有机化学 ›› 2018, Vol. 38 ›› Issue (7): 1779-1785.DOI: 10.6023/cjoc201801044 上一篇    下一篇

研究论文

两种具有高弛豫率的双核非离子型磁共振对比剂

孙宏顺a,b, 李玉龙b, 蒋蕻b, 郭成a, 沈临江a,c   

  1. a 南京工业大学 化学与分子工程学院 南京 211816;
    b 南京科技职业学院 江苏省磁共振靶向显像剂工程实验室 南京 210048;
    c 南京工业大学 数理科学学院 南京 211816
  • 收稿日期:2018-01-29 修回日期:2018-03-04 发布日期:2018-03-29
  • 通讯作者: 沈临江 E-mail:ljshen@njtech.edu.cn
  • 基金资助:

    江苏省高校自然科学基金(No.17KJB320001)、江苏省高校品牌专业建设工程(No.PPZY2015B179)、江苏省高等学校大学生创新创业训练计划(No.201712920001Y)和江苏省青蓝工程资助项目.

Two Binuclear Nonionic Magnetic Resonance Contrast Agents with High Relaxivity

Sun Hongshuna,b, Li Yulongb, Jiang Hongb, Guo Chenga, Shen Linjianga,c   

  1. a College of Chemistry and Molecular Engineering, Nanjing Tech University, Nanjing 211816;
    b Targeted MRI Contrast Agents Laboratory of Jiangsu Province, Nanjing Polytechnic Institute, Nanjing 210048;
    c School of Physical and Mathematical Sciences, Nanjing Tech University, Nanjing 211816
  • Received:2018-01-29 Revised:2018-03-04 Published:2018-03-29
  • Contact: 10.6023/cjoc201801044 E-mail:ljshen@njtech.edu.cn
  • Supported by:

    Project supported by the Natural Science Foundation in Jiangsu Province (No. 17KJB320001), the Top-notch Academic Programs Project of Jiangsu Higher Education Institutions (No. PPZY2015B179), the Training Program of Students Innovation and Entrepreneurship in Jiangsu Province (No. 201712920001Y), and the Qing Lan Project of Jiangsu Province.

磁共振成像技术被广泛应用于诊断医学和软组织成像,而磁共振对比剂有助于提高成像对比度.报道了两种基于钆-DOTA-酰肼结构的新型双核非离子型磁共振对比剂[(Gd-DOTAH)2-DYMB和(Gd-DOTAH)2-DYMBP]的设计、合成及弛豫性能.在0.5 T磁场下,测得其纵向弛豫率分别为每分子11.4和11.7 L·mmol-1·s-1或5.7和5.9 L·mmol-1· Gd-1·s-1,高于目前临床使用的单核大环对比剂钆-DOTA.体外磁共振成像研究显示该两种磁共振对比剂具有提高诊断灵敏度和准确度的应用潜力.

关键词: 磁共振成像, 对比剂, 合成, 弛豫率, DOTA-酰肼, 钆-DOTA

Magnetic resonance imaging (MRI) is widely used in diagnostic medicine and soft tissue imaging. Contrast agents (CAs) can improve the specificity of MRI enhancement. Herein, the design, synthesis and relaxivity of two novel binuclear nonionic Gd-based DOTA-hydrazide derived MRI contrast agents, (Gd-DOTAH)2-DYMB and (Gd-DOTAH)2-DYMBP are reported. They have improved longitudinal relaxivity values of 11.4 and 11.7 L·mmol-1·s-1 per molecule or 5.7 and 5.9 L·mmol-1·Gd-1·s-1 at 0.5 T, respectively, which are higher than that of the mononuclear clinical macrocyclic agent Gd-DOTA. And in vitro MRI studies suggest the potential of these two agents as MRI contrast agents in improving the diagnostic sensitivity and accuracy.

Key words: magnetic resonance imaging (MRI), contrast agents, synthesis, relaxivity, DOTA-hydrazide, Gd-DOTA