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Tacrolimus, a rapamycin target protein inhibitor, exerts anti-cystic echinococcosis effects both in vitro and in vivo.
Acta Tropica ( IF 2.1 ) Pub Date : 2020-09-18 , DOI: 10.1016/j.actatropica.2020.105708
Muzhabaier Muhedier 1 , Jintian Li 2 , Hui Liu 3 , Guizhi Ma 4 , Kuerbannisha Amahong 3 , Renyong Lin 3 , Guodong Lü 2
Affiliation  

In view of a growing need for new treatment options for human cystic echinococcosis (CE), we aimed to investigate the efficacy of mTOR pathway inhibitors against CE in vitro and in vivo. Among the seven mTOR inhibitors evaluated, tacrolimus (TAC) showed significant dose- and time-dependent killing of cultured protoscoleces and cysts in vitro. Notably, the oral administration of TAC (4 mg/kg/day) to CE mice model highly effectively reduced both the weight and number of parasitic cysts. Transmission electron microscopy revealed that TAC destroys the ultrastructure of cysts, both in vitro and in vivo. Furthermore, TAC had no significant effect on blood glucose, body weight, liver, or kidney functions in mice. We further observed that the ATP levels and glucose content of cysts reduced upon TAC treatment, indicating that inhibiting mTORC1 activity possibly affects glucose metabolism in the cysts of mice. Based on our experimental data, TAC emerged as a promising anti-cyst drug that efficiently inhibits the growth of cysts.



中文翻译:

他克莫司是雷帕霉素的靶蛋白抑制剂,在体外和体内均发挥抗囊性棘球co病的作用。

鉴于对人囊性棘球co虫病(CE)的新治疗选择的需求日益增长,我们旨在研究mTOR途径抑制剂在体外体内对CE的疗效。在评估的七种mTOR抑制剂中,他克莫司(TAC)在体外对培养的原生色素和囊肿具有明显的剂量和时间依赖性杀灭作用。值得注意的是,对CE小鼠口服TAC(4 mg / kg / day)可以有效地减轻寄生虫囊肿的重量和数量。透射电子显微镜揭示,TAC破坏囊肿的超微结构,二者在体外体内。此外,TAC对小鼠的血糖,体重,肝或肾功能无明显影响。我们进一步观察到,TAC处理后囊肿的ATP水平和葡萄糖含量降低,表明抑制mTORC1活性可能会影响小鼠囊肿的葡萄糖代谢。根据我们的实验数据,TAC成为一种有前途的抗囊肿药物,可有效抑制囊肿的生长。

更新日期:2020-09-24
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