Instituto Universitario de Enfermedades Tropicales y Salud Pública de Islas Canarias, Universidad de La Laguna, Avda. Astrofísico F. Sánchez s/n, 38206 La Laguna, Tenerife, Spain.
Instituto Universitario de Bio-Orgánica Antonio González (IUBO AG), Centro de Investigaciones Biomédicas de Canarias (CIBICAN), Universidad de La Laguna (ULL), Avda. Astrofísico F. Sánchez, 2, 38206 La Laguna, Tenerife, Spain.
Mar Drugs. 2019 Jul 19;17(7):420. doi: 10.3390/md17070420.
genus is a widely distributed and opportunistic parasite with increasing importance worldwide as an emerging pathogen in the past decades. This protozoan has an active trophozoite stage, a cyst stage, and is dormant and very resistant. It can cause keratitis, an ocular sight-threatening disease, and granulomatous amoebic encephalitis, a chronic, very fatal brain pathology. In this study, the amoebicidal activity of sixteen oxasqualenoid metabolites and semisynthetic derivatives were tested against Neff. The results obtained point out that iubol () and dehydrothyrsiferol () possess potent activities, with IC values of 5.30 and 12.83 µM, respectively. The hydroxylated congeners thyrsiferol () and 22-hydroxydehydrothyrsiferol (), active in the same value range at IC 13.97 and 17.00 µM, are not toxic against murine macrophages; thus, they are solid candidates for the development of new amoebicidal therapies.
纳氏棘阿米巴属是一种广泛分布且具有机会性的寄生虫,在过去几十年中,作为一种新兴的病原体,其在全球范围内的重要性日益增加。这种原生动物具有活跃的滋养体阶段、囊泡阶段,处于休眠状态且具有很强的抵抗力。它可引起角膜炎,这是一种威胁视力的眼部疾病,以及肉芽肿性阿米巴脑炎,这是一种慢性的、非常致命的脑部疾病。在这项研究中,测试了 16 种氧化角鲨烯代谢物和半合成衍生物对 Neff 的杀阿米巴活性。得到的结果表明,伊博醇()和去氢硫代胆甾醇()具有很强的活性,IC 值分别为 5.30 和 12.83 µM。羟基同系物硫代胆甾醇()和 22-羟基去氢硫代胆甾醇()在 IC 13.97 和 17.00 µM 时具有相同的活性,对鼠巨噬细胞没有毒性;因此,它们是开发新的杀阿米巴疗法的可靠候选药物。