两亲性双核钆(Ⅲ)配合物的合成与肝选择MRI增强  

Synthesis of Amphiphilic Dimers of Gd(Ⅲ) Complexes and Their Liver-selective Contrast Enhancement in MRI

作　　者：周锦兰[1] 万福贤[1] 俞开潮[1] 丁尚武[2] 

机构地区：[1]华中科技大学化学系,武汉430074 [2]台湾中山大学化学系与纳米科技中心

出　　处：《高等学校化学学报》2005年第8期1391-1394,共4页Chemical Journal of Chinese Universities

基　　金：国家自然科学基金(批准号:20275011);波谱与原子分子物理国家重点实验室基金(T012045);台湾"大学追求卓越计划"(A-92-N-FA01-2-4-5)资助.

摘　　要：通过二乙三胺五乙酸单环酸酐和乙二胺四乙酸单环酸酐分别与L-赖氨酸苄酯的双酰化反应,制得两种含有双胺羧螯合单元的配体.它们与GdCl3·6H2O反应得到相应的两亲性双核钆(Ⅲ)配合物.表征了配体和配合物的结构,测试了配合物的纵向弛豫效能(R1).进行了双DTPA酰(L-赖氨酸苄酯)钆(Gd2-3a)的急性毒性和与Gd-DTPA的动物T1加权成像对比实验.结果表明,这两种新配合物的R1都高于Gd-DTPA.Gd2-3a无明显急性毒性,且比Gd-DTPA对肝区实质细胞有更长时间和更大程度的选择性增强.Benzyl ester of L-lysine was bis-acylated with diethylenetriaminepentaacetic monoanhydride （DTPA-MA） and ethylenediaminetetraacetic monoanhydride （EDTA-MA） respectively to produce two dimeric ligands. The reactions of these two ligands with GdCl3·6H2O yield amphiphilic bi-nuclear Gd（Ⅲ） complexes. These new ligands and their respective Gd（Ⅲ） complexes were characterized by IR, ^1H NMR and elemental analysis. The dimeric complexes show higher relaxivities as compared to that of Complex Gd-DTPA which is widely used in clinic diagnoses. The Gd （Ⅲ） complex with bis- diethylenetriaminepentaacetate of benzyl ester of lysine（Gd2z · 3a） exhibits no obvious toxicity and offers a higher MRI signal enhancement as well as longer retention time in the t1-weighted imaging of Wistar rat liver tissue compared to complex Gd-DTPA.

关 键 词：双亲性 二倍体造影剂 双钆(Ⅲ)配合物 弛豫效能(R1) 肝选择成像 对比增强 

分 类 号：O614.33[理学—无机化学] O657.61[理学—化学]