茶氨酸和其衍生物茶氨酸氯香酰胺对高转移的人乳腺癌细胞生长的抑制作用  

Inhibitory effects of theanine and TClC on the growth of human breast cancer cells

作　　者：吴菲[1] 田绘绘 季德鑫[1] 张华荣[1] 刘真真[1] 朱荣芹 刘昆[1] 姚建文[1] 张国营[1] 

机构地区：[1]烟台大学药学院分子药理学实验室,烟台264005

出　　处：《安徽农业大学学报》2014年第6期911-916,共6页Journal of Anhui Agricultural University

基　　金：国家科技部十二五"863"项目(2012AA020206);山东省科技攻关项目(2009GG10002087);山东省自然科学基金项目(ZR2012HM016)共同资助

摘　　要：旨在评估茶氨酸(T)和本实验室合成的新颖的茶氨酸衍生物-茶氨酸氯香酰胺(TClC)对高转移的人乳腺癌MDA-MB-231细胞生长的抑制作用,并对其作用的机制进行初步探究。采用MTT法检测不同浓度的T和TClC对MDA-MB-231细胞体外生长的影响,采用Western blotting对MDA-MB-231细胞中与癌细胞凋亡相关蛋白的表达以及药物作用可能的分子靶点进行检测。结果显示,随着浓度的增高,T和TClC对人乳腺癌MDA-MB-231细胞体外生长的抑制作用逐渐增强,TClC的抑制作用要明显强于T;T和TClC均能够下调抗凋亡蛋白Bcl-2的表达水平,同时上调促凋亡蛋白Bax的表达水平,使Bcl-2/Bax比率减少。此外,T和TClC均能抑制血管内皮生长因子受体VEGFR1和核转录因子NF-κB的表达,而TClC的抑制作用要明显强于T。T和TClC对这些蛋白水平的调节作用可能是抑制MDA-MB-231细胞生长的重要机制之一。这些结果表明,T和TClC对治疗高转移的人乳腺癌可能具有广阔的应用前景。This study was to assess the inhibitory effects of theanine （T） and TC1C （a synthesized novel theanine derivative） on the growth of highly-metastasis human breast MDA-MB-231 cells and explore the mecha- nisms of such an inhibition. The MTT assay was used to evaluate the effects of different concentrations of T and TC1C on the grown of in vitro MDA-MB-231 cells. Western blot analysis was employed to detect the expressions of apoptosis-related proteins and the possible targets of drug actions in the MDA-MB-231 cells. The experimental results showed that the inhibitory effects of T and TC1C on the growth of MDA-MB-231 cells are gradually en- hanced with the increase of the concentrations. TC1C showed a much stronger inhibition of cell growth than T. T. TCIC down-regulated the expression level of antiapoptotic Bcl-2 protein and up-regulated the expressions of proapoptotic Bax protein, leading to the reduction of Bcl-2/Bax ratio. In addition, T and TC1C reduced the protein level of NF-r,B and VEGFR1. TC1C exhibited much stronger effects on regulating these proteins than T. The ex- pression regulation of these proteins by TC1C and T might be one of the important mechanisms of the cell growth suppression. All these findings suggested that T and TC1C may have potential to the treatment of highly-metastasis human breast cancer.

关 键 词：茶氨酸 茶氨酸氯香酰胺 高转移人乳腺癌 体外抑制 

分 类 号：S571.1[农业科学—茶叶生产加工]