一类具有高水合常数的钆类核磁共振成像造影剂的研究

郝士婧; 熊儒琳; 程丽坤; 胡爱国

doi:10.14135/j.cnki.1006-3080.2016.01.005

郝士婧 , 熊儒琳 , 程丽坤 , 胡爱国

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一类具有高水合常数的钆类核磁共振成像造影剂的研究

1.
华东理工大学材料科学与工程学院, 上海市先进聚合物材料重点实验室, 上海 200237

通讯作者: 胡爱国, hagmhsn@ecust.edu.cn

基金项目: 国家自然科学基金(21274042)
中图分类号: O621.3

A New Type of Magnetic Resonance Imaging Contrast Agents with High Hydration Numbers

1.
Shanghai Key Laboratory of Advanced Polymeric Materials, School of Materials Science and Engineering, East China University of Science and Technology, Shanghai 200237, China

Corresponding author: HU Ai-guo, hagmhsn@ecust.edu.cn

CLC number: O621.3

摘要: 合成了一类具有高水合常数(q)的钆类造影剂,该类配合物由金属钆与含有2个氮氧化基团和4个羧酸基团的有机配体组成,具有高水合常数的特点。通过核磁氢谱、碳谱以及高分辨质谱对配体及配合物的结构进行了表征。通过荧光寿命分析检测配合物的q值在3左右。该类配合物的纵向弛豫率(r₁)为8.5~10.1 (mM)^-1·s^-1,约为商用造影剂二乙三胺五乙酸合钆(Gd-DTPA)的3倍。细胞实验证实该类造影剂具有很低的细胞毒性,这在临床应用中是非常关键的。该类配合物具有合成简便、弛豫率高以及毒性低等特点,为制备更低成本、更高性能的造影剂打下基础。
- 氮氧化合物 /
- 钆(Ⅲ)配合物 /
- 核磁共振成像造影剂 /
- 纵向弛豫率 /
- 水合常数
Abstract: A series of Gd(Ⅲ) complexes were synthesized and evaluated as potential magnetic resonance imaging (MRI) contrast agents.The ligands of these complexes are featured with two hyphenated amine-N-oxide and four carboxyl groups,providing the complexes with high hydration numbers (q,the number of inner-sphere water molecules).The structures of the ligands and complexes were characterized with ¹H-NMR,¹³C-NMR and ESI-MS.Preliminary results on 1.5T MRI measurement of the complexes showed high r₁ values (longitudinal relaxivity) of 8.5-10.1 (mM)^-1·s^-1.The q value of the complexes was determined as up to 3 with fluorescence lifetime analysis with their Eu(Ⅲ) analogues.Cell tests revealed low cytotoxicity of the complexes,which is essential for clinical applications.The structural simplicity,the high relaxivity and the low toxicity of the complexes provide a new solution for the development of highly efficient MRI contrast agents.
- N-oxides /
- gadolinium complexes /
- MRI contrast agents /
- longitudinal relaxivity /
- hydration numbers

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一类具有高水合常数的钆类核磁共振成像造影剂的研究

通讯作者: 胡爱国, hagmhsn@ecust.edu.cn

1. 华东理工大学材料科学与工程学院, 上海市先进聚合物材料重点实验室, 上海 200237

收稿日期: 2015-05-05
网络出版日期: 2016-02-29

基金项目: 国家自然科学基金(21274042)

关键词:

摘要: 合成了一类具有高水合常数(q)的钆类造影剂,该类配合物由金属钆与含有2个氮氧化基团和4个羧酸基团的有机配体组成,具有高水合常数的特点。通过核磁氢谱、碳谱以及高分辨质谱对配体及配合物的结构进行了表征。通过荧光寿命分析检测配合物的q值在3左右。该类配合物的纵向弛豫率(r₁)为8.5~10.1 (mM)^-1·s^-1,约为商用造影剂二乙三胺五乙酸合钆(Gd-DTPA)的3倍。细胞实验证实该类造影剂具有很低的细胞毒性,这在临床应用中是非常关键的。该类配合物具有合成简便、弛豫率高以及毒性低等特点,为制备更低成本、更高性能的造影剂打下基础。