S. Dall'Angelo, N. Bandaranayaka, A. D. Windhorst, D. J. Vugts, D. van der Born, M. Onega, L. F. Schweiger, M. Zanda, D. O'Hagan



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Nuclear Medicine and Biology

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Author Address

Windhorst, AD Vrije Univ Amsterdam Med Ctr, Dept Nucl Med & PET Res, Boelelaan 1117, NL-1007 MB Amsterdam, Netherlands Univ Aberdeen, Inst Med Sci, Coll Life Sci & Med, Aberdeen AB25 2ZD, Scotland Univ St Andrews, EaStChem Sch Chem, St Andrews KY16 9ST, Fife, Scotland Univ St Andrews, St Andrews KY16 9ST, Fife, Scotland Vrije Univ Amsterdam Med Ctr, Dept Nucl Med & PET Res, NL-1007 MB Amsterdam, Netherlands

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Introduction: 5-[F-18]Fluoro-5-deoxyribose ([F-18]FDR) 3 was prepared as a novel monosaccharide radiotracer in a two-step synthesis using the fluorinase, a C-F bond forming enzyme, and a nucleoside hydrolase. The resulting [F-18]FDR 3 was then explored as a radiotracer for imaging tumours (A431 human epithelial carcinoma) by positron emission tomography in a mice model.
Methods: 5-[F-18]Fluoro-5-deoxyribose ([F-18]FDR) 3, was prepared by incubating S-adenosyl-L-methionine (SAM) and [F-18]fluoride with the fluorinase enzyme, and then incubating the product of this reaction, [F-18]-5′-fluoro-5′-deoxadenosine ([F-18]FDA) 2, with an adenosine hydrolase to generate [F-18]FDR 3. The enzymes were freeze-dried and were used on demand by dissolution in buffer solution. The resulting [F-18]FDR 3 was then administered to four mice that had tumours induced-from the A431 human epithelial carcinoma cell line.
Results: The tumour (A431 human epithelial carcinoma) bearing mice were successfully imaged with [F-18]FDR 3. The radiotracer displayed good tumour imaging resolution. A direct comparison of the uptake and efflux of [F-18]FDR 3 with 2-[F-18]fluoro-2-deoxyglucose ([F-18]FDG) was made, revealing comparative tumour uptake and imaging potential over the first 10-20 min. The study revealed however that [F-18]FDR 3 does not accumulate in the tumour as efficiently as [F-18]FDG over longer time periods.
Conclusions: [F-18]FDR 3 can be rapidly synthesised in a two enzyme protocol and used to image tumours in small animal models. (C) 2013 Elsevier Inc. All rights reserved.