^(125)I-RC-160的标记及与NCI-H446细胞体外受体结合特性的研究  

The preparation of ^(125)I-RC-160 and its in vitro binding characteristics to the receptors of NCI-H446 cell line

作　　者：李富军[1] 汪静[1] 邓敬兰[1] 李焰 

机构地区：[1]第四军医大学西京医院,西安710032 [2]第四军医大学口腔医院,西安710032

出　　处：《核技术》2002年第5期321-326,共6页Nuclear Techniques

基　　金：国家自然科学基金资助 (39870 2 18)课题

摘　　要：为探索高比活度12 5I -生长抑素类似物 (RC - 160 )的制备及与小细胞肺癌 (SCLC)细胞株-NCI-H4 46体外受体结合特性。12 5I -RC - 160采用氯胺T法标记 ,C18反向色谱柱纯化 ,硅胶纸层析检测。12 5I-RC - 160与NCI -H4 46细胞进行体外结合实验、饱和结合实验和竞争结合实验。12 5I -RC - 160标记率为 5 4.34 % ,比活度 1.85TBq/ (mmol·L- 1) ,放射化学纯度 (RCP)为 92 % ;Scatchard作图提示 ,Kd 为 1.71× 10 - 10 mol/L ,Bmax为 1.0 6× 10 5个 /细胞。制备的12 5I -RC - 160达到体外受体配体结合分析的标准 ;12 5I-RC - 160与NCI -H4 46的结合具有温度时间依赖性、可饱和性、可逆性及特异 ;12 5I -RC - 160与NCI -H4 46细胞生长抑素受体的结合符合单位点系统。To investigate the preparation of 125 I- somatostatin analogy (RC-160) and its binding characteristics to NCI-H446 cell receptors. RC-160 was labeled with Na 125 I using chloramines-T method, then purified by C 18 reverse phase chromatography and examined by silica chromatographic paper. Time-binding correlation test, temperature-binding correlation test, saturable binding test and competition binding test between NCI-H446 cells and 125 I-RC-160 were carried out. The labeling rate of 125 I-RC-160 was 54.34%. The specific activity of 125 I-RC-160 was 1.85TBq/mmol·L -1 . The radiochemical purity was 92%. The value of K d and B max was 1.71×10 -10 mol/L and 1.06×10 5 site /cell respectively. The labeled 125 I-RC-160 could be used for receptor analysis and the iodination of RC-160 does not change its binding to somatostatin receptor. The results demonstrated that the binding of 125 I-RC-160 to NCI-H446 cell possessed the reversibility, specificity, saturability, and was time and temperature dependent. The NCI-H446 cell line expresses somatostatin receptors with high density and affinity. The binding is in accordance with single site system.

关 键 词：RC-160 标记 NCI-H446 细胞体外受体 结合特性 生长抑素 小细胞肺癌 碘125 受体介导核素治疗 放射性核素 

分 类 号：R734.2[医药卫生—肿瘤] R730.55[医药卫生—临床医学]