Fiot Julien, Sanon Souleymane, Azas Nadine, Mahiou Valérie, Jansen Olivia, Angenot Luc, Balansard Guy, Ollivier Evelyne
Laboratory of Pharmacognosy, Faculty of Pharmacy, Marseille, France.
J Ethnopharmacol. 2006 Jun 30;106(2):173-8. doi: 10.1016/j.jep.2005.12.030. Epub 2006 Jan 27.
The chemical composition of total alkaloids from leaves and roots of Guiera senegalensis was investigated. Three beta-carboline alkaloids were purified: in addition to harman and tetrahydroharman, known in roots and leaves, harmalan (dihydroharman) was isolated for the first time from roots of Guiera senegalensis. Guieranone A, a naphthyl butenone, was also purified from leaves and roots. The in vitro antiplasmodial activity and the cytotoxicity of extracts and pure compounds were evaluated. Each total alkaloid extract and beta-carboline alkaloids presented an interesting antiplasmodial activity associated with a low cytotoxicity. Harmalan was less active than harman and tetrahydroharman. Guieranone A showed a strong antiplasmodial activity associated with a high cytotoxicity toward human monocytes. Its cytotoxicity was performed against two cancer cell lines and normal skin fibroblasts in order to study its anticancer potential: guieranone A presented a strong cytotoxicity against each cell strains. Finally, we evaluated the potent synergistic antimalarial interaction between Guiera senegalensis and two plants commonly associated in traditional remedies: Mitragyna inermis and Pavetta crassipes. Three associations evaluated were additive. A synergistic effect was shown between total alkaloids extracted from leaves of Guiera senegalensis and those of Mitragyna inermis. This result justified the traditional use of the plants in combination to treat malaria.
对塞内加尔盖拉（Guiera senegalensis）叶和根中总生物碱的化学成分进行了研究。纯化出三种β-咔啉生物碱：除了根和叶中已知的哈尔满和四氢哈尔满外，首次从塞内加尔盖拉根中分离出哈尔马兰（二氢哈尔满）。还从叶和根中纯化出了一种萘基丁烯酮——盖拉酮A。对提取物和纯化合物的体外抗疟活性及细胞毒性进行了评估。每种总生物碱提取物和β-咔啉生物碱均表现出有趣的抗疟活性，且细胞毒性较低。哈尔马兰的活性低于哈尔满和四氢哈尔满。盖拉酮A表现出较强的抗疟活性，但对人单核细胞具有较高的细胞毒性。为了研究其抗癌潜力，对两种癌细胞系和正常皮肤成纤维细胞进行了细胞毒性测试：盖拉酮A对每种细胞株均表现出较强的细胞毒性。最后，我们评估了塞内加尔盖拉与传统疗法中常用的两种植物——无刺帽蕊木（Mitragyna inermis）和厚叶巴韦特木（Pavetta crassipes）之间强大的协同抗疟相互作用。所评估的三种组合均为相加作用。塞内加尔盖拉叶中提取的总生物碱与无刺帽蕊木叶中提取的总生物碱之间表现出协同效应。这一结果证明了这些植物联合用于治疗疟疾的传统用法是合理的。
