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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。
OBJECTIVE: To study the binding properties of iodine [Tyr3] -octreotide (TOC) and 125I-HPNS-TOC to the small cell lung cancer cell line NCI-H446. Methods 125I-HPNS-TOC was prepared by Bolton-Hunter reagent and its receptor was analyzed by radioligand and somatostatin receptor (SSTR) positive cell NCI-H446. Results Linkage-labeled 125I-HPNS-TOC retained its original biological activity and had high affinity with SSTR. Conclusion The 125I-HPNS-TOC can be successfully prepared by using Bolton-Hunter reagent with high binding ability to SSTR. This experiment provides a preliminary study of 125I-HPNS-TOC in receptor-mediated tumor radionuclide therapy.