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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 order to explore the method of 131I-labeled chlorotoxin BmK CT, the stability of the marker, the binding ability with cells and its distribution in glioma-bearing Wistar rats were studied. The BmK CT was cloned, expressed and purified, BmK CT was indirectly labeled by Bolton-Hunter method. The glioma-bearing Wistar rats were injected with 131I-BmKCT through the tail vein of the tail of the rats and then were sacrificed at different time points. The blood, major organs and tumors were taken and the% ID / g). The results showed that the labeling rate of 131I-BmK CT was 37.8 ± 8.9% and the radiochemical purity was more than 95%. The highest specific binding rate to rat C6 glioma cells was 39.62%. Within 24 hours after intravenous injection of 131I-BmK CT, the radioactive radioactivity of rats was rapidly cleared. The radioactivity mainly accumulated in the liver, lung and kidney, and mainly accumulated in the kidneys and cleared after 24 hours. The radioactivity of other tissues and organs decreased gradually with time. 131I-BmK CT imaging of tumor-bearing rats showed high uptake of tumor tissue and up to a maximum of 6.79 ± 0.29.131I-BmK CT (T / NT) ratio between tumor and contralateral normal tissue Specific binding of glioma cells, with better animal in vivo kinetic performance and tumor uptake, is expected to be used in the diagnosis and treatment of glioma, but requires a lot of research.