基于毛细管电泳酶微反应器的吉非替尼对表皮生长因子受体抑制率的测定  

The determination of gefitinib on epidermal growth factor receptor inhibition rate by capillary electrophoresis enzyme micro-reactor

作　　者：申刚义[1] 于婉婷[1] 张爱芹[2] 刘美蓉[3] 王宁[1] 

机构地区：[1]中央民族大学中国少数民族传统医学国家民委-教育部重点实验室,北京100081 [2]中央民族大学,生命与环境科学学院,北京100081 [3]中国科学院化学研究所,北京100090

出　　处：《分析试验室》2014年第4期392-394,共3页Chinese Journal of Analysis Laboratory

基　　金：国家自然科学基金项目(81001595)资助

摘　　要：采用共价键法将表皮生长因子受体固定在毛细管内壁,制备了一种毛细管电泳酶微反应器。结合毛细管电泳高效分离技术,以三磷酸腺苷为底物,吉非替尼为抑制剂,利用表皮生长因子受体酶微反应器在线测定了吉非替尼对皮生长因子受体的抑制性能。结果显示,吉非替尼可竞争性的抑制三磷酸腺苷与表皮生长因子受体的结合,从而影响三磷酸腺苷与表皮生长因子受体的结合量以及产物二磷酸腺苷的生成量。根据不同浓度吉非替尼下三磷酸腺苷峰面积的变化计算了吉非替尼对表皮生长因子受体的抑制率。同时绘制了抑制曲线,得到IC50值为32.44±0.82μmol/L。实验表明该酶微反应器可实际用于酪氨酸激酶抑制剂的抑制率的快速测定。An epidermal growth factor receptor enzyme micro-reactor was prepared using covalent binding method, and it employed firstly for studying the inhibition of Gefitinib to epidermal growth factor receptor based on capillary electrophoresis on line. The results showed that the Gefitinib could inhibit obviously the interaction between adenosine triphosphate and epidermal growth factor receptor. The inhibitor curve was drawn according to inhibition rates obtained from different concentrations of Gefitinib, and the IC50 value of Gefitinib was obtained with 32.44 ± 0.82 μmol/L. The technique is expected to be applied to enzyme inhibitor screening, enzyme kinetics, proteomics and related areas.

关 键 词：表皮生长因子受体 酶微反应器 毛细管电泳 EGFR 吉非替尼 抑制率 

分 类 号：O657.8[理学—分析化学]