高等学校化学学报 ›› 2002, Vol. 23 ›› Issue (1): 49.

• 研究论文 • 上一篇    下一篇

二乙三胺五乙酸吡哆醇酯配体及其钆配合物的合成、弛豫率和肝靶向性研究

丁雄军, 卓仁禧, 付功成   

  1. 教育部生物医用高分子材料开放实验室, 武汉大学化学系, 武汉 430072
  • 收稿日期:2000-11-11 出版日期:2002-01-24 发布日期:2002-01-24
  • 通讯作者: 卓仁禧(1931年出生),男,教授,博士生导师,中国科学院院士,从事生物医用高分子材料研究
  • 基金资助:

    国家自然科学基金(批准号:29874028)资助

Studies on the Synthesis, Relaxivity and Liver-targeting of DTPA-Pyridoxol Ester Gadolinium Complexes

DING Xiong-Jun, ZHUO Ren-Xi, FU Gong-Cheng   

  1. Key Laboratory of Biomedical Polymer Materials, Ministry of Education; Department of Chemistry, Wuhan University, Wuhan 430072, China
  • Received:2000-11-11 Online:2002-01-24 Published:2002-01-24

摘要: 由维生素B6族化合物吡哆醇及其衍生物与二乙三胺五乙酸(DTPA)双酸酐反应合成了一系列二乙三胺五乙酸吡哆醇酯配体.将这些配体与GdCl3·6H2O反应后得到了钆配合物.测定了这些配合物在水溶液中水质子的纵向弛豫率R1.与母体配合物GdDTPA相比,R1值略有提高.配体用放射性核素99Tc标记,研究了其肝靶向性.结果表明,配体2和6的肝靶向性较为明显.动物核磁共振成像实验进一步证实由这两种配体合成的钆配合物对大鼠肝部的造影信号明显增强

关键词: 核磁共振成像造影剂, 吡哆醇, 肝靶向性, 钆配合物, 弛豫率

Abstract: Several new DTPA-pyridoxol ester ligands were synthesized by reacting diethylene-triam inepentaacetic anhydride(DTPAA) with pyridoxol derivatives. Their gadolinium complexes were also prepared. Their T1 relaxivities in water were measured. The 99Tc-labelled combination radioactivity experiment with liver cells and kidney cells of mice showed that ligands 2 and 6 possessed an excellent liver-targeting property. The results of animal MR imaging experiment further confirmed that the signals in liver were obviously strengthened after injection of Gd2 and Gd6.

Key words: MRI contrast agent, Pyridoxol, Liver targeting, Godolinium complex, Relaxivity

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