胰岛素-5-氟尿嘧啶偶联物在体外的细胞毒性和细胞亲和性  

Cytotoxicity and cellular affinity of insulin-5-fluorouracil conjugate in vitro

作　　者：黄娟[1] 王建伟[1] 张志荣[1] 

机构地区：[1]四川大学靶向药物及传递系统教育部重点实验室,四川成都610041

出　　处：《华西药学杂志》2007年第3期245-247,共3页West China Journal of Pharmaceutical Sciences

基　　金：国家自然科学基金资助项目(批准号:30430770)

摘　　要：目的研究胰岛素-5-氟尿嘧啶偶联物(insulin-5-Fu)在体外的细胞毒性和细胞亲和性。方法通过MTT比色法和荧光标记成像来检测insulin-5-Fu对正常肝细胞和肝癌细胞的作用效应。结果偶联物在体外能够与肝癌细胞迅速地特异性结合;在中、低浓度下对肝癌细胞具有与原药相近的细胞毒性,对于正常细胞,其初期毒性较低;在高浓度下对正常细胞和肿瘤细胞的毒性急剧增加。结论以胰岛素为靶向载体的偶联物能够靶向肿瘤细胞,在中、低浓度范围内能够达到与原药相近的抑瘤效果,对正常细胞的毒性表现出时间延迟现象,高浓度时具有一定的细胞毒性。OBJECTIVE To study the cytotoxicity and cellular affinity of insulin - 5 - fluorouracil conjugate in vitro. METHODS Examination was conducted on normal liver cells and hepatocarcinoma cells using MTT assay and fluorescence imaging of FITC labelled conjugate. RESULTS This conjugate could rapidly and specifically bind to hepatocarcinoma cells. It had similar cytotoxicity as 5 - Fu on hepatocarcinoma cells under middle or low concentration, and lower cell toxicity on normal liver cells in the initial stage, while at high concentration the cytotoxicity increased rapidly on both hepatocarcinoma cells and normal liver cells. CONCLUSION This conjugate could target hepatocarcinoma cells with similar anti - tumor effect as 5 - Fu on hepatocarcinoma cells under middle or low concentration. And it also shows the ＂delayed cytotoxicity effcts＂ on normal liver cells. Higher cytotoxicity on both hepatocarcinoma cells and normal liver cells could be oloserved at the high concentration.

关 键 词：胰岛素-5-氟尿嘧啶偶联物 细胞毒性 细胞亲和性 

分 类 号：R965[医药卫生—药理学]