紫杉醇-抗HER2MAb偶联物体外抗肿瘤活性的研究

The research on anti-tumor effect of paclitaxel-HER2 monoclonal antibody conjugate in vitro

目的研究紫杉醇(Paclitaxel,TAX)与抗HER2(Human epidermal growth factor receptor2,表皮生长因子受体2)单克隆抗体(MAb)偶联物(TAX-抗HER2MAb)体外抗肿瘤作用。方法实验细胞为MCF-7乳癌细胞,MTT法检测细胞增殖抑制作用,进行统计学分析;FCM检测细胞凋亡率;琼脂糖凝胶电泳分析凋亡细胞基因组DNA;Western-blot检测细胞HER2蛋白表达水平。结果在相同药物浓度下偶联物对肿瘤细胞抑制率明显高于TAX,具有统计学意义(P<0.05);半数抑制率药物浓度(IC50)相差20%,具有统计学意义(P<0.05);FCM和琼脂糖凝胶电泳DNA检测分析,偶联物作用的细胞凋亡效果明显高于TAX,Western-blot检测出偶联物作用的肿瘤细胞HER2蛋白表达量明显降低。结论 TAX-抗HER2MAb偶联物体外抗肿瘤作用明显高于TAX。

Objective To investigate the antitumours effect of the Paclitaxel and the HER2（Human epidermal growth factor receptor2）monoclonal antibody conjugates in vitro.Methods using MTT method to detect the depressant effect of MCF-7 cell multiplication and analyze with principle of statistics;using FC method to detect the rate of MCF-7 cell apoptosis;using agarose gel electrophoresis to analyze DNA of MCF-7 cell apoptosis;using Western-blot to detect the expression of the protein of HER2.Results in the same drug level,the depressant effect of the conjugate group was more than the TAX group（P0.05）.the IC50 of the conjugate group is 20% lower than the TAX group（P0.05）.using FCM and agarose Gel Electrophoresis to analyze cell DNA,the effect of the apoptosis in conjugate groups are apparently better than TAX groups,to compare with other groups,the conjugate groups have lower HER2 protein expression to the tumor cell.Conclusion the antitumours effect of TAX-HER2 monoclonal antibody conjugate group is higher than TAX group in vitro.