New lycorine-type alkaloid from Lycoris traubii and evaluation of antitrypanosomal and antimalarial activities of lycorine derivatives
New lycorine-type alkaloid from Lycoris traubii and evaluation of antitrypanosomal and antimalarial activities of lycorine derivatives
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DOI：
10.1016/j.bmc.2008.10.061
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发表时间：
2008-12-15
影响因子：
3.5
通讯作者：
Takayama, Hiromitsu
中科院分区：
文献类型：
--
作者：
Toriizuka, Yosuke;Kinoshita, Eri;Takayama, Hiromitsu
从石蒜科石蒜属（Lycoristraubii）植物海沃德（Hayward）的地上部分和鳞茎中分离得到一个新的石蒜碱衍生物LT 1（4）。经光谱分析和半合成确定其结构为1-O-（3'S）-羟基丁酰石蒜碱。一些石蒜碱酯衍生物，包括LT 1的抑制活性，对布氏锥虫布氏锥虫，与昏睡病相关的寄生虫，并对恶性疟原虫，疟疾的病原体进行了检查。其中2-O-乙酰石蒜碱（6）对寄生虫T. B. LT_1（4）、1-O-（3 ′ R）-羟基丁酰石蒜碱（8）、1，2-二-O-丁酰石蒜碱（11）和1-O-丙酰石蒜碱（12）在体外抗恶性疟原虫试验中显示出显著的活性。(C)2008爱思唯尔有限公司保留所有权利。
A new lycorine derivative LT1 (4) was isolated from the aerial part and bulbs of Lycoris traubii Hayward (Amaryllidaceae). Its structure including absolute con. guration was established by spectroscopic analysis and semi-synthesis to be 1-O-(3'S)-hydroxybutanoyllycorine. Some lycorine ester derivatives including LT1 were examined for their inhibitory activity against Trypanosoma brucei brucei, the parasite associated with sleeping sickness, and against Plasmodium falciparum, the causative agent of malaria. Among them, 2-O-acetyllycorine (6) showed the most potent activity against parasitic T. b. brucei, and LT1 (4), 1-O-(3'R)-hydroxybutanoyllycorine (8), 1,2-di-O-butanoyllycorine (11), and 1-O-propanoyllycorine (12) showed significant activity against P. falciparum in an in vitro experiment. (C) 2008 Elsevier Ltd. All rights reserved.