Nuclear Science and Techniques

《核技术》(英文版) ISSN 1001-8042 CN 31-1559/TL     2019 Impact factor 1.556

Nuclear Science and Techniques ›› 2010, Vol. 21 ›› Issue (5): 302-305 doi: 10.13538/j.1001-8042/nst.21.302-305

• RADIOCHEMISTRY, RADIOPHARMACEUTICALS AND NUCLEAR MEDICIN • Previous Articles     Next Articles

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

SUN Xin CHU Taiwei WANG Xiangyun   

  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
PDF ShareIt Export Citation
SUN Xin, CHU Taiwei, WANG Xiangyun. Tumor angiogenesis imaging agent: biodistribution of 131I-YG5 and 131I-Boc-YG5.Nuclear Science and Techniques, 2010, 21(5): 302-305     doi: 10.13538/j.1001-8042/nst.21.302-305

Abstract:

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.

Key words: Radioiodination, Angiogenesis, Biodistribution, NGR, Deiodination, t-butyloxycarbonyl