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目的探讨松萝Usnea diffracta中功效化合物赤星衣酸甲酯的体外抗癌活性及其作用机制。方法采用MTT法检测不同质量浓度的赤星衣酸甲酯对宣威肺癌XWLC-05细胞、肝癌HepG2细胞、乳腺癌MCF-7细胞的体外抗癌活性;以流式细胞技术分析赤星衣酸甲酯对HepG2细胞周期的调节作用;通过基因芯片技术分析赤星衣酸甲酯对MCF-7细胞基因表达的影响。结果赤星衣酸甲酯能够显著抑制XWLC-05、HepG2、MCF-7细胞的增殖,其体外抗癌作用具有明显的量效关系,对3株癌细胞的半数抑制浓度(IC_(50))分别为8.818、11.905、13.328μg/mL。赤星衣酸甲酯主要阻滞HepG2细胞于G_0/G_1期。基因芯片分析得到MCF-7细胞差异倍数大于1.5的mRNA有2 394个,其中1 605个下调,789个上调。结论赤星衣酸甲酯为首次从松萝中分离得到,且具有较强的抗癌活性,其作用机制可能与调节细胞周期和蛋白激酶信号通路有关。
Objective To investigate the in vitro antitumor activity of the active compound sodium takylate in Usnea diffracta and its mechanism. Methods MTT assay was used to determine the antitumor activity of different concentrations of methyl xylate in XWLC-05 cells, HepG2 cells and MCF-7 cells. X-ray fluorescence spectrometry (FCM) On the regulation of HepG2 cell cycle; gene chip analysis of the impact of methyl acid methylate on MCF-7 cells gene expression. Results Methyldc acid methyl ester could significantly inhibit the proliferation of XWLC-05, HepG2 and MCF-7 cells. The anti-cancer activity in vitro had a dose-effect relationship. The half inhibitory concentration (IC 50) Was 8.818, 11.905, 13.328 μg / mL. Methyldithronate mainly blocks HepG2 cells in G_0 / G_1 phase. There were 2 394 mRNAs with a multiple of 1.5 in MCF-7 cells by gene chip analysis, of which 1 605 were down-regulated and 789 were up-regulated. Conclusion It is the first time that methyl crotonate is isolated from pineapple and has a strong anticancer activity. Its mechanism may be related to the regulation of cell cycle and protein kinase signaling pathway.