Sesquiterpene lactones from Carpesium abrotanoides L. and their activity in inducing protective autophagy
Sesquiterpene lactones from Carpesium abrotanoides L. and their activity in inducing protective autophagy
复制标题
Carpesium abrotanoides L. 的倍半萜内酯及其诱导保护性自噬的活性。
DOI：
10.1080/14786419.2021.1955881
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发表时间：
2021-07-15
影响因子：
2.2
通讯作者：
Li, Shun-Lin
中科院分区：
文献类型：
--
作者：
Yang, Bao-Jia;Wang, Juan;Li, Shun-Lin
从广西产的天名精（Carpesium abrotanoides L.）在综合光谱数据分析的基础上确定了它们的结构。筛选所有化合物的细胞毒活性，化合物6显示出对五种人癌细胞系（包括A549、HepG 2、HCT 116、MDA-MB-231和CNE 2）的最强活性（IC 50 2.73 - 7.21 μ M）。进一步研究化合物6。化合物6以剂量依赖性方式有效地诱导G2/M细胞周期停滞和ROS积累，这进一步导致癌细胞的凋亡。有趣的是，化合物1和6也可以激活保护性自噬，这是首次报道的倍半萜分离自Carpesium abrotanoides。此外，化合物1和6可分别诱导173.2%和163.7%的溶酶体生物合成。综上所述，铁名精中的倍半萜内酯类化合物具有诱导癌细胞凋亡和保护性自噬的作用，为进一步研究铁名精中的倍半萜内酯类化合物提供了一系列具有潜在临床应用价值的化合物。
Fourteen sesquiterpene lactones were isolated from the whole plant of Carpesium abrotanoides L. Their structures were determined on the basis of comprehensive spectroscopic data analysis. All compounds were screened for their cytotoxic activity, and compound 6 showed the strongest activity (IC50 2.73 - 7.21 mu M) against five human cancer cell lines, including A549, HepG2, HCT116, MDA-MB-231, and CNE2. Compound 6 was further investigated. Compound 6 effectively induced G2/M cell cycle arrest and ROS accumulation in a dose-dependent manner, which further led to apoptosis in cancer cells. Interestingly, compounds 1 and 6 could also activate protective autophagy, which was reported for the first time in sesquiterpene isolated from Carpesium abrotanoides. In addition, compounds 1 and 6 could induce lysosomal biogenesis by 173.2% and 163.7%, respectively. In sum, sesquiterpene lactones from Carpesium abrotanoides could induce apoptosis and protective autophagy in cancer cells, which provide a serial of compounds with potential clinical applications.