:: Volume 19, Issue 2 (4-2021) ::
Int J Radiat Res 2021, 19(2): 357-363 Back to browse issues page
18-F-Fluoroglucosylation of an arginine-arginine-leucine peptide as a potential tumor imaging agent for positron emission tomography
R.F. Wang, Z.G. Wang, M.M. Yu, Y.H. Chen, B. Shi, W. Xue
Department of Nuclear Medicine, the Affiliated Hospital of Qingdao University, Qingdao, China , mingmingyu@vip.sina.com
Abstract:   (3158 Views)
Background: Based on the principle of oxime formation, 18F labeling of polypeptides can be achieved via a reaction between an aldehyde group-containing 18F-prosthetic group and an aminooxy-modified polypeptide. The focus of this study was to investigate the one-step synthesis of 2-[18F] fluoro-2-deoxyglucose (18F-FDG)- arginine-arginine-leucine (RRL) from open-ring 18F-FDG and the aminooxy-modified RRL peptide cyclo(RRLfK)-ONH2 and to study the biological distribution of 18F-FDG-RRL in a nude mouse model of human neuroglioma. Materials and Methods: The aminooxy-modified RRL peptide cyclo(RRLfK)-ONH2 was used as the precursor to react with 18F-FDG at 100 ℃ and different pH values for 30 minutes to synthesize 18F-FDG-RRL. The labeling yield, radiochemical purity, and in-vitro stability of the product were measured, and the biological distribution of 18F-FDG-RRL in tumor-bearing nude mice was analyzed at 30 minutes, 60 minutes and 120 minutes. Results: The labeling yield of 18F-FDG-RRL was (25.5±5.0) % at a pH of 2.0, and its radiochemical purity was greater than 95%. 18F-FDG-RRL was mainly excreted through the kidneys, with rapid blood clearance. One hour after injection, the uptake of 18F-FDG-RRL in tumors was (1.83±0.12) injected dose per gram of tissue (%ID/g), with a tumor/muscle ratio of 7.03±0.04, a tumor/blood ratio of 4.36±0.21 and a tumor/brain ratio of 7.53±1.37. Conclusion: The synthesis of 18F-FDG-RRL can be achieved through oximation. This method is straightforward and easy to promote. 18F-FDG-RRL has rapid blood clearance and high uptake by tumors.
Keywords: Oxime, 2-fluoro-2-deoxyglucose, arginine-arginine-leucine, peptide.
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Type of Study: Original Research | Subject: Medical Physics



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Volume 19, Issue 2 (4-2021) Back to browse issues page