Department of Pharmacology and Therapeutics, University of Ibadan, Ibadan, Nigeria.
Parasitol Res. 2012 Feb;110(2):521-6. doi: 10.1007/s00436-011-2516-z. Epub 2011 Jul 26.
Human African trypanosomiasis is a neglected tropical disease with complex clinical presentation, diagnosis, and difficult treatment. The available drugs for the treatment of trypanosomiasis are old, expensive, and less effective, associated with severe adverse reactions and face the problem of drug resistance. This situation underlines the urgent need for the development of new, effective, cheap, and safe drugs for the treatment of trypanosomiasis. The search for new antitrypanosomal agents in this study is based on ethnomedicine. In vitro antitrypanosomal activity of 36 plant extracts from 10 plant species from Nigerian ethnomedicine was evaluated against bloodstream forms of Trypanosoma brucei rhodesiense STIB 900. Cytotoxic activity was determined against mammalian L6 cells. Alamar blue assay was used to measure the endpoint of both antitrypanosomal and toxicity assays. The ethyl acetate extract of leaves of Ocimum gratissimum Linn. (Labiatae) showed the highest antitrypanosomal activity (IC(50) of 2.08 ± 0.01 μg/ml) and a high selective index of 29. Furthermore, the hexane, ethyl acetate, or methanol extracts of Trema orientalis (L.) Blume (Ulmaceae), Pericopsis laxiflora (Benth. ex Baker) Meeuwen, Jatropha curcas Linn. (Euphorbiaceae), Terminalia catappa Linn. (Combretaceae), and Vitex doniana Sweet (Verbenaceae) displayed remarkable antitrypanosomal activity (IC(50) 2.1-17.2 μg/ml) with high selectivity indices (20-80) for trypanosomes. The antitrypanosomal activity of T. catappa and T. orientalis against T. brucei rhodesiense (STIB 900) is being reported for the first time in Nigerian ethnomedicine, and these plants could be a potential source of antitrypanosomal agents.
人体感染非洲锥虫病是一种被忽视的热带病，其临床表现、诊断复杂，治疗困难。现有的抗锥虫病药物较为陈旧、昂贵且疗效欠佳，与严重的不良反应相关，并面临耐药性问题。这种情况突出表明，迫切需要开发新的、有效、廉价且安全的抗锥虫病药物。本研究中针对新的抗锥虫药物的寻找基于民族医学。对来自尼日利亚民族医学的 10 种植物的 36 种植物提取物的抗锥虫血腔期活性进行了评估，所用的病原体为布氏冈比亚锥虫 STIB 900。采用哺乳动物 L6 细胞测定细胞毒性。采用 Alamar blue 法测定抗锥虫和毒性测定的终点。非洲菊（Labiatae）叶的乙酸乙酯提取物表现出最高的抗锥虫活性（IC50 为 2.08 ± 0.01 μg/ml）和 29 的高选择指数。此外，Trema orientalis（Ulmaceae）、Pericopsis laxiflora（Benth. ex Baker）Meeuwen、Jatropha curcas Linn.（Euphorbiaceae）、Terminalia catappa Linn.（Combretaceae）和 Vitex doniana Sweet（Verbenaceae）的正己烷、乙酸乙酯或甲醇提取物也表现出显著的抗锥虫活性（IC50 为 2.1-17.2 μg/ml），对锥虫的选择性指数为 20-80。T. catappa 和 T. orientalis 对布氏冈比亚锥虫（STIB 900）的抗锥虫活性在尼日利亚民族医学中尚属首次报道，这些植物可能是抗锥虫药物的潜在来源。
