生长抑素-葡聚糖的99Tcm标记及体外结合分析
99Tcm Labeling and in Vitro Biding of Dextran-somatostatin conjugate
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摘要: 采用还原氨化方法,将天然生长抑素(SMS)与葡聚糖(Dx20)偶联,并以125I-奥曲肽(125I-Tyr3-Octreotide)为放射配基,进行受体竞争结合实验,测定了SMS-Dx50的IC50;以SnCl2为还原剂对SMS-Dx50进行99Tcm标记,并进行99Tcm- SMS-Dx50受体结合分析,考察其对生长抑素受体的亲合能力。结果表明:SMS-Dx50保持了对SMS 2型受体的高亲和力;其IC50与奥曲肽的IC50(0.79 nmol/L)相近,为5.95 nmol/L;99Tcm- SMS-Dx50标记率>85%, 经PD-10柱分离纯化,其放化纯度>98%;99Tcm- SMS-Dx50对生长抑素2型受体特异性结合为25%~40%,保持了较高的亲和力;SMS-Dx50适合于99Tcm标记,可用于生长抑素受体阳性肿瘤诊断的进一步研究Abstract: Natural somatostatin and dextran-20 are used to synthesis somatostatin-dextran (SMS-Dx20). The in vitro somatostatin receptor competition binding study of somatostatin-dextran is carried out by using rat brain cortex membranes (express somatostatin receptor type 2) and 125I-Tyr3-Octreotide as a radioligand. The somatostatin-dextran conjugate is then labelled with 99Tcm using SnCl2 as reduce agent and tested for its in vitro binding properties. The somatostatin-dextran conjugate shows high somatostatin receptor binding affinity, i.e. in the same nM range as the reference ligand Octreotide (IC50 ~ 5.95 nmol/L). The labeling efficiency is more than 85%. The specific binding of 99Tcm labeled somatostatin-dextran conjugate Is 30%-40%. The somatostatin-dextran conjugate is worthy of further investigation for 99Tcm radiolabeling with diagnostic posibilities for somatostatin receptor positive tumors