School of Pharmacy, Shanghai Jiao Tong University, Shanghai 200240, PR China.
Department of Pharmaceutical Sciences, School of Pharmacy, Texas Tech University Health Sciences Center, Amarillo, TX 79106, USA.
Eur J Med Chem. 2013 Oct;68:473-481. doi: 10.1016/j.ejmech.2013.07.018. Epub 2013 Aug 11.
Four new sesquiterpenoid dimers (lineariifolianoids E-H, 1-4), five new sesquiterpenoids (5-9), and seven known sesquiterpenoids (10-16) were isolated from the aerial parts of Inula lineariifolia Turcz. Their structures were determined by spectroscopic data analysis and X-ray diffraction studies. The compounds were then evaluated for their in vitro cytotoxicity against two human breast cancer cell lines (MCF-7 and MDA-MB-231) and one normal breast cell line (MCF-10A). Lineariifolianoid E (1) showed IC50 values of 1.56 μM and 2.75 μM against MCF-7 and MDA-MB-231, respectively. However, lineariifolianoid E demonstrated low toxicity to MCF-10A cells, which indicated a selective cytotoxicity for tumor cells. Further studies also presented that lineariifolianoid E had significant, dose-dependent effects on cell cycle progression and apoptosis in breast cancer cells.
从线叶旋覆花(Inula lineariifolia Turcz.)的地上部分分离得到四个新的倍半萜二聚体(线叶旋覆花二聚体 E-H,1-4)、五个新的倍半萜(5-9)和七个已知的倍半萜(10-16)。通过光谱数据分析和 X 射线衍射研究确定了它们的结构。然后评估了这些化合物对两种人乳腺癌细胞系(MCF-7 和 MDA-MB-231)和一种正常乳腺细胞系(MCF-10A)的体外细胞毒性。线叶旋覆花二聚体 E(1)对 MCF-7 和 MDA-MB-231 的 IC50 值分别为 1.56 μM 和 2.75 μM。然而,线叶旋覆花二聚体 E 对 MCF-10A 细胞的毒性较低,表明其对肿瘤细胞具有选择性细胞毒性。进一步的研究还表明,线叶旋覆花二聚体 E 对线粒体途径诱导的 MCF-7 细胞凋亡和细胞周期阻滞具有显著的、剂量依赖性的作用。