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

Selective cytotoxicity, inhibition of cell cycle progression, and induction of apoptosis in human breast cancer cells by sesquiterpenoids from Inula lineariifolia Turcz.
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DOI:
10.1016/j.ejmech.2013.07.018
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发表时间:
2013-10
影响因子:
6.7
通讯作者:
Zhang R
Zhang R
中科院分区:
医学1区
文献类型:
--
作者:
Qin JJ;Jin HZ;Huang Y;Zhang SD;Shan L;Voruganti S;Nag S;Wang W;Zhang WD;Zhang R

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从旋覆花地上部分分离得到4个新的倍半萜二聚体,5个新的倍半萜(5-9)和7个已知的倍半萜(10-16)。通过光谱分析和X-射线衍射法确定了它们的结构。然后评价了这些化合物对两个人乳腺癌细胞系(MCF-7和MDA-MB-231)和一个正常乳腺细胞系(MCF-10A)的体外细胞毒性。其IC50值分别为1.5 6μM和2.75μM,对MCF7和MDAMB 2 31的IC50值分别为2.75和1.5 6。而线叶菊酯E对MCF-10A细胞的毒性较低,对肿瘤细胞具有选择性杀伤作用。进一步的研究还表明,线叶油烷类化合物E对乳腺癌细胞的细胞周期进程和凋亡有显著的剂量依赖性影响。
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.