https://scholars.lib.ntu.edu.tw/handle/123456789/553464
Title: | Evaluation of 5-[ 18 F]fluoro-2?-deoxycytidine as a tumor imaging agent: A comparison of [ 18 F]FdUrd, [ 18 F]FLT and [ 18 F]FDG | Authors: | Yu H.-M. Chiu C.-H. Chen W.-T. Wu C.-H. Lin P.-Y. Huang Y.-Y. Chen J.-H. KAI-YUAN TZEN Shiue C.-Y. Lin W.-J. |
Keywords: | Nucleosides; PET; Proliferation; [ 18 F]FdCyd; [ 18 F]FLT | Issue Date: | 2019 | Journal Volume: | 148 | Start page/Pages: | 152-159 | Source: | Applied Radiation and Isotopes | Abstract: | One of the hallmarks of cancer is increased cell proliferation. Measurements of cell proliferation by estimation of DNA synthesis with several radiolabeled nucleosides have been tested to assess tumor growth. Deoxycytidine can be phosphorylated by deoxycytidine kinase (dCK) and is incorporated into DNA. This study evaluated a radiofluorinated deoxycytidine analog, 5-[ 18 F]fluoro-2′-deoxycytidine ([ 18 F]FdCyd), as a proliferation probe and compared it with 5-[ 18 F]fluoro-2′-deoxyuridine ([ 18 F]FdUrd), 3′-deoxy-3'-[ 18 F]fluorothymidine ([ 18 F]FLT), and [ 18 F]fluorodeoxyglucose ([ 18 F]FDG) in a tumor-bearing mouse model. [ 18 F]FdCyd was synthesized from two precursors by direct electrophilic substitution. The serum stability and partition coefficient of [ 18 F]FdCyd were evaluated in vitro. Positron emission topography (PET) imaging of Lewis lung carcinoma (LLC)-bearing mice with [ 18 F]FdCyd, [ 18 F]FdUrd, [ 18 F]FLT, and [ 18 F]FDG were evaluated. [ 18 F]FdCyd was stable in mouse serum and normal saline for up to 4 h. With all radiotracers except [ 18 F]FLT, PET can clearly delineate the tumor lesion. [ 18 F]FdCyd and [ 18 F]FdUrd showed high accumulation in the liver and kidney. The SUV and tumor-to-muscle (T/M) ratios derived from PET imaging of the radiotracers were [ 18 F]FDG > [ 18 F]FdCyd > [ 18 F]FdUrd > [ 18 F]FLT. Selective retention in tumors with a favorable tumor/muscle ratio makes [ 18 F]FdCyd a protential candidate for further investigation as a proliferation imaging agent. ? 2019 Elsevier Ltd |
URI: | https://scholars.lib.ntu.edu.tw/handle/123456789/553464 | ISSN: | 0969-8043 | DOI: | 10.1016/j.apradiso.2019.03.034 | SDG/Keyword: | Biomolecules; Body fluids; Cell proliferation; Mammals; Polyethylene terephthalates; Radioactive tracers; Topography; Electrophilic substitutions; Lewis lung carcinomata; Nucleosides; Partition coefficient; Proliferation; Tumor imaging agents; [^18F]FdCyd; [^18F]FLT; Tumors; 3' fluorothymidine f 18; 5 fluoro 2' deoxycytidine f 18; 5 fluoro 2' deoxyuridine f 18; fluorodeoxyglucose f 18; radiopharmaceutical agent; tracer; unclassified drug; 5-fluoro-2'-deoxycytidine; deoxycytidine; floxuridine; fluorodeoxyglucose f 18; radiopharmaceutical agent; animal cell; animal experiment; animal model; animal tissue; Article; C57BL 6 mouse; cell proliferation; diagnostic imaging; drug accumulation; drug screening; drug stability; drug synthesis; fluorination; hydrophilicity; in vitro study; Lewis carcinoma; Lewis lung carcinoma cell; male; mouse; nonhuman; partition coefficient; positron emission tomography; positron emission tomography-computed tomography; priority journal; radioactivity; tumor growth; animal; blood; C57BL mouse; procedures; tissue distribution; tumor cell line; xenograft; Animals; Cell Line, Tumor; Deoxycytidine; Floxuridine; Fluorodeoxyglucose F18; Heterografts; Male; Mice; Mice, Inbred C57BL; Positron-Emission Tomography; Radiopharmaceuticals; Tissue Distribution |
Appears in Collections: | 醫學院附設醫院 (臺大醫院) |
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