Acta Chimica Sinica ›› 2012, Vol. 70 ›› Issue (09): 1066-1072.DOI: 10.6023/A1112275 Previous Articles     Next Articles

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新型PET 核素68Ga 标记D-脱氧葡萄糖的合成及生物学评价

杨志, 朱华   

  1. 北京大学肿瘤医院暨北京市肿瘤防治研究所 核医学科 恶性肿瘤发病机制及转化研究教育部重点实验室 北京 100142
  • 收稿日期:2011-12-27 修回日期:2012-02-27 出版日期:2012-05-14 发布日期:2012-05-18
  • 通讯作者: 杨志 E-mail:pekyz@163.com
  • 基金资助:

    国家自然科学基金(Nos. 81071198, 81172082)资助项目.

Synthesis and Evaluation of New Nuclides Ga-68 Labeled D-Glucose for Potential PET Imaging Agent

Yang Zhi, Zhu Hua   

  1. Key Laboratory of Carcinogenesis and Translational Research (Ministry of Education), Department of Nuclear Medicine, Peking University Cancer Hospital & Institute, Beijing 100142
  • Received:2011-12-27 Revised:2012-02-27 Online:2012-05-14 Published:2012-05-18
  • Supported by:

    Project supported by the National Natural Science Foundation of China (Nos. 81071198, 81172082).

Starting from D-glucosamine (DG), the precursor compound 2-(4-isothiocyanatobenzyl)- 1,4,7,10-tetraazacyclo-dodecane-1,4,7,10-tetraacetic acid-D-glucose (DG-DOTA) was synthesized for potential radioactive imaging agents. Its structure was characterized by infrared, 1H NMR, LC-MS and ESI-HRMS. 68Ga is a generator-produced nuclide and does not require cyclotron on site. By careful selection of radiolabeling conditions, 68Ga-DOTA-DG was synthesized in short time and high yield by microwave synthesis system. Then, its binding affinity was tested by K-562, Hela and A431 tumor cell lines. The synthesis and evaluation of 68Ga-labeled DOTA-DG, not only provides a useful assessment of the stage of cancer by imaging tumor metabolites compared with 18F-FDG, but also develops a PET imaging agent.

Key words: gallium-68, 2-amino-deoxy-D-glucose, microwave-assisted synthesis, PET imaging