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目的评估化合物1-[4’-((3R,5R)-金刚烷基)苯基)]正丁胺盐酸盐(T44)的体外抗肿瘤活性,并初步探索可能的分子机制,为这种化合物的综合应用提供实验依据。方法四甲基偶氮唑蓝比色法检测T44对细胞的体外生长抑制作用;细胞形态观察法研究T44对细胞形态的影响;流式细胞仪法检测T44作用下肿瘤细胞周期和凋亡率的变化;蛋白印迹法检测T44对不同周期蛋白表达的影响;细胞划痕实验检测T44对肿瘤细胞迁移能力的影响。结果 T44对检测的11株肿瘤细胞的增殖均有抑制效果,对正常细胞人胚肺成纤维细胞也具有一定的增殖抑制作用,半数抑制浓度值为(16.58±3.49)μmol/L,高于受测的大部分肿瘤细胞;T44能导致肿瘤细胞凋亡和周期阻滞;T44能影响周期蛋白的表达并能降低HCT116细胞的迁移能力。结论 T44主要通过促进细胞凋亡来发挥抗肿瘤作用。
AIM To evaluate the antitumor activity of 1 - [4 ’- ((3R, 5R) -adamantyl) phenyl)] n-butylamine hydrochloride (T44) in vitro and to explore the possible molecular mechanisms for this The comprehensive application of compounds provides experimental evidence. Methods MTT colorimetric assay was used to detect the effect of T44 on cell growth in vitro. The cell morphology was used to study the effect of T44 on cell morphology. Flow cytometry was used to detect the cell cycle and apoptosis rate of T44 cells The protein expression of T44 was detected by Western blotting. The cell scratch assay was used to detect the effect of T44 on the migration of tumor cells. Results T44 had inhibitory effect on the proliferation of 11 tumor cell lines and also had some inhibitory effects on normal human embryonic lung fibroblasts. The median inhibitory concentration (TCD) was (16.58 ± 3.49) μmol / L, which was higher than that of T44 can lead to tumor cell apoptosis and cycle arrest; T44 can affect the expression of cyclin and reduce the migration ability of HCT116 cells. Conclusion T44 exerts anti-tumor effect mainly through promoting apoptosis.