In vitro antitrypanosomal activity of plant terpenes against Trypanosoma brucei
In vitro antitrypanosomal activity of plant terpenes against Trypanosoma brucei
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DOI：
10.1016/j.phytochem.2011.07.015
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发表时间：
2011-11-01
期刊：
影响因子：
3.8
通讯作者：
Yamada, Haruki
中科院分区：
文献类型：
--
作者：
Otoguro, Kazuhiko;Iwatsuki, Masato;Yamada, Haruki
在筛选抗锥虫化合物的过程中，评价了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）对布氏锥虫的体外抗锥虫活性。其中22个萜类化合物具有抗锥虫活性。特别是，α-桉叶醇，hinesol，nardosinone和4-peroxy-1，2，4，5-tetrahydro-alpha-santonin都表现出选择性和有效的抗锥虫体外活性。详细介绍了24种萜类化合物与两种抗锥虫药物（依氟鸟氨酸和苏拉明）的体外抗锥虫特性和细胞毒性。这一发现代表了第一次报告的有前途的杀锥虫活性，这些萜烯。目前的研究结果也提供了一些有价值的洞察力方面的构效关系和可能的作用模式的化合物。(C)2011爱思唯尔有限公司保留所有权利。
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 Trypanosome brucei brucei. Among them, 22 terpenes exhibited antitrypanosomal activity. In particular, alpha-eudesmol, hinesol, nardosinone and 4-peroxy-1,2,4,5-tetrahydro-alpha-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. (C) 2011 Elsevier Ltd. All rights reserved.