Research Center for Tropical Diseases, Kitasato Institute for Life Sciences, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo 108-8641, Japan.
Phytochemistry. 2011 Nov;72(16):2024-30. doi: 10.1016/j.phytochem.2011.07.015. Epub 2011 Aug 16.
During the course of screening to discover antitrypanosomal compounds, 24 known plant terpenes (6 sesquiterpenes, 14 sesquiterpene lactones and 4 diterpenes) were evaluated for in vitro antitrypanosomal activity against Trypanosoma brucei brucei. Among them, 22 terpenes exhibited antitrypanosomal activity. In particular, α-eudesmol, hinesol, nardosinone and 4-peroxy-1,2,4,5-tetrahydro-α-santonin all exhibited selective and potent antitrypanosomal activities in vitro. Detailed here in an in vitro antitrypanosomal properties and cytotoxicities of the 24 terpenes compared with two therapeutic antitrypanosomal drugs (eflornithine and suramin). This finding represents the first report of promising trypanocidal activity of these terpenes. Present results also provide some valuable insight with regard to structure-activity relationships and the possible mode of action of the compounds.
在筛选抗锥虫化合物的过程中，评估了 24 种已知植物萜类化合物（6 种倍半萜、14 种倍半萜内酯和 4 种二萜）对布鲁氏锥虫的体外抗锥虫活性。其中，22 种萜类化合物具有抗锥虫活性。特别是α-艾杜醇、海松醇、nardosinone 和 4-过氧-1,2,4,5-四氢-α-山酮都表现出体外选择性和强效的抗锥虫活性。本文详细比较了这 24 种萜类化合物与两种治疗性抗锥虫药物（依氟鸟氨酸和苏拉明）的体外抗锥虫特性和细胞毒性。这一发现代表了这些萜类化合物具有潜在杀锥虫活性的首次报道。目前的结果还为化合物的结构-活性关系和可能的作用模式提供了一些有价值的见解。
