Synthesis of 1-O-acetylbritannilactone analogues from Inula britannica and in vitro evaluation of their anticancer potential
Synthesis of 1-O-acetylbritannilactone analogues from Inula britannica and in vitro evaluation of their anticancer potential
复制标题
不列颠旋覆花 1-O-乙酰基不列颠内酯类似物的合成及其体外抗癌潜力评价
DOI：
10.1039/c4md00209a
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发表时间：
2014-09
期刊：
影响因子：
--
通讯作者：
Jin-Ming Gao
中科院分区：
文献类型：
--
作者：
Shuai Dong;Yang-Yang Han;Ming Lei;Jin-Ming Gao
从药用植物旋覆花（Inula britannica）的花中分离得到的倍半萜内酯1-O-乙酰基旋覆花内酯（1-O-acetylbritannilactone，ABL）具有较强的体外抗癌活性。已有研究表明ABL的6-羟基侧链酯类似物具有较好的抗癌活性。为了寻找新的天然抗癌药物，通过在ABL的6-OH位引入N/O原子和进行芳环酯化反应，合成了一系列新型ABL类似物，并对其体外抗癌活性和细胞毒性机理进行了研究。用代表性活性化合物4a处理HeLa细胞显示出诱导凋亡（如通过双参数细胞荧光分析所揭示的）和激活半胱天冬酶-3。流式细胞仪分析证实4a具有明显阻滞细胞周期于G2/M期的能力。
The natural product 1-O-acetylbritannilactone (ABL), a sesquiterpene lactone (STL) isolated from flowers of the medicinal plant Inula britannica, was found to have potent anticancer activity in vitro. Previous studies showed that the 6-OH side chain ester analogues of ABL displayed better anticancer activity. In order to look for new natural-product-based anticancer agents, a series of novel ABL analogues was synthesized by N/O-atom introduction and aromatic ring esterification at the 6-OH position of ABL, and the in vitro anticancer activities and mechanistic basis of cytotoxicity of the resulting compounds were investigated. Treatment of HeLa cells with the representative active compound 4a showed induction of apoptosis, as revealed by a biparametric cytofluorimetric analysis, and activation of caspase-3. The ability of 4a to obviously arrest the cell cycle at the G2/M phase was confirmed by flow cytometric analysis.
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影响因子：
20.3
作者：
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