Abstract：
We examined the antiamoebic effect of several imidazothiazole derivatives on Acanthamoeba castellanii of the T4 genotype. Trypan blue exclusion assays and haemocytometer counting were used to determine the reduction in A. castellanii trophozoite proliferation, in response to treatment with these compounds. To determine the effects of these compounds on host cells, lactate dehydrogenase assay was performed using HeLa cell lines. Amoebicidal assays revealed that the tested compounds at concentrations of 50 µM significantly inhibited amoebae trophozoites compared to controls. Compounds 1m and 1zb showed the highest amoebicidal effects eradicating 70% and 67% of A. castellanii, respectively. The compounds blocked both the encystation and excystation process in A. castellanii. Compounds 1m and 1zb blocked 61% and 55%, respectively, of amoeba binding to human cells. Moreover, the compounds showed minimal cytotoxic effects against host cells and considerably reduced amoeba-mediated host cell death. Overall, our study revealed that compounds 1m and 1zb have excellent antiamoebic potential, and should be considered in the development of curative antiamoebic medications in future studies. Further work is critical to determine the translational value of these findings.
摘要：
我们研究了几种咪唑并噻唑衍生物对T4基因型的棘阿米巴的抗阿米巴作用。台盼蓝排除试验和血细胞计数器计数用于确定castellanii滋养体增殖的减少。响应这些化合物的治疗。为了确定这些化合物对宿主细胞的影响，使用HeLa细胞系进行乳酸脱氢酶测定。杀菌试验表明，与对照组相比，浓度为50µM的测试化合物显着抑制变形虫滋养体。化合物1m和1zb显示出最高的杀变形虫效果，根除了70％和67％的卡氏A。分别。这些化合物阻断了卡斯特兰氏杆菌的包封和脱落过程。化合物1m和1zb阻断61%和55%，分别,变形虫与人类细胞的结合。此外，这些化合物对宿主细胞的细胞毒性作用最小，并大大减少了变形虫介导的宿主细胞死亡。总的来说,我们的研究表明，化合物1m和1zb具有优异的抗阿米巴潜能，在未来的研究中，应考虑开发治疗性抗阿米巴药物。进一步的工作对于确定这些发现的翻译价值至关重要。
