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

doi:10.7538/tws.2011.24.03.0146

同位素 ›› 2011, Vol. 24 ›› Issue (3): 146-150.DOI: 10.7538/tws.2011.24.03.0146

• 放射性药物和标记化合物 • 上一篇下一篇

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

邓新荣¹;杜进²;翟士桢¹;沈亦佳¹;罗志福¹

1. 中国原子能科学研究院同位素研究所，北京102413;2. 中国同位素公司，北京100045

收稿日期:1900-01-01 修回日期:1900-01-01 出版日期:2011-08-20 发布日期:2011-08-20

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

DENG Xin-rong¹;DU Jin²;ZHAI Shi-zhen¹;Shen Yi-jia¹;LUO Zhi-fu¹

1. Department of Isotope, China Institute of Atomic Energy, Beijing 102413, China；2. China Isotope Corporation, Beijing 100045， China

Received:1900-01-01 Revised:1900-01-01 Online:2011-08-20 Published:2011-08-20

摘要/Abstract

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。

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

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.

Key words: ¹⁷⁷Lu-DTPA-BIS-BIOTIN, avidin, dextran, Tyr3-octreotide, binding

邓新荣 ;杜进 ;翟士桢 ;沈亦佳 ;罗志福 . 奥曲肽-葡聚糖-亲和素的偶联及其与¹⁷⁷Lu-DTPA-BIS-BIOTIN的体外结合[J]. 同位素, 2011, 24(3): 146-150.

DENG Xin-rong;DU Jin;ZHAI Shi-zhen;Shen Yi-jia;LUO Zhi-fu. ¹⁷⁷Lu-DTPA-BIS-BIOTIN Binding of Octreotide-dextran-avidinated PANC-1 Cell Lines in Vitro[J]. Journal of Isotopes, 2011, 24(3): 146-150.

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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

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