Tumor angiogenesis imaging agent:biodistribution of ^(131)I-YG5 and ^(131)I-Boc-YG5  

作　　者：SUN Xin CHU Taiwei WANG Xiangyun 

机构地区：[1]Beijing National Laboratory for Molecular Sciences, Radiochemistry and Radiation Chemistry Key Laboratory of Fundamental Science, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China

出　　处：《Nuclear Science and Techniques》2010年第5期302-305,共4页核技术（英文）

基　　金：Support by National Natural Science Foundation of China (No. 20771011 and 21071010);the Ministry of Science and Technology of China (No. 2006CB705700)

摘　　要：The cyclic peptide YG5 and the t-butyloxycarbonyl(Boc)-modified analog(Boc-YG5) were labeled with radioiodine.The radiochemical purity of 131I-YG5 or 131I-Boc-YG5 was almost 100% after purification by RP-HPLC.Biodistribution in BALB/C nude mice bearing MCF-7 tumor was measured.After t-butyloxycarbonyl(Boc)-modification,the 131I-Boc-YG5 was quite resistant to deiodination in vivo,resulting in negligible radioactivity accumulation in thyroid.The radiotracer clearance in tumor became faster,the absolute tumor uptake decreased for 131I-Boc-YG5,but the tumor-to-tissue uptake ratios increased.The uptake ratios of tumor to muscle,blood,heart,and lung at 1 h post injection reached 4.73,1.70,4.09 and 1.70,respectively.It is demonstrated that Boc-group is an effective prosthetic one to prevent deiodination in vivo and improve tumor imaging for radioiodinated NGR.The cyclic peptide YG5 and the t-butyloxycarbonyl（Boc）-modified analog（Boc-YG5） were labeled with radioiodine.The radiochemical purity of ^131I-YG5 or ^131I-Boc-YG5 was almost 100% after purification by RP-HPLC.Biodistribution in BALB/C nude mice bearing MCF-7 tumor was measured.After t-butyloxycarbonyl（Boc）-modification,the ^131I-Boc-YG5 was quite resistant to deiodination in vivo,resulting in negligible radioactivity accumulation in thyroid.The radiotracer clearance in tumor became faster,the absolute tumor uptake decreased for ^131I-Boc-YG5,but the tumor-to-tissue uptake ratios increased.The uptake ratios of tumor to muscle,blood,heart,and lung at 1 h post injection reached 4.73,1.70,4.09 and 1.70,respectively.It is demonstrated that Boc-group is an effective prosthetic one to prevent deiodination in vivo and improve tumor imaging for radioiodinated NGR.

关 键 词：放射性碘标记 肿瘤 生物分布 显像剂 反相高效液相色谱法 银 放射化学纯度 摄取率 

分 类 号：S859.84[农业科学—临床兽医学] Q51[农业科学—兽医学]