125I-HPNS-TOC的制备及其结合特性分析

目的研究联接标记法制备碘Tyr3]-octreotide(TOC),以及125I-HPNS-TOC与小细胞肺癌株NCI-H446的受体结合特性。方法以Bolton-Hunter试剂为联接剂,制备125I-HPNS-TOC,并以其为放射性配基,与生长抑素受体(somatostatinreceptor,SSTR)阳性细胞NCI-H446进行受体分析。结果联接标记法制备的125I-HPNS-TOC保持原有的生物活性,与SSTR结合具有高亲和力。结论用Bolton-Hunter试剂可成功制备125I-HPNS-TOC,与SSTR结合力高。本实验为125I-HPNS-TOC在受体介导的肿瘤放射性核素治疗提供了前期研究。

Synthesis of 125I-HPNS-TOC and Analyses on Its Binding Characteristic

Objective To preparing iodine labeled Tyr3]-octreotide (TOC) with conjugation labeling, and assessing the characteristic of ~ 125 I-HPNS-TOC binding to the receptors within NCI-H446 cell lines. Methods ~ 125 I-HPNS-TOC, labeled with Bolton-Hunter reagent, were used as a radioligand to analyze the binding characteristic to somatostatin receptors (SSTR) on positive NCI-H446 cell lines. Results ~ 125 I-HPNS-TOC, labeled with conjugation labeling, keeps its own characteristic, and has high affinity bound to SSTR. Conclusions ~ 125 I-HPNS-TOC can be succeed preparing with Bolton-Hunter reagents, and has high affinity to SSTR. Our experiment provides an initial evidence for the using of ~ 125 I-HPNS-TOC in the radionuclide therapy of SSTR positive tumors mediated by receptor.