Radiosynthesis and preliminary biological evaluation of N-(2-[18F]fluoropropionyl)-L-glutamine as a PET tracer for tumor imaging
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Caihua Tang1,2, Ganghua Tang1, Siyuan Gao1, Shaoyu Liu1, Fuhua Wen1, Baoguo Yao1 and Dahong Nie1
1 PET-CT Center, Department of Nuclear Medicine, The First Affiliated Hospital, Sun Yat-Sen University, Guangzhou, P.R. China
2 Department of Nuclear Medicine, The Fifth Affiliated Hospital, Sun Yat-Sen University, Zhuhai, P.R. China
Ganghua Tang, email:
Dahong Nie, email:
Keywords: [18F]FPGLN; glutamine; positron emission tomography; biologic evaluation; tumor imaging
Received: December 22, 2015 Accepted: April 16, 2016 Published: May 03, 2016
In this study, radiosynthesis and biological evaluation of a new [18F]labeled glutamine analogue, N-(2-[18F]fluoropropionyl)-L-glutamine ([18F]FPGLN) for tumor PET imaging are performed. [18F]FPGLN was synthesized via a two-step reaction sequence from 4-nitrophenyl-2-[18F]fluoropropionate ([18F]NFP) with a decay-corrected yield of 30 ± 5% (n=10) and a specific activity of 48 ± 10 GBq/μmol after 125 ± 5 min of radiosynthesis. The biodistribution of [18F]FPGLN was determined in normal Kunming mice and high uptake of [18F]FPGLN was observed within the kidneys and quickly excreted through the urinary bladder. In vitro cell experiments showed that [18F]FPGLN was primarily transported by Na+-dependent system XAG- and was not incorporated into proteins. [18F]FPGLN displayed better stability in vitro than that in vivo. PET/CT studies revealed that intense accumulation of [18F]FPGLN were shown in human SPC-A-1 lung adenocarcinoma and PC-3 prostate cancer xenografts. The results support that [18F]FPGLN seems to be a possible PET tracer for tumor imaging.
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