Euphorkanlide A, a Highly Modified Ingenane Diterpenoid with a C-24 Appendage from Euphorbia kansuensis
Euphorkanlide A, a Highly Modified Ingenane Diterpenoid with a C-24 Appendage from Euphorbia kansuensis
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Euphorkanlide A，一种来自甘肃大戟的高度修饰的具有 C-24 附件的天然二萜类化合物
DOI：
10.1021/acs.orglett.9b01315
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发表时间：
2019
期刊：
影响因子：
5.2
通讯作者：
Yin Sheng
中科院分区：
文献类型：
--
作者：
Yan Xue Long;Sang Jun;Chen Shi Xin;Li Wei;Tang Gui Hua;Gan Li She;Yin Sheng
大戟内酯A(1)是从甘肃大戟根中分离得到的一种高度修饰的金刚烷二萜化合物，其C24附件形成了一个新的六氢异苯并呋喃稠合的19元大环双内酯环体系。通过大量的光谱分析和量子化学计算确定了其结构。化合物1对一组癌细胞株(IC50s<；5μM)显示显著的细胞毒性。机制研究表明，1可诱导耐药细胞株HCT-15/5-FU产生ROS，导致细胞周期停滞和细胞凋亡。
Euphorkanlide A (1), a highly modified ingenane diterpenoid with a C24appendage forming an additional hexahydroisobenzofuran-fused 19-membered macrocyclic bis-lactone ring system was isolated from the roots ofEuphorbia kansuensis. Its structure was determined by extensive spectroscopic analysis and quantum-chemical calculations. Compound1showed significant cytotoxicities against a panel of cancer cell lines (IC50s< 5 μM). Mechanistic study revealed that1could induce the generation of ROS, leading to cell cycle arrest and cell apoptosis in drug-resistant cancer cell line HCT-15/5-FU.