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奥曲肽-葡聚糖-亲和素的偶联及其与177Lu-DTPA-BIS-BIOTIN的体外结合

177Lu-DTPA-BIS-BIOTIN Binding of Octreotide-dextran-avidinated PANC-1 Cell Lines in Vitro

    摘要
  • 摘要: 以葡聚糖为载体，奥曲肽为导向分子合成了生长抑素配体化合物奥曲肽-葡聚糖-亲和素（Tyr3-octreotide-dxtran 40-avidin，TOC-Dx40-Av）；在体外模拟肿瘤预定位二步法以177Lu-DTPA-BIS-BIOTIN对TOCDx40-Av培养的PANC-1细胞的结合特性进行了研究。将长满人源胰腺癌细胞PANC1的24孔板置于含有TOC-Dx40-Av的缓冲液中培养，2 h后洗去上清液，再用含不同浓度177Lu-DTPA-BIS-BIOTIN（177Lu-DTPA-BIS-BIOTIN的摩尔质量范围为48.8～391 pmol）的缓冲液继续培养细胞，使177Lu-DTPA-BIS-BIOTIN与细胞上的亲和素结合，测定细胞上结合的放射性计数，考察TOC-Dx40-Av与177Lu-DTPA-BIS-BIOTIN的结合特性以评价合成的大分子亲和素连接物的活性。实验结果显示，奥曲肽葡聚糖亲和素的化学纯度>99%，其中亲和素的含量为6.46 g/L。体外细胞结合实验结果表明，177Lu-DTPA-BIS-BIOTIN能快速与细胞上连接的亲和素结合，生物素与亲和素的摩尔比约为1∶1达到平衡。

     

    Abstract: Tyr3-octreotide, dextran-40 and avidin were used to prepare octreotide-dextran-avidin (TOC-Dx40-Av). DTPA-BIS-BIOTIN was labelled with 177Lu. The in vitro somatostatin receptor binding study was carried out by pretargeted method using TOC-Dx40-Av and 177Lu-DTPA-BIS-BIOTIN. The 24 well cell culture plates were prepared with PANC-1 cell monolayer and then incubated with TOC-Dx40-Av. After two washed with PBS, the cells were incubated with different concentration of 177Lu-DTPA-BIS-BIOTIN(48.8～391 pmol).Cells uptake was evaluated with γ counter. The results showed that the chemical purity of TOC-Dx40-Av was over 99%. The results also showed that TOC-Dx40-Av remained high receptor binding affinity to somatostatin receptor which indicated that TOC-Dx40-Av could bind to 177Lu-DTPA-BIS-BIOTIN with the molar ratio of 1∶1 on the cell surface.

     

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