Adewunmi C O, Agbedahunsi J M, Adebajo A C, Aladesanmi A J, Murphy N, Wando J
Drug Research and Production Unit, Faculty of Pharmacy, Obafemi Awolowo University, Ile-Ife, Osun state, Nigeria.
J Ethnopharmacol. 2001 Sep;77(1):19-24. doi: 10.1016/s0378-8741(01)00247-1.
Trypanosoma congolense and T. brucei bloodstream form parasites were propagated axenically in suitable standard media at 34 degrees C. The effects of 33 plant extracts, fractions and pure compounds were evaluated on two clones of T. brucei and drug-sensitive and multi-drug-resistant clones of T. congolense. The cytotoxic activity of the trypanocidal extracts was also evaluated on calf aorta endothelial cells in vitro. Of the extracts tested, 22% killed T. congolense IL 1180 at a concentration of 100 microg/ml while 18% killed 90-100% of T. brucei ILTat 1.4 at the same concentration. However, 6% of the active extracts killed 93% of a dyskinetoplastid form of T. brucei IL Tat 1.1, indicating that the intact kinetoplast is a target of some of the compounds tested. Of the 12 extracts that displayed activity against drug sensitive trypanosomes, 66.7% had trypanocidal activity on a multi-drug-resistant clone, T. congolense IL 3338. The extracts of Eugenia uniflora, Acacia artaxacantha, Terminalia ivorensis, T. superba and Alchornea cordifolia had median lethal concentrations of between 13 and 69 microg/ml on both the drug-sensitive, IL 1180 and multi-drug-resistant clone, IL 3338. The median lethal doses of the active plant extracts on the calf aorta endothelial cells varied between 112 and 13750 microg/ml while the calculated selective indices ranged between 0.71 and 246.8 indicating bright prospects for the development of some of these extracts as potential trypanocidal agents.
刚果锥虫和布氏锥虫血流形式的寄生虫在34摄氏度下于合适的标准培养基中进行无细胞培养繁殖。评估了33种植物提取物、馏分和纯化合物对布氏锥虫的两个克隆以及刚果锥虫的药物敏感克隆和多药耐药克隆的作用。还在体外对小牛主动脉内皮细胞评估了杀锥虫提取物的细胞毒性活性。在所测试的提取物中，22%在浓度为100微克/毫升时杀死了刚果锥虫IL 1180，而18%在相同浓度下杀死了90%-100%的布氏锥虫ILTat 1.4。然而，6%的活性提取物杀死了93%的布氏锥虫IL Tat 1.1的动基体缺失型，这表明完整的动基体是一些测试化合物的作用靶点。在对药物敏感的锥虫显示出活性的12种提取物中，66.7%对多药耐药克隆刚果锥虫IL 3338具有杀锥虫活性。番樱桃、阿拉伯金合欢、象牙楝、大花楝和心叶刺篱木的提取物对药物敏感的IL 1180克隆和多药耐药克隆IL 3338的半数致死浓度在13至69微克/毫升之间。活性植物提取物对小牛主动脉内皮细胞的半数致死剂量在112至13750微克/毫升之间，而计算出的选择性指数在0.71至246.8之间，这表明这些提取物中的一些作为潜在杀锥虫剂开发具有光明前景。
