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首页> 外文期刊>The American Journal of Tropical Medicine and Hygiene >Triclabendazole and its two main metabolites lack activity against schistosoma mansoni in the mouse model.
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Triclabendazole and its two main metabolites lack activity against schistosoma mansoni in the mouse model.

机译：Triclabendazole及其两种主要代谢产物在小鼠模型中对曼氏血吸虫没有活性。

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Some have claimed that triclabendazole, a safe and efficacious drug for the treatment of fascioliasis, also exhibits antischistosomal properties, but results are conflicting. We assessed the effect of triclabendazole and its two main metabolites against two different strains of Schistosoma mansoni harbored in mice. Low worm burden reductions (18.6-35.9%) were observed in mice infected with an Egyptian strain of S. mansoni and treated with a single dose of 120 mg/kg 3 days before infection or single/double doses of 120-200 mg/kg 7 weeks after infection. Triclabendazole failed to significantly reduce hepatic and intestinal tissue egg loads, and eggs of all developmental stages were observed. Administration of 400 mg/kg of either triclabendazole, triclabendazole sulphone, or triclabendazole sulfphoxide to mice infected with a Liberian strain of S. mansoni resulted in worm burden reductions < 10%. In comparison, high worm burden reductions (82-100%) were observed in S. mansoni-infected mice treated with single oral doses of 400, 500, or 500 mg/kg twice a day praziquantel, regardless of the S. mansoni strain. We conclude that triclabendazole and its main metabolites display weak and inconsistent schistosomicidal activities.
机译：一些人声称三氯苯达唑是一种安全有效的治疗筋膜病的药物，它还具有抗血吸虫病的特性，但结果相矛盾。我们评估了三氯苯达唑及其两种主要代谢物对小鼠体内藏匿的曼氏血吸虫的两种不同品系的影响。在感染埃及曼氏沙门氏菌的小鼠中，感染前3天以120 mg / kg的单次剂量或120-200 mg / kg的单次/两次剂量处理的小鼠中观察到的蠕虫负担降低率较低（18.6-35.9％）感染后7周。 Triclabendazole未能显着降低肝脏和肠道组织的卵负荷，并且观察到了所有发育阶段的卵。对感染了曼氏沙门氏菌利比里亚毒株的小鼠施用400 mg / kg的三氯苯达唑，三氯苯达唑砜或三氯苯达唑亚砜可减少蠕虫负担，降低<10％。相比之下，在每天两次口服吡喹酮单次口服剂量分别为400、500或500 mg / kg的曼氏葡萄球菌感染的小鼠中，无论曼氏葡萄球菌菌株如何，均可观察到较高的蠕虫减负（82-100％）。我们得出的结论是三氯苯达唑及其主要代谢产物显示出弱和不一致的血吸虫杀虫活性。

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