氟尿嘧啶-花生凝集素结合物与LoVo细胞的结合特性研究  

Study on Binding Characteristics of 5-Fluorouracil-Peanut Agglutinin Conjugates to LoVo Cells

作　　者：蔡勤[1] 赵栋[1] 聂宇[1] 张志荣[1] 

机构地区：[1]四川大学靶向药物及传递系统重点实验室,成都610041

出　　处：《中国药学杂志》2008年第15期1153-1157,共5页Chinese Pharmaceutical Journal

基　　金：博士点基金资助项目(20050610086)

摘　　要：目的研究氟尿嘧啶-花生凝集素结合物与细胞的作用。方法采用一步法制备得到结合物。应用荧光显微镜定性观察结合物与细胞的结合。应用MTT法检测结合物的细胞毒作用。结果LoVo细胞与结合物呈浓度依赖性结合;但Chang细胞不结合结合物。结合物对癌细胞的细胞毒作用呈浓度依赖性和时间依赖性。结论结合物可选择性地与癌细胞结合,并保留抗癌活性。OBJECTIVE To investigate the interaction between cells and conjugates of 5-fluorouracil-peanut agglutinin （5-Fu- PNA）. METHODS The FITC-labeled conjugates and conjugates were prepared. The coloreetal cancer cell line LoVo and the normal human liver cell line Chang were incubated with the FITC-labeled conjugates at 4 %. The fluorescence microscope was used to observe the binding of the FITC-labeled conjugates to the cells. In order to investigate the eytotoxicity of the conjugates on LoVo cells at 37 %, MTT method was adopted. RESULTS LoVo cells binded with the FITC-labeled conjugates and the cell-associated fluorescence intensity was dose-dependent while Chang cells didnt bind with the FITC-labeled conjugutes. The conjugates killed LoVo cells in a dose-dependent and time-dependent manner as that of the free drug. Compared with the free drug, there was a time-delayed effect and a little weaker eytotoxie effect for the conjugates. CONCLUSION The results showed that the cytotoxicity of 5-Fu was maintained after conjugation with peanut agglutinin. The conjugates could selectively bind to the cancer cells. It suggested the binding be specific. The uptake of the conjugates by cells may use an active manner to increase its selectivity to target tissues and to reduce its side effect on healthy tissues. However, the potential of the conjugate as a targeting agent for colorectal cancer needs to be furlher investigated in vivo.

关 键 词：花生凝集素 氟尿嘧啶 结合物 

分 类 号：R965[医药卫生—药理学]