诊疗一体化探针^64Cu-DOTA-TATE的制备、质量控制及分子影像  

Radio-synthesis,Quality Control and Micro-PET Imaging of ^(64)Cu-DOTA-TATE

作　　者：刘菲[1] 谢卿[1] 刘特立 徐晓霞 郭晓轶 李囡[1] 朱华[1] 杨志[1] LIU Fei;XIE Qing;LIU Teli;XU Xiaoxia;GUO Xiaoyi;LI Nan;ZHU Hua;YANG Zhi(Key Laboratory of Carcinogenesis and Translational Research （Ministry of Edncation/Beijing） , Department of Nuclear Medicine, Peking University Cancer Hospital ＆ Institute, Beijing 100142, China)

机构地区：[1]北京大学肿瘤医院暨北京市肿瘤防治研究所核医学科,恶性肿瘤发病机制及转化研究教育部重点实验室,北京100142

出　　处：《高等学校化学学报》2018年第4期695-700,共6页Chemical Journal of Chinese Universities

基　　金：北京市科技新星项目(批准号：Z171100001117020); 国家自然科学基金(批准号：81371592,81401467); 北京市自然科学基金(批准号：7162041); 北京市卫生局基金“215”学科骨干项目(批准号：2015-3-072)资助

摘　　要：采用放射性核素^(64)Cu标记生长抑素类似物DOTA-3-酪氨酰基-奥曲肽(DOTA-TATE),制备了生长抑素受体显像分子探针^(64)Cu-DOTA-TATE;分别测试了其在5%(体积分数)的人血清白蛋白(HSA)和0.9%(体积分数)生理盐水中的稳定性.将^(64)Cu-DOTA-TATE经尾静脉注射入荷胰腺癌细胞裸鼠体内,并分别于注射后1,4和10 h进行小动物正电子发射断层(Micro-PET)显像.结果表明,经固相萃取小柱(Sep-Pak)分离纯化后,^(64)Cu-DOTA-TATE的放射化学纯度>99%,且40 h内在5%HSA和0.9%生理盐水中有良好的稳定性.Micro-PET显像结果表明,随着时间延长,肿瘤区域对^(64)Cu-DOTA-TATE放射性摄取增加.^(64)Cu-DOTA-TATE有望成为较好的生长抑素类似物的PET显像剂.To investigate the potential of ^64Cu labeled DOTA-[Tyr3]-octreotate（ DOTA-TATE） molecular probe in detecting somatostatin receptor（ SSTR） positive tumors. The somatostatin analogue DOTA-TATE was radiolabeled with ^64Cu to prepare ^64Cu-DOTA-TATE. The stability of the probe was measured in 5%（ volume ratio） HSA and 0. 9%（ volume ratio） saline solutions. After purification,18. 5 MBq of ^64Cu-DOTA-TATE was injected intravenously to nude mice bearing human pancreatic cancer via tail vein,micro-PET images were taken after radiotracer injection 1 and 10 h. After purification with 80%（ volume ratio） ethanol, the radiochemical purity of ^64Cu-DOTA-TATE was over 99%,and could keep stable for 40 h in 5% HSA and0. 9% saline solutions. As shown in micro-PET imaging,tumor uptake was visualized after post injection 1 h,with the uptake increased after 10 h. ^64Cu-DOTA-TATE may be useful for imaging somatostatin receptorpositive tumors.

关 键 词：生长抑素 64Cu-DOTA-3-酪氨酰基-奥曲肽 质量控制 神经内分泌肿瘤 

分 类 号：O629.72[理学—有机化学] O615[理学—化学]