Tumor targeting efficacy of a novel PET radiotracer (1)8F-AlF-NOTA-PRGD2 in mice.
- Author:
Hubing WU
1
;
Quanshi WANG
;
Yanjiang HAN
;
Wenlan ZHOU
;
Hongsheng LI
;
Ying TIAN
;
Qiaoyu WANG
Author Information
- Publication Type:Journal Article
- MeSH: Animals; Cell Line, Tumor; Fluorine Radioisotopes; Glioblastoma; diagnostic imaging; Humans; Mice; Mice, Nude; Oligopeptides; Positron-Emission Tomography; methods; Radioactive Tracers
- From: Journal of Southern Medical University 2014;34(1):51-55
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVETo investigate the tumor targeting efficacy of (18)F-AlF-NOTA-PRGD2, a novel radiotracer of Arginine-glycine-aspartic acid (RGD) peptides.
METHODS(18)F-AlF-NOTA-PRGD2 was synthesized in one-step by conjugating NOTA-PRGD2 with (18)F-AlF at 100 degrees celsius;. The tumor targeting efficacy and in vivo biodistribution profile of (18)F-AlF-NOTA-PRGD2, 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.
RESULTSNOTA-PRGD2 was (18)F-fluorinated successfully in one-step with a yield of 17%-25% within 15-20 min. Radioactivity biodistribution study confirmed the tumor-targeting ability of (18)F-AlF-NOTA-PRGD2 in the tumor-bearing mice. At 1 and 2 h following injection, (18)F-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 (18)F-AlF-NOTA-PRGD2 in the mouse model and clearly displayed the tumor, but microPET/CT showed a much better image quality.
CONCLUSION(18)F-AlF-NOTA-PRGD2 prepared by one-step radiosynthesis can selectively target to the tumor, demonstrating its potential as a good radiotracer for tumor imaging.
