Abstract

Even though the Chagas' disease, caused by the protozoan Trypanosoma cruzi, was described 100years ago by Carlos Chagas, it still represents a major public health concern and is found in 18 developing countries in South and Central America. In Brazil, Benznidazole (Rochagan) is the only drug with trypanocidal activity available in the market, despite its several side effects and limited efficacy in the chronic phase of the infection. In view of the need for new substances displaying biological activity against T. cruzi, there has been growing interest in research toward the attainment of compounds capable of acting on the parasite while being devoid of serious side effects. In this context, this study aims to evaluate the in vivo therapeutic activity of dibenzylbutyrolactone lignans (-)-cubebin and (-)-hinokinin during the acute phase of infection by T. cruzi. As a study criterion, animals with acute parasitemia were investigated by tissue morphometric analysis. There was significant parasitemia reduction in the groups of animals treated with (-)-cubebin or (-)-hinokin oral administration, compared to the negative control. Values close to those of the uninfected control were found in the groups treated with (-)-cubebin and (-)-hinokinin via kariometry, showing that there was positive cellular response compared to the infected control.

摘要

尽管由原生动物克氏锥虫引起的恰加斯病在 100 年前就被卡洛斯·查加斯描述过,但它仍然是一个主要的公共卫生关注点,在南美和中美 18 个发展中国家都有发现。在巴西,贝那唑啉(罗氏甘)是市场上唯一具有杀锥虫活性的药物,尽管它有许多副作用,并且在感染的慢性阶段疗效有限。鉴于需要具有针对 T. cruzi 的生物活性的新物质,人们对研究能够在没有严重副作用的情况下作用于寄生虫的化合物的兴趣日益浓厚。在这种情况下,本研究旨在评估二苄基丁内酯木脂素(-)-胡椒酚和(-)-扁柏脂素在 T. cruzi 感染的急性期的体内治疗活性。作为研究标准,通过组织形态计量分析研究了伴有急性寄生虫血症的动物。与阴性对照组相比,经(-)-胡椒酚或(-)-扁柏脂素口服治疗的动物寄生虫血症明显减少。经 kariometry 治疗的(-)-胡椒酚和(-)-扁柏脂素组的数值接近未感染对照组,表明与感染对照组相比,细胞反应呈阳性。

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