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首页> 外文期刊>Antimicrobial agents and chemotherapy. >Efficacies of albendazole sulfoxide and albendazole sulfone against In vitro-cultivated Echinococcus multilocularis metacestodes.
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Efficacies of albendazole sulfoxide and albendazole sulfone against In vitro-cultivated Echinococcus multilocularis metacestodes.

机译：阿苯达唑亚砜和阿苯达唑砜对体外培养的多球棘球meta球菌的功效。

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摘要

The metacestode stage of Echinococcus multilocularis is the causative agent of alveolar echinococcosis (AE), a parasitic disease affecting the liver, with occasional metastasis into other organs. Benzimidazole carbamate derivatives such as mebendazole and albendazole are currently used for chemotherapeutic treatment of AE. Albendazole is poorly resorbed and is metabolically converted to its main metabolite albendazole sulfoxide, which is believed to be the active component, and further to albendazole sulfone. Chemotherapy with albendazole has been shown to have a parasitostatic rather than a parasitocidal effect; it is not effective in all cases, and the recurrence rate is rather high once chemotherapy is stopped. Thus, development of new means of chemotherapy of AE is needed. This could include modifications of benzimidazoles and elucidiation of the respective biological pathways. In this study we performed in vitro drug treatment of E. multilocularis metacestodes with albendazole sulfoxide and albendazole sulfone. High-performance liquid chromatography analysis of vesicle fluids showed that the drugs were taken up rapidly by the parasite. Transmission electron microscopic investigation of parasite tissues and nuclear magnetic resonance spectroscopy of vesicle fluids demonstrated that albendazole sulfoxide and albendazole sulfone had similar effects with respect to parasite ultrastructure and changes in metabolites in vesicle fluids. This study shows that the in vitro cultivation model presented here provides an ideal first-round test system for screening of antiparasite drugs.
机译：多叶棘球oc球的前肠阶段是肺泡棘球co病（AE）的病原体，是一种影响肝脏的寄生虫病，偶有转移到其他器官的现象。苯并咪唑氨基甲酸酯衍生物，如甲苯苯达唑和阿苯达唑目前被用于AE的化学治疗。阿苯达唑的吸收较差，并且被代谢转化为其主要代谢产物阿苯达唑亚砜（据信是活性成分），并进一步转化成阿苯达唑砜。阿苯达唑的化学疗法已显示出具有抑寄生作用，而不具有杀寄生作用。它并非在所有情况下都有效，并且一旦停止化疗，复发率就很高。因此，需要开发新的AE化学疗法。这可能包括苯并咪唑的修饰和相应生物途径的阐明。在这项研究中，我们进行了阿苯达唑亚砜和阿苯达唑砜对多叶大肠杆菌的体外药物治疗。囊泡液的高效液相色谱分析表明，该药物被寄生虫迅速吸收。寄生虫组织的透射电子显微镜研究和囊泡液的核磁共振波谱表明，阿苯达唑亚砜和阿苯达唑砜对寄生虫超微结构和囊泡液中代谢物的变化具有相似的作用。这项研究表明，此处介绍的体外培养模型为筛选抗寄生虫药物提供了理想的第一轮测试系统。

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