Department of Forensic Medicine, Hebei Key Laboratory of Forensic Medicine, Hebei Medical University, Shijiazhuang 050017, Hebei Province, China.
Z Naturforsch C J Biosci. 2012 Jul-Aug;67(7-8):375-80. doi: 10.1515/znc-2012-7-804.
Eight sesquiterpene lactones were isolated from the roots of Inula helenium and flowers of I. japonica. Among them, isoalantolactone (3) and santamarine (6) exhibited significant growth inhibitory activities against gynecologic cancer cell lines, while others weakly inhibited the growth of the cell lines (IC50 < or = 100 microM). In addition, 3 significantly inhibited the tumour growth of S180 tumour-bearing mice. Compounds 3 and 6 were not toxic to human embryonic lung fibroblast cells in vitro. These results demonstrated that the antitumour activities are closely related to the structures of the compounds, that is, an alpha-exomethylene-gamma-lactone ring is necessary for these activities.
从旋覆花属植物土木香根和旋覆花的花中分离得到 8 个倍半萜内酯。其中，异土木香内酯（3）和山金车二醇（6）对妇科癌细胞系表现出显著的生长抑制活性，而其他化合物则较弱地抑制细胞系的生长（IC50 < 或 = 100 microM）。此外，3 显著抑制 S180 荷瘤小鼠的肿瘤生长。化合物 3 和 6 在体外对人胚肺成纤维细胞无毒性。这些结果表明，抗肿瘤活性与化合物的结构密切相关，即α-外亚甲基-γ-内酯环是这些活性所必需的。
