Al18F labeled sulfonamide-conjugated positron emission tomography tracer in vivo tumor-targeted imaging |
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Authors: | Fan Liu Biao Zhao Xiao-Tian Xia Jia-Rui Yan Fa-Quan Yu Guo-Ping Yan Jia Hu Si Chen Yu-Fang Wang Hui Liu Xiao-Li Lan Yong-Xue Zhang |
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Institution: | 1. School of Chemical Engineering and Pharmacy, Wuhan Institute of Technology, Wuhan, China
School of Chemistry, Physics, and Mechanical Engineering, Queensland University of Technology, Brisbane, Queensland, Australia;2. School of Materials Science and Engineering, Wuhan Institute of Technology, Wuhan, China;3. Center for PET of Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, China;4. School of Chemical Engineering and Pharmacy, Wuhan Institute of Technology, Wuhan, China |
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Abstract: | An ideal positron emission tomography (PET) tracer should be highly extractable by the tumor tissue or organ that contains low toxicity and can provide high-resolution images in vivo. In this work, the aim was to evaluate the application of Al18F-labeled 1,4,7-triazacyclononane-1,4,7-triacetic acid containing sulfonamide group (18F-Al-NOTA-SN) as a potential tumor-targeting signal-enhanced radioactive tracer in PET. SN as a tumor-targeting group was incorporated to NOTA to make a ligand. Subsequently, this ligand reacted with Na18F and AlCl3 to produce a compound 18F-Al-NOTA-SN. This compound was further characterized and its property in regard to cell cytotoxicity assay, microPET imaging, biodistribution, cell uptake assay, and tumor selectivity in vitro and in vivo, was also investigated. 18F-Al-NOTA-SN possessed low cell cytotoxicity and uptake to COS-7 and 293T healthy cells and high cell cytotoxicity and uptake to MDA-MB-231, HepG2, and HeLa tumor cells in vitro. Moreover, 18F-Al-NOTA-SN showed good tumor-targeting property and high PET signal enhancement of HeLa tumors, liver, and kidneys in mice, as well as the uptake ratios of tumor to blood and tumor to muscle, were 4.98 and 3.87, respectively. 18F-Al-NOTA-SN can be accepted to be kidney and liver eliminated earlier and show a potential tumor-targeting signal-enhanced radioactive tracer in PET. |
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Keywords: | 18F-labeled tracer NOTA positron emission computed tomography sulfonamide tumor-targeting property |
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