华东理工大学学报（自然科学版）2018，Vol.44Issue(2)：168-174,7.DOI:10.14135/j.cnki.1006-3080.20170331003
一种高稳定性钆类核磁共振成像造影剂的合成
Synthesis of a Highly Stable Gadolinium Based MRI Contrast Agent
摘要
Abstract
Magnetic Resonance Imaging(MRI)is a powerful method for clinical diagnosis and therapy due to the distinguishing characteristics of providing high-quality three-dimensional images of soft tissue without the need for harmful ionizing radiation.Complexes of gadolinium(Ⅲ)have proven to be especially effective M RI contrast agents,as it is estimated that they are needed for over 30% of the patients to accelerate relaxation rate of in vivo water protons,thus enhancing the contrast of different biological tissues and definition between normal tissues and diseased parts.For more sensitive small-molecule gadolinium-based M RI contrast agents,one essential requirement is to increase the hydration number q, which enhances the gadolinium's relaxivity.However,with the concern of chronic kidney disease(CKD) and nephrogenic systemic fibrosis(NSF),competition between strong chelate stability and free water coordination sites has increasingly become a challenge to M RI enhancement agent design.A highly stable N-oxide-DTPA-bisamide-based Gd(Ⅲ)complex with 3 coordinated water molecules is synthesized.The general methods such as 1 H-NMR,13C-NMR and ESI-MS spectroscopy are used to characterize the structures of the ligand and the complex.T he hydration number determined by the fluorescence lifetime of its Europium(Ⅲ)analogue is 3.M RI measurement show s much higher relaxivity value(16.39 mM -1·s-1) than commercial contrast agents.By fitting the potentiometric data with HYPERQUAD program,the formation constants of the Gd(Ⅲ)complex are calculated and demonstrated a superior stability over Gd-DTPA-BMA(Omniscan?).Meanwhile,in vivo imaging shows good imaging quality and cell tests reveal low cytotoxicity of the complexes,which indicate its great potential for future clinical applications.关键词
核磁共振成像造影剂/氮氧化/水合常数/弛豫率/稳定性Key words
MRI contrast agents/N-oxides/hydration number/relaxivity/stability分类
化学化工引用本文复制引用
程丽坤,钱伟桥,丁云,胡爱国..一种高稳定性钆类核磁共振成像造影剂的合成[J].华东理工大学学报（自然科学版）,2018,44(2):168-174,7.基金项目
国家自然科学基金(21274042) （21274042）
