Abstract：
The study aimed to conduct in vitro biological assessments of hydantoin and thiohydantoin compounds against mature Schistosoma mansoni worms, evaluate their cytotoxic effects and predict their pharmacokinetic parameters using computational methods. The compounds showed low in vitro cytotoxicity and were not considered hemolytic. Antiparasitic activity against adult S. mansoni worms was tested with all compounds at concentrations ranging from 200 to 6.25 μM. Compounds SC01, SC02, and SC03 exhibited low activity. Compounds SC04, SC05, SC06 and SC07 caused 100 % mortality within 24 h of incubation at a concentration of 100 and 200 μM. Thiohydantoin SC04 exhibited the highest activity, resulting in 100 % mortality after 24 h of incubation at a concentration of 50 μM and IC50 of 28 µM. In the ultrastructural analysis (SEM), the compound SC04 (200 µM) induced integumentary changes, formation of integumentary blisters, and destruction of tubercles and spicules. Therefore, the SC04 compound shows promise as an antiparasitic against S. mansoni.
摘要：
该研究旨在对海内酰脲和硫内酰脲化合物对成熟的曼氏血吸虫进行体外生物学评估，使用计算方法评估其细胞毒性作用并预测其药代动力学参数。所述化合物显示低的体外细胞毒性并且不被认为是溶血的。用浓度范围为200至6.25μM的所有化合物测试了对成虫S.mansoni蠕虫的抗寄生虫活性。化合物SC01、SC02和SC03表现出低活性。化合物SC04、SC05、SC06和SC07在100和200μM的浓度下孵育24小时内引起100%死亡率。硫内酰脲SC04表现出最高的活性，在50μM的浓度和28μM的IC50孵育24小时后导致100%死亡率。在超微结构分析(SEM)中，化合物SC04（200µM）诱导外皮变化，外皮水泡的形成，以及结节和针状体的破坏。因此,SC04化合物显示出有望作为抗曼氏芽孢杆菌的抗寄生虫药。
