^(131)I-BmK CT的制备及其在胶质瘤荷瘤大鼠体内分布与显像研究  

Preparation of ^(131)I-BmK CT and bio-distribution and imaging in glioma-bearing rats

作　　者：乔文礼[1] 赵晋华[1] 邵晓霞[2] 张志勇 刘兴峰 汪太松[1] 金文雅[1] 姚玉平[1] 

机构地区：[1]上海交通大学附属第一人民医院核医学科,上海200080 [2]同济大学蛋白质研究所,上海200092 [3]上海欣科医药有限公司,上海201108

出　　处：《核技术》2011年第3期213-216,共4页Nuclear Techniques

基　　金：国家自然科学基金项目(30770600);上海市科委国际科技合作基金项目(07SP07004)资助

摘　　要：为探索131I标记蝎氯毒素BmK CT的方法,研究标记物的稳定性、与细胞的结合能力及其在胶质瘤荷瘤Wistar大鼠体内的分布,通过克隆、表达、纯化得到多肽BmK CT,并采用Bolton-Hunter法间接标记BmK CT。胶质瘤荷瘤Wistar大鼠鼠尾静脉注射131I-BmKCT后于不同时间显像,并于不同时间处死,取血液、主要脏器及肿瘤,测定每克组织百分注射剂量率(%ID/g)。结果显示,131I-BmK CT的标记率为37.8±8.9%,放化纯>95%,其与大鼠C6脑胶质瘤细胞的最高特异性结合率为39.62%。静脉注射131I-BmK CT后24h内,大鼠血液放射性清除迅速,放射性主要聚集在肝脏、肺脏、肾脏,24h后主要积聚在肾脏并经其清除,其他组织器官的放射性随时间逐渐降低。131I-BmK CT胶质瘤荷瘤大鼠显像示肿瘤组织摄取高,肿瘤与对侧正常组织放射性计数比值(T/NT)最高可达6.79±0.29。131I-BmK CT能与C6大鼠脑胶质瘤细胞特异性结合,具有较理想的动物体内动力学表现和肿瘤摄取,有望用于脑胶质瘤的诊断和治疗,但需要进行大量研究。In this work, we explored the method of radiolabeling scorpion toxin peptide BmK CT, and investigated the stability, the ability of cell conjugation of ^1^3^1I-BmK CT, and its distribution and imaging in glioma-bearing Wistar rats. After cloning, expression, and purification, BmK CT was labeled with ^1^3^1I by indirect labeling （Bolton- Hunter method）. ^1^3^1I-BmK CT was injected into the tail vein of glioma-bearing rats, and imaged at 1, 4, 8, 24 and 48 h. The rats were sacrificed by cervical dislocation, and tissue samples were studied. ^1^3^1I-BmK CT was successfully prepared with the overall yield of 37.8 ± 8.9%. The radiochemical purity was more than 95%. The specific binding efficiency of ^1^3^1I-BmK CT with C6 glioma cell was 39.62%. In the first 24 h after injection, the bio-distribution in rats showed rapid blood clearance. Most of the radioactivity was observed in liver, lung and kidney. After 24 h, the bio-distribution showed renal clearance, especially at the peak time of accumulation, when the tumor could be viewed clearly. The largest uptake ratio of tumor to non-tumor （background） （T/NT） at 4 h was 6.79 ± 0.29. In conclusion, ^1^3^1I-BmK CT can be prepared and specifically conjugate with C6 glioma cell. Good bio-distribution was observed in glioma-bearing rats. Nevertheless, great deal of research work needed to be done before clinical application of the medicin.

关 键 词：BMK CT 同位素标记 大鼠 生物分布 

分 类 号：R730.44[医药卫生—肿瘤]