地胆草倍半萜内酯化合物体外抗肿瘤作用的研究

The Antitumor Effects in vitro of Sesquiterpene Lactones from Elephantopus scaber

采用四甲基偶氮唑盐比色法和琼脂糖凝胶电泳法等研究地胆草倍半萜内酯化合物scabertopin（1）和isodeoxyelephantopin（2）在体外对SMMC-7721、Hela和Caco-2三种肿瘤细胞增殖的影响。发现这两个化合物在1～100 μM浓度内对三种肿瘤细胞增殖有显著的抑制作用，且呈一定剂量依赖关系。二者抑制SMMC-7721细胞增殖的IC50值分别为29.27和9.54 μM；抑制Hela细胞增殖的IC50值分别为22.19和25.39 μM；抑制Caco-2细胞增殖的IC50值分别为35.99和25.76 μM。时效性实验还显示2对Hela细胞增殖的抑制作用呈时间依赖关系。2浓度 100 μM作用Hela细胞48 h琼脂糖凝胶电泳显示明显的细胞凋亡“梯状”条带（DNA ladder），提示isodeoxyelephantopin抑制Hela细胞作用是通过诱导其凋亡。

The antitumor effects of sesquiterpene lactones scabertopin and isodexyelephantopin from the whole plant of Elephantopus scaber were studied in vitro on SMMC-7721, Hela and Caco-2 cancer cell lines. In MTr assay, scabertopin and isodexyelephantopin at the dose of 1-100 μM markedly inhibited the growth of three cancer cell lines in dose-dependent manner. The IC50 value of scabertopin and isodexyelephantopin on SMMC-7721 cells after 48 h of treatment were 29.27 and 9.54 μM,respectively,with their IC50 value on Hela cells of 22.19 and 25.39 μM and on Caco-2 cells of 35.99 and 25.76 μM. The time-effect experiment also showed that isodexyelephantopin inhibited the growth of Hela cells in time-dependent manner. DNA agarose gel electrophoresis of Hela cells revealed obvious nuclear fragmentation （DNA ladder） treated with isodexyelephantopin for 48 h, which suggested the compound could induce the apoptosis of Hela cell.