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目的探讨荷包牡丹碱对人肺腺癌细胞A549的增殖抑制作用并对其作用机制进行研究。方法 MTT比色法检测荷包牡丹碱在不同浓度及不同时间对人肺癌细胞A549的增殖抑制作用。利用TUNEL法探讨荷包牡丹碱诱导人肺腺癌细胞A549的凋亡效果;流式细胞术(FMC)测定荷包牡丹碱对A549肿瘤细胞周期的分布;比色法测定荷包牡丹碱对半胱天冬酶(caspase)-3蛋白活性的影响。结果荷包牡丹碱对人肺腺癌细胞A549增殖抑制作用随着药物浓度的升高和作用时间的延长而增强;荷包牡丹碱对A549肿瘤细胞具有明显的凋亡效应;荷包牡丹碱与A549肿瘤细胞作用后,发生S期阻滞(P<0.05);荷包牡丹碱促使caspase-3蛋白活化(P<0.05)。结论荷包牡丹碱能有效抑制人肺腺癌细胞A549的生长,使细胞周期阻滞在S期,进一步诱导其凋亡,并使caspase-3蛋白活化。caspase-3蛋白的激活可能在荷包牡丹碱诱导A549细胞凋亡过程中起重要作用。
Objective To investigate the inhibitory effect of bicuculline on the proliferation of human lung adenocarcinoma A549 cells and its mechanism of action. Methods MTT assay was used to detect the inhibitory effect of bicuculline on the proliferation of human lung cancer cell line A549 at different concentrations and different times. The apoptosis of human lung adenocarcinoma A549 cells induced by bicuculline was investigated by TUNEL method. The distribution of bicuculline-treated A549 tumor cells by flow cytometry (FCM) was determined by flow cytometry (FCM) Effect of caspase-3 protein activity. Results The inhibitory effect of bicuculline on the proliferation of human lung adenocarcinoma A549 cells was enhanced with the increase of drug concentration and prolongation of action time. Cinchonine had obvious apoptosis effect on A549 tumor cells. (P <0.05). Caspase-3 protein was activated by bicuculline (P <0.05). Conclusion bicuculline can effectively inhibit the growth of human lung adenocarcinoma cell A549, arrest cell cycle in S phase, further induce apoptosis and activate caspase-3 protein. Activation of caspase-3 protein may play an important role in the apoptosis of A549 cells induced by bicuculline.