以L-茶氨酸作对照,评估本实验室合成的新颖的茶氨酸衍生物-茶氨酸溴香酰胺(TBrC)对人肝癌HepG2细胞系体内外生长的抑制作用,并初步探究其作用的分子机制。采用MTT法检测不同浓度的TBrC对HepG2细胞体外生长的影响,应用蛋白质印迹法检测解析HepG2细胞中与癌细胞凋亡和生长密切相关蛋白的表达和药物可能作用的分子靶点。此外,建立动物肿瘤模型,与对照组茶氨酸和临床常用抗癌药物五氟尿嘧啶组相比较,评价TBrC对荷瘤裸鼠人肝癌HepG2肿瘤生长的抑制效果。实验结果显示,TBrC抑制人肝癌细胞体内外生长的活性超过其母体化合物茶氨酸分别为3倍和4倍以上,对小鼠生长无明显毒性。TBrC比茶氨酸更显著地抑制肝癌细胞生长因子受体c-Met和抗凋亡的Bcl-2等蛋白的表达;此外,TBrC大大上调促进凋亡的Bax蛋白的表达。TBrC抑制c-Met信号传导通路,下调Bcl-2/Bax蛋白比率可能是其作用的分子机制之一。这些结果提示,TBrC具有广泛应用于临床治疗和(或)辅助治疗人肝癌和其他癌症的潜力。 L-Theanine was used as a control to evaluate the inhibitory effect of TBRC, a novel theanine derivatives synthesized in our laboratory, on the growth of HepG2 cells in vitro and in vivo Molecular mechanism. The effects of different concentrations of TBrC on the growth of HepG2 cells were detected by MTT assay. The molecular targets of HepG2 cells which were closely related to the apoptosis and growth of HepG2 cells and the potential role of drugs were analyzed by Western blotting. In addition, animal models of cancer were established to evaluate the inhibitory effect of TBrC on HepG2 tumor growth in nude mice bearing nude mice compared with the control group, theanine and the commonly used anticancer drug pentafluorouracil group. The results showed that TBrC inhibited the growth of human hepatocellular carcinoma cells in vitro and in vivo activity than its parent compound theanine were 3 times and 4 times, no significant toxicity on the growth of mice. TBrC inhibited the expression of hepatocellular carcinoma cell growth factor receptor c-Met and anti-apoptotic Bcl-2 more significantly than theanine. In addition, TBrC significantly up-regulated the expression of Bax protein that promotes apoptosis. TBrC inhibits c-Met signaling pathway and down-regulation of Bcl-2 / Bax protein ratio may be one of its molecular mechanisms. These results suggest that TBrC has the potential to be widely used in clinical treatment and / or adjuvant treatment of liver cancer and other cancers.