Tumor targeting efficacy of a novel PET radiotracer 18F-AlF-NOTA-PRGD2 in mice
- VernacularTitle:PET显像剂18F-AlF-NOTA-PRGD2的肿瘤靶向性
- Author:
Hubing WU
1
;
Quanshi WANG
;
Yanjiang HAN
;
Wenlan ZHOU
;
Hongsheng LI
;
Ying TIAN
;
Qiaoyu WANG
Author Information
1. 南方医科大学南方医院PET中心
- Keywords:
glioma;
U87MG;
positron emission tomography;
radiotracer;
receptor imaging;
18F-AlF-NOTA-PRGD2
- From:
Journal of Southern Medical University
2014;(1):51-55
- CountryChina
- Language:Chinese
-
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.
