Marín Clotilde, Boutaleb-Charki Samira, Díaz Jesús G, Huertas Oscar, Rosales María J, Pérez-Cordon Gregorio, Guitierrez-Sánchez Ramon, Sánchez-Moreno Manuel
Department of Parasitology, University of Granada, Granada, Spain.
J Nat Prod. 2009 Jun;72(6):1069-74. doi: 10.1021/np8008122.
A set of flavonoids from Consolida oliveriana, kaempferol (1), quercetin (2), trifolin (3), and acetyl hyperoside (5) and their O-acetyl derivatives (1a, 2a, 3a), and octa-O-acetylhyperoside (4) showed leishmanicidal activity against promastigote as well as amastigote forms of Leishmania spp. The cellular proliferation, metabolic, and ultrastructural studies showed that the acetylated compounds 2a, 3a, and 4 were highly active against Leishmania (V.) peruviana, while 2a as well as 4 were effective against Leishmania (V.) braziliensis. These compounds were not cytotoxic and are effective at similar concentrations up to or lower than the reference drugs (pentostam and glucantim).
从毛茛叶飞燕草(Consolida oliveriana)中提取的一组黄酮类化合物,山奈酚(1)、槲皮素(2)、三叶豆苷(3)、乙酰金丝桃苷(5)及其O - 乙酰化衍生物(1a、2a、3a)以及八 - O - 乙酰金丝桃苷(4),对利什曼原虫的前鞭毛体和无鞭毛体形式均表现出杀利什曼原虫活性。细胞增殖、代谢和超微结构研究表明,乙酰化化合物2a、3a和4对秘鲁利什曼原虫(Leishmania (V.) peruviana)具有高活性,而2a以及4对巴西利什曼原虫(Leishmania (V.) braziliensis)有效。这些化合物无细胞毒性,且在与参考药物(喷他脒和葡糖胺锑)相同或更低的浓度下有效。