Ortiz Javier E, Piñeiro Mauricio, Kaiser Marcel, Mäser Pascal, Bastida Jaume, Feresin Gabriela E
Instituto de Biotecnología, Facultad de Ingeniería, Universidad Nacional de San Juan, San Juan, Argentina.
Consejo Nacional de Investigaciones Científicas y Técnicas (CONICET), CCT CONICET San Juan, San Juan, Argentina.
Chem Biodivers. 2025 Aug;22(8):e202500015. doi: 10.1002/cbdv.202500015. Epub 2025 Mar 27.
Diseases caused by trypanosomatid parasites like human African trypanosomiasis (HAT), Chagas disease (CD), leishmaniasis, and malaria are persistent health problems in developing countries that still demand new drug development. The species of the Amaryllidoideae subfamily (Amaryllidaceae) represent a vast source of alkaloids with a wide range of bioactive properties, including antiparasitic effects. The aim of this study was to evaluate the antiparasitic activity of the alkaloids hamayne, 7-hydroxyclivonine, 4-O-methylnangustine, and candimine against Trypanosoma brucei rhodesiense, Trypanosoma cruzi, Leishmania donovani, and Plasmodium falciparum parasites. The alkaloids were isolated from the leaves of Hippeastrum argentinum and Hippeastrum escoipense using several chromatographic techniques and then identified by GC-MS, UPLC-MS/MS, and NMR data. The compounds were assessed against different life cycle stages of these four parasites. Furthermore, the cytotoxic activity of the alkaloids against L6 rat skeletal myoblast cells was tested. P. falciparum was very sensible to 7-hydroxyclivonine. Candimine showed significant antiparasitic activity against all the evaluated parasites, especially T. b. rhodesiense. Candimine merits deeper research regarding its effect against trypanosomatid parasites as a lead compound for the development of alternative treatments for HAT, CD, and malaria.
由锥虫寄生虫引起的疾病,如人类非洲锥虫病(昏睡病)、恰加斯病(美洲锥虫病)、利什曼病和疟疾,在发展中国家仍然是持续存在的健康问题,仍需要开发新的药物。石蒜科石蒜亚科的植物是生物碱的丰富来源,具有广泛的生物活性,包括抗寄生虫作用。本研究的目的是评估生物碱哈马因、7-羟基克利夫宁、4-O-甲基南古斯丁和坎迪明对罗德西亚布氏锥虫、克氏锥虫、杜氏利什曼原虫和恶性疟原虫的抗寄生虫活性。使用多种色谱技术从阿根廷朱顶红和埃斯科皮氏朱顶红的叶子中分离出生物碱,然后通过气相色谱-质谱联用仪(GC-MS)、超高效液相色谱-串联质谱仪(UPLC-MS/MS)和核磁共振数据进行鉴定。对这四种寄生虫的不同生命周期阶段评估了这些化合物。此外,还测试了生物碱对L6大鼠骨骼肌成肌细胞的细胞毒性活性。恶性疟原虫对7-羟基克利夫宁非常敏感。坎迪明对所有评估的寄生虫均表现出显著的抗寄生虫活性,尤其是罗德西亚布氏锥虫。坎迪明作为治疗昏睡病、美洲锥虫病和疟疾替代疗法开发的先导化合物,其对锥虫寄生虫的作用值得深入研究。