While searching for novel anti-echinococcosis drugs, we have been focusing on glycolysis which is relied on by Echinococcus for energy production and intermediates for other metabolic processes. The aim of this study was to investigate the potential therapeutic implication of glycolytic inhibitors on Echinococcus. Our results demonstrate that at an initial concentration of 40 μM, all inhibitors of glycolysis used in the current experiment [3-bromopyruvate (3-BrPA), ornidazole, clorsulon (CLS), sodium oxamate and 2,6-dihydroxynaphthalene (NA-P2)] show considerable in vitro effects against Echinococcus granulosus protoscoleces and Echinococcus multilocularis metacestodes. Among them, 3-BrPA exhibited the highest activity which was similar to that of nitazoxanide (NTZ) and more efficacious than albendazole (ABZ). The activity of 3-BrPA was dose dependent and resulted in severe ultrastructural destructions, as visualized by electron microscopy. An additional in vivo study in mice infected with E. multilocularis metacestodes indicates a reduction in parasite weight after the twice-weekly treatment of 25 mg/kg 3-BrPA for 6 weeks, compared to that of the untreated control. In particular, in contrast to ABZ, the administration of 25 mg/kg 3-BrPA did not cause toxicity to the liver and kidney in mice. Similarly, at the effective dose against Echinococcus larvae, 3-BrPA showed no significant toxicity to human hepatocytes. Taken together, the results suggest that interfering with the glycolysis of the parasite may be a novel chemotherapeutical option and 3-BrPA, which exhibited a remarkable activity against Echinococcus, may be a promising potential drug against cystic echinococcosis (CE) and alveolar echinococcosis (AE).

中文翻译：

---

3-溴丙酮酸盐抗棘球E球菌的体外和体内作用。

在寻找新型抗棘球co虫病药物时，我们一直专注于糖酵解，棘球cus球菌依赖糖酵解来产生能量，而其他代谢过程则依赖于中间体。这项研究的目的是调查糖酵解抑制剂对棘球oc球菌的潜在治疗意义。我们的结果表明，在初始浓度为40μM时，当前实验中使用的所有糖酵解抑制剂[3-溴丙酮酸（3-BrPA），奥硝唑，氯磺隆（CLS），草酸钠和2,6-二羟基萘（NA-P2 ）]对颗粒棘球棘球pro菌和多球棘球meta球菌都有明显的体外作用。其中3-BrPA的活性最高，与硝唑尼特（NTZ）相似，并且比阿苯达唑（ABZ）更有效。如电子显微镜所见，3-BrPA的活性是剂量依赖性的，并导致严重的超微结构破坏。另一项针对感染多叶大肠杆菌的小鼠的体内研究表明，与未治疗的对照组相比，每周两次两次25 mg / kg 3-BrPA处理6周后，寄生虫重量减少。特别是，与ABZ相比，给予25 mg / kg的3-BrPA不会对小鼠的肝脏和肾脏产生毒性。同样，以有效剂量对抗棘球E虫幼虫，3-BrPA对人肝细胞无明显毒性。两者合计，结果表明，干扰寄生虫的糖酵解可能是一种新的化学治疗选择和3-BrPA，它们对棘球chin球菌表现出显着的活性，