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[顺铂(II)喷他脒对布氏布氏锥虫引起的绵羊实验性锥虫病的抗寄生虫活性]

[Antiparasitic activity of Cis-Pt (II) pentamidine in experimental trypanosomiasis of sheep caused by Trypanosoma brucei brucei].

作者信息

Dreyfuss G, Gayral P, Dubost G, Nicolas J A, Craciunescu D

机构信息

Laboratoire de Parasitologie, Faculté de Médecine de Limoges.

出版信息

Bull Soc Pathol Exot Filiales. 1988;81(3 Pt 2):626-31.

PMID:3197258
Abstract

The failure of trypanocidal therapeutics have made it a duty to use other classes of molecules which show a comparable trypanocidal efficacy with well-known medicines. In this study, the authors have evaluated the trypanocidal activity of a Cis-Platinum (II) salt, DNA-intercalating medicine used in antineoplastic therapeutics, associated with pentamidine: Cis-Pt (II) pentamidine. After primary screenings on a murine model of T. brucei brucei, Cis-Pt (II) pentamidine was evaluated on an experimental sheep trypanosomiasis model, standardized by the Institute of Neurological Epidemiology and Tropical Neurology of Limoges (France). Cis-Pt (II) pentamidine was able to cure infected mice, without relapse, after a single subcutaneous injection of 12.5 mg.kg-1 body weight. In sheep trypanosomiasis, the same treatment was used successfully during the first stage of infection. Neurological stage susceptibility and pharmacokinetics in sheep will be evaluated in a further study.

摘要

杀锥虫疗法的失败使得使用其他类分子成为一项必要任务,这些分子需与知名药物具有相当的杀锥虫功效。在本研究中,作者评估了一种顺铂(II)盐(一种用于抗肿瘤治疗的DNA嵌入药物)与喷他脒联合使用时的杀锥虫活性:顺铂(II)喷他脒。在对布氏布氏锥虫小鼠模型进行初步筛选后,在法国利摩日神经流行病学和热带神经病学研究所标准化的实验性绵羊锥虫病模型上评估了顺铂(II)喷他脒。顺铂(II)喷他脒在单次皮下注射12.5mg·kg-1体重后能够治愈感染的小鼠且无复发。在绵羊锥虫病中,相同的治疗方法在感染的第一阶段成功使用。绵羊的神经阶段易感性和药代动力学将在进一步的研究中进行评估。

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Bull Soc Pathol Exot Filiales. 1988;81(3 Pt 2):626-31.
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