Martín-Montes Álvaro, Martínez-Camarena Álvaro, Lopera Alberto, Bonastre-Sabater Irene, Clares M Paz, Verdejo Begoña, García-España Enrique, Marín Clotilde
Departamento de Parasitología, Instituto de Investigación Biosanitaria (IBS. Granada), Hospitales Universitarios de Granada, Universidad de Granada, Severo Ochoa s/n, 18071 Granada, Spain.
Instituto de Ciencia Molecular (ICMol), Universidad de Valencia, C/Catedrático José Beltrán 2, 46980 Paterna, Spain.
Pharmaceutics. 2023 Mar 20;15(3):992. doi: 10.3390/pharmaceutics15030992.
Due to the urgent need for finding effective and free of secondary effect treatments for every clinical form of Leishmaniasis, a series of synthetic xylene, pyridine and, pyrazole azamacrocycles were tested against three species. A total of 14 compounds were tested against J774.2 macrophage cells which were models for host cells, and against promastigote and amastigote forms of each studied parasite. Amongst these polyamines, one proved effective against another one for and and another one was selective solely for These compounds showed leishmanicidal activity and reduced parasite infectivity and dividing ability. Action mechanism studies gave a hint that compounds were active against due to their ability to alter parasite metabolic pathways and reduce (except Py33333) parasitic Fe-SOD activity.
由于迫切需要为每种临床类型的利什曼病找到有效且无副作用的治疗方法，对一系列合成的二甲苯、吡啶和吡唑氮杂大环化合物针对三种物种进行了测试。总共14种化合物针对作为宿主细胞模型的J774.2巨噬细胞以及每种研究寄生虫的前鞭毛体和无鞭毛体形式进行了测试。在这些多胺中，一种对另一种有效，另一种仅对有选择性。这些化合物表现出杀利什曼原虫活性，并降低了寄生虫的感染性和分裂能力。作用机制研究表明，这些化合物对有活性是由于它们能够改变寄生虫的代谢途径并降低（除Py33333外）寄生虫的铁超氧化物歧化酶活性。
