Sheir Sherin K, Elmongy Elshaymaa I, Mohamad Azza H, Osman Gamalat Y, Bendary Shimaa E, Ahmed Abdullah A S, Binsuwaidan Reem, El-Sayed Ibrahim El-Tantawy
Zoology Department, Faculty of Science, Menoufia University, Shibin El Kom 32511, Egypt.
Department of Pharmaceutical Sciences, College of Pharmacy, Princess Nourah bint Abdulrahman University, P.O. Box 84428, Riyadh 11671, Saudi Arabia.
Pharmaceutics. 2023 Apr 10;15(4):1200. doi: 10.3390/pharmaceutics15041200.
This work describes the synthesis of quinoline-based --heterocyclic arenes and their biological evaluation as molluscicides against adult snails as well as larvicides against larvae (miracidia and cercariae). Molecular docking studies were demonstrated to investigate their affinity for cysteine protease protein as an interesting target for antiparasitics. Compound showed the best docking results followed by in comparison to the co-crystallized ligand D1R reflected by their binding affinities and RMSD values. The egg production, hatchability of snails and ultrastructural topography of cercariae using SEM were assessed. Biological evaluations (hatchability and egg-laying capacity) revealed that the quinoline hydrochloride salt was the most effective compound against adult snails, whereas the indolo-quinoline derivative had the most efficiency against miracidia, and the acridinyl derivative was the most effective against cercariae and caused 100% mortality. and were found to modulate the biological responses of snails with/without infection and larval stages that will affect infection. caused deleterious morphological effects on cercariae. caused inhibition in the number of eggs/snail/week and reduced reproductive rate to 43.8% in all the experimental groups. and can be recommended as an effective molluscicide of plant origin for the control program of schistosomiasis.
这项工作描述了喹啉基杂环芳烃的合成及其作为杀螺剂对成年蜗牛以及作为杀幼虫剂对幼虫(毛蚴和尾蚴)的生物学评价。进行了分子对接研究,以研究它们对半胱氨酸蛋白酶蛋白的亲和力,该蛋白是抗寄生虫药物的一个有趣靶点。与共结晶配体D1R相比,化合物显示出最佳的对接结果,其次是 ,这通过它们的结合亲和力和均方根偏差值得以体现。使用扫描电子显微镜评估了蜗牛的产卵量、孵化率以及尾蚴的超微结构形貌。生物学评价(孵化率和产卵能力)表明,喹啉盐酸盐是对成年蜗牛最有效的化合物,而吲哚喹啉衍生物对毛蚴最有效,吖啶基衍生物对尾蚴最有效且导致100%死亡率。发现 和 可调节感染和未感染蜗牛以及幼虫阶段的生物学反应,这将影响感染。 对尾蚴造成有害的形态学影响。 在所有实验组中导致每只蜗牛每周的产卵数量受到抑制,繁殖率降低至43.8%。 和 可作为一种有效的植物源杀螺剂推荐用于血吸虫病防控计划。