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同位素  2011 

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

, PP. 146-150

Keywords: 177Lu-DTPA-BIS-BIOTIN,亲和素,葡聚糖,奥曲肽,偶联

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Abstract:

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-dxtran40-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,2h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48.8~391pmol)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6.46g/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。

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