Tumor targeting efficacy of a novel PET radiotracer 18F-AlF-NOTA-PRGD2 in mice
WU Hubing
WANG Quanshi
HAN Yanjiang
ZHOU Wenlan
LI Hongsheng
TIAN Ying
WANG Qiaoyu
Abstract：Objective To investigate the tumor targeting efficacy of 18F-AlF-NOTA-PRGD2, a novel radiotracer of Arginine-glycine-aspartic acid (RGD) peptides. Methods 18F-AlF-NOTA-PRGD2 was synthesized in one-step by conjugating NOTA-RGD2 with 18F-AlF at 100℃. The tumor targeting efficacy and in vivo biodistribution profile of 18F-AlF-NOTA-RGD2, following intravenous injection via the tail vein, were evaluated in a nude mouse model bearing subcutaneous U87MG glioblastoma xenograft by radioactivity biodistribution assessment, PET/CT and microPET/CT. Results NOTA-RGD2 was 18F-fluorinated successfully in one-step with a yield of 17%-25%within 15-20 min. Radioactivity biodistribution study confirmed the tumor-targeting ability of 18F-AlF-NOTA-PRGD2 in the tumor-bearing mice. At 1 and 2 h following injection, 18F-AlF-NOTA-PRGD2 uptake in the tumor reached 4.14 ± 1.44 and 2.80 ± 1.18%ID/g (t=1.910, P=0.070) with tumor/brain ratios of 2.95 ± 0.61 and 5.21 ± 2.62, respectively (t=-1.686, P=0.167). Both PET/CT and microPET/CT were capable of showing the radioactivity biodistribution of 18F-AlF-NOTA-PRGD2 in the mouse model and clearly displayed the tumor, but microPET/CT showed a much better image quality. Conclusion 18F- AlF- NOTA- PRGD2 prepared by one- step radiosynthesis can selectively target to the tumor, demonstrating its potential as a good radiotracer for tumor imaging.
Keywords：gliomaU87MGpositron emission tomographyradiotracerreceptor imaging18F-AlF-NOTA-PRGD2
Publication Date：2014-01-01
Online Publishing Date：2025-08-15(First online date of this platform, not the publication date of the document)
Pages：5( 51-55 )