Keiser Jennifer, El Ela Nadia Abou, El Komy Engy, El Lakkany Naglaa, Diab Tarek, Chollet Jacques, Utzinger Jürg, Barakat Rashida
Swiss Tropical Institute, Basel, Switzerland.
Am J Trop Med Hyg. 2006 Aug;75(2):287-91.
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.
一些人声称,三氯苯达唑作为一种治疗肝片吸虫病的安全有效药物,也具有抗血吸虫特性,但结果相互矛盾。我们评估了三氯苯达唑及其两种主要代谢产物对小鼠体内两种不同曼氏血吸虫菌株的作用。在感染埃及曼氏血吸虫菌株的小鼠中,在感染前3天给予单剂量120mg/kg或感染后7周给予单剂量/双剂量120 - 200mg/kg,观察到蠕虫负荷降低幅度较低(18.6 - 35.9%)。三氯苯达唑未能显著降低肝脏和肠道组织中的虫卵负荷,且观察到了所有发育阶段的虫卵。给感染利比里亚曼氏血吸虫菌株的小鼠施用400mg/kg的三氯苯达唑、三氯苯达唑砜或三氯苯达唑亚砜,导致蠕虫负荷降低<10%。相比之下,无论曼氏血吸虫菌株如何,用单剂量400、500或500mg/kg吡喹酮每天两次口服治疗的曼氏血吸虫感染小鼠中,观察到了较高的蠕虫负荷降低率(82 - 100%)。我们得出结论,三氯苯达唑及其主要代谢产物表现出微弱且不一致的杀血吸虫活性。