Research Center for Tropical Diseases, Kitasato Institute for Life Sciences, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo 108-8641, Japan.
J Nat Med. 2012 Jul;66(3):558-61. doi: 10.1007/s11418-011-0613-z. Epub 2011 Nov 25.
During our search to discover new antitrypanosomal compounds, eight known plant compounds (three phenolic compounds and five kawa lactones) were evaluated for in vitro activity against Trypanosoma brucei brucei. Among them, we found two phenolic compounds and three kawa lactones possessing an α-pyrone influenced antitrypanosomal property. In particular, β-phenethyl caffeate, farnesyl caffeate and dihydrokawain exhibited high or moderate selective and potent antitrypanosomal activity in vitro. We detail here the antitrypanosomal activity and cytotoxicities of the compounds, in comparison with two commonly used antitrypanosomal drugs (eflornithine and suramin). Our findings represent the first report of the promising trypanocidal activity of these compounds.
在我们寻找新的抗锥虫化合物的过程中,评估了八种已知的植物化合物(三种酚类化合物和五种卡瓦内酯)对布氏锥虫的体外活性。其中,我们发现两种酚类化合物和三种卡瓦内酯具有受α-吡喃酮影响的抗锥虫特性。特别是β-苯乙基咖啡酸酯、法呢基咖啡酸酯和二氢卡瓦酮在体外表现出高或中等选择性和强效的抗锥虫活性。我们在这里详细介绍了这些化合物的抗锥虫活性和细胞毒性,并与两种常用的抗锥虫药物(依氟鸟氨酸和苏拉明)进行了比较。我们的发现代表了这些化合物具有有前途的杀锥虫活性的首次报道。