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将茶氨酸为母体合成的茶氨酸衍生物茶氨酸溴香酰胺(TBrC)与茶氨酸作比较,评估茶氨酸溴香酰胺对人宫颈癌细胞体内外生长的抑制作用与其分子机制。应用MTT等方法检测不同浓度的TBrC对人宫颈癌细胞体外生长的影响,运用蛋白质印迹法检测解析这些人宫颈癌细胞中与凋亡和生长密切相关蛋白的表达和药物可能的作用靶点。此外,通过建立动物肿瘤模型,评价TBrC对荷瘤裸鼠人宫颈癌生长的抑制效果。实验结果显示,TBrC抑制人宫颈癌细胞体内外生长的活性超过其母体化合物茶氨酸多倍,对小鼠生长无明显毒性;TBrC作用的分子机制之一可能与抑制VEGFR1-Bcl-2/Bax信号传导通路相关。研究结果提示,TBrC具有广泛应用于临床治疗和(或)辅助治疗人宫颈癌和其他癌症的潜力。
The theanine malein derivative of theanine was synthesized as theanine bromine amide (TBrC) and theanine compared to evaluate the theanine bromine amide human cervical cancer cell growth inhibition in vitro and in vivo and its molecular mechanisms . The effects of different concentrations of TBrC on the growth of human cervical cancer cells were detected by MTT method. The expression of proteins closely related to apoptosis and growth in these human cervical cancer cells were analyzed by Western blotting and the possible target of the drug. In addition, we evaluated the inhibitory effect of TBrC on the growth of human cervical cancer in nude mice by establishing animal tumor models. The experimental results showed that TBrC could inhibit the growth of human cervical cancer cells in vitro and in vivo more than its parent compound theanine and had no obvious toxicity on the growth of mice. One of the molecular mechanisms of TBrC may be related to the inhibition of VEGFR1-Bcl-2 / Bax Signaling pathway related. The results suggest that TBrC has the potential to be widely used in clinical treatment and / or adjuvant treatment of cervical cancer and other cancers.