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倍半萜类化合物从土木香中对人乳腺癌细胞的选择性细胞毒性、细胞周期进程抑制和诱导凋亡。

Selective cytotoxicity, inhibition of cell cycle progression, and induction of apoptosis in human breast cancer cells by sesquiterpenoids from Inula lineariifolia Turcz.

机构信息

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.

出版信息

Eur J Med Chem. 2013 Oct;68:473-481. doi: 10.1016/j.ejmech.2013.07.018. Epub 2013 Aug 11.

Abstract

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.

摘要

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。

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