新型胺羧单酯-酰胺钆配合物的合成及其对大鼠肝区T_1弛豫增强作用  

Synthesis and MRI Relaxation Enhancement of Mono-exter-amido Gadolinium Complexes

作　　者：俞开潮[1,2] 万福贤[1] 张焱[1] 周锦兰[1] 卢广[3] 刘买利[3] 丁尚武[2,3] 

机构地区：[1]华中科技大学化学系,武汉430074 [2]高雄中山大学化学系与纳米科技中心,中国台湾高雄80424 [3]中国科学院武汉物理与数学研究所,波谱与原子分子物理国家重点实验室,武汉430071

出　　处：《无机化学学报》2004年第4期389-393,共5页Chinese Journal of Inorganic Chemistry

基　　金：国家自然科学基金(No.20275011); 台湾教育部"大学追求卓越计划"(No.A-91-N-FA01-2-4);波谱与原子分子物理国家重点实验室开放课题资助项目。

摘　　要：通过DTPA、EDTA单活化酯与双乳酸酰乙二胺二醇、双乳酸酰己二胺二醇反应,合成了四种新型胺羧单酯鄄酰胺配体及其钆配合物。表征了配体和配合物的结构,测定了钆配合物水溶液水质子的弛豫效能。选取其中一个配合物进行了动物急性毒性测试和活体T1加权成像实验。结果表明:该配合物无明显急性毒性,且对大鼠肝区质子有明显的增强。Four new ester-amido ligands were synthesized by esterification of mono-iso-butyl diethylenetriaminepen-taacetate and mono-iso-butyl ethylenediaminetetraacetate with N,N'-ethylene bis-lactamide and N,N'-1,6-hexam-ethylenebislactamide,respectively.The corresponding Gd(Ⅲ) complexes were made by reacting the ligands with Gd 2 O 3 .All ligands and complexes were characterized by FT-IR,1 H NMR and elemental analysis.The measured longitudinal relaxivity of these complexes were all higher than that of Gd-DTPA.The investigation on cute toxici-ty and T 1 -weighted imaging of complex derived from mono-N,N'-ethylenebislactamide ester diethlenetriaminepen-taacetate were performed.No cute toxicity was found.The tested complex exhibited the higher enhancement on MRI signal intensity in rat liver,comparing with Gd-DTPA.

关 键 词：胺羧单酯-酰胺 钆配合物 合成 肝靶向造影剂 弛豫效能 T1加权磁共振成像 肝癌 早期诊断 

分 类 号：R735.7[医药卫生—肿瘤] R730.4[医药卫生—临床医学]