Positron labeled antioxidants: Synthesis and tissue biodistribution of 6-deoxy-6-[18F]fluoro-l-ascorbic acid |
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| Affiliation: | 1. Division of Earth and Environmental Science, Graduate School of Science and Engineering, Kagoshima University, 1-21-35 Korimoto, Kagoshima 890-0065, Japan;2. Department of Human Environmental Science, Graduate School of Human Development and Environment, Kobe University, 3-11 Tsurukabuto, Nada, Kobe 657-8501, Japan;3. Water and Environmental Engineering, Graduate School of Engineering, Nagasaki University, 1-14 Bunkyo-machi, Nagasaki 852-8521, Japan;4. Department of Applied Science, Okayama University of Science, 1-1 Ridaicho, Okayama 700-0005, Japan;1. Institute of Nuclear Chemistry, Johannes Gutenberg University Mainz, 55128 Mainz, Germany.;2. Department of Nuclear Medicine, Hannover Medical School, 30625 Hannover, Germany.;1. Servicio de Medicina Nuclear, Clínica Universidad de Navarra, Pamplona, Navarra, España;2. Servicio de Radiofarmacia, Clínica Universidad de Navarra, Pamplona, Navarra, España;3. Servicio de Anatomía Patológica, Clínica Universidad de Navarra, Pamplona, Navarra, España;1. Department of Radiation Oncology, Brigham and Women’s Hospital, Dana–Farber Cancer Institute and Harvard Medical School, Boston, MA, USA;2. Medical Physics Program, Department of Physics and Applied Physics, University of Massachusetts Lowell, Lowell, MA, USA;1. National Center for Tuberculosis Control and Prevention, Chinese Center for Disease Control and Prevention, No. 155, Changbai Road, Beijing, China;2. Respiratory Diseases Department of Nanlou, Chinese People''s Liberation Army General Hospital, Beijing, China;3. PATH, China Office, Beijing, China;4. Bill and Melinda Gates Foundation, China Office, Beijing, China;5. Stanley Ho Centre for Emerging Infectious Diseases, Faculty of Medicine, Chinese University of Hong Kong, Hong Kong, China;6. Department of Clinical Laboratory, Shang Hai Pulmonary Disease Hospital, Shanghai, China;1. Department of Molecular Oncology, BC Cancer Agency, Vancouver, BC V5Z 1L3, Canada;2. Department of Chemistry, University of British Columbia, Vancouver, BC V6T 1Z1, Canada;3. Department of Functional Imaging, BC Cancer Agency, Vancouver, BC V5Z 4E6, Canada;4. Department of Radiology, University of British Columbia, Vancouver, BC V5Z 1M9, Canada |
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| Abstract: | A one-pot synthesis of 6-deoxy-6-[18F]fluoro-l-ascorbic acid (18F-DFA) has been developed via nucleophilic displacement of a cyclic sulfate with no-carrier-added [18F]fluoride ion. Isolated radiochemical yields of around 15% were obtained with radiochemical purity of over 99% after overall synthesis time of 90 min. Tissue distribution studies with 18F-DFA in rats showed high uptake of radioactivity in the adrenals, kidneys, liver and small intestine—organs known to have high concentrations of l-ascorbic acid. The slow and low uptake of radioactivity in the brain was observed between 10 and 120 min after i.v. injection. In vivo behavior of 18F-DFA in mice bearing 3-methylcholanthrene-induced fibrosarcoma demonstrated its ability to accumulate in the tumor. |
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