Synthesis and biological property evaluation of <sup>90</sup>Y radiolabeled glycosylated somatostatin

ZHAI Shizhen1 DU Jin1; 3 SHEN Yijia2 HU Chunlin2 HE Chuan2 ZHAO Lei1 1

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Synthesis and biological property evaluation of ⁹⁰Y radiolabeled glycosylated somatostatin

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- Synthesis and biological property evaluation of ⁹⁰Y radiolabeled glycosylated somatostatin
- NUCLEAR TECHNIQUES Issue 5, (2007)
- 作者机构：
  
  1. 北京大学基础医学院生物物理系
  2. 中国原子能科学研究院同位素研究所
  3. 北京大学基础医学院生物物理系,北京,100083
  4. 北京100083 中国原子能科学研究院同位素研究所北京102413 中国同位素公司北京,100045
- 作者简介：
- 基金信息：
  
  国家自然科学基金(30370421);教育部留学回国人员科研启动基金资助项目
- DOI：
  CLC： R817
- Published：01 May 2007
- 稿件说明：
移动端阅览
[1]翟士桢,杜进,沈亦佳,胡春林,何川,赵磊.糖基化生长抑素~(90)Y标记及体内外生物学评价[J].核技术,2007(05):454-458.

ZHAI Shizhen1 DU Jin1, 3 SHEN Yijia2 HU Chunlin2 HE Chuan2 ZHAO Lei1 1. Synthesis and biological property evaluation of ⁹⁰Y radiolabeled glycosylated somatostatin[J]. Nuclear techniques, 2007, (5): 454-458.
[1]翟士桢,杜进,沈亦佳,胡春林,何川,赵磊.糖基化生长抑素~(90)Y标记及体内外生物学评价[J].核技术,2007(05):454-458. DOI：

ZHAI Shizhen1 DU Jin1, 3 SHEN Yijia2 HU Chunlin2 HE Chuan2 ZHAO Lei1 1. Synthesis and biological property evaluation of ⁹⁰Y radiolabeled glycosylated somatostatin[J]. Nuclear techniques, 2007, (5): 454-458. DOI：

摘要

以天然生长抑素（Somatostatin

SMS）、葡聚糖-70(Dextran

)及双功能螯合剂2-甲基-6-对氨基苯基二乙三胺五乙酸（1B4M-DTPA）为原料

合成糖基化生长抑素SMS-Dx

-DTPA并进行90Y标记;以125I-奥曲肽(

125

I-Tyr

-Octreotide)为放射配基

进行受体竞争结合实验

测定SMS-Dx

-DTPA的IC

值;并用

Y-DTPA-Dx

-SMS进行正常大鼠体内分布和血浆清除实验。结果表明:配体化合物SMS-Dx

-DTPA保持了对生长抑素2型受体的高亲和力

其IC

值与SMS相近;

Y-DTPA-Dx

-SMS在正常大鼠体内血浆半衰期为6.39h

主要浓聚于肝、脾并经肾排泄

与葡聚糖的代谢途径基本一致

肾上腺、胰腺具有较高的放射性摄取

且24h内基本保持不变

Y-DTPA-Dx

-SMS对生长抑素受体阳性组织具有靶向性

有望成为一种新型生长抑素受体阳性肿瘤治疗剂。

Abstract

Natural somatostatin （SMS）

dextran-70 (Dx

) and a bifunctional chelator 2- methyl-6-（p-amidobenzyl） -diethylenetriaminepentaacetic acid （1B4M-DTPA） were used to synthesize a novel somatostatin-dextran-DTPA (SMS-Dx

-DTPA) conjugate and radiolabeled with

Y. An in vitro somatostatin receptor competition binding study was carried out by using

125

I-Tyr

-Octreotide as a radioligand to measure the IC

value of SMS-Dx

-DTPA. Bio- distribution and blood half-life of

Y-DTPA-Dx

-SMS were investigated in normal rats. The results show that SMS-Dx70-DTPA has a high receptor binding affinity to somatostatin receptor subtype 2

with the IC

value being in the same range as somatostatin. The blood half-life of

Y-DTPA-Dx

-SMS in normal rats was 6.39h post-injection. Digestion and excretion of

Y-DTPA-Dx

-SMS was mainly through the hepatobiliary and kidney systems. Increased uptake was seen in the adrenals and pancreas

and it kept almost constant during 24h. Therefore

Y-DTPA-Dx

-SMS has targeting properties towards somatostatin receptor positive organs and it may become a promising therapeutic agent candidate for somatostatin receptor positive tumors.

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Synthesis and biological property evaluation of 90Y radiolabeled glycosylated somatostatin

DOI：

摘要

Abstract

关键词

Keywords

references

Synthesis and biological property evaluation of ⁹⁰Y radiolabeled glycosylated somatostatin