高等学校化学学报

高等学校化学学报 ›› 2005, Vol. 26 ›› Issue (8): 1391.

• 研究论文 • 上一篇    下一篇

两亲性双核钆(Ⅲ)配合物的合成与肝选择MRI增强

周锦兰1, 万福贤1, 俞开潮1,2, 丁尚武2   

  1. 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, 高雄804-24
  • 收稿日期:2004-12-01 出版日期:2005-08-10 发布日期:2005-08-10
  • 通讯作者: 俞开潮(1956年出生),男,博士,副教授.从事生物医用试剂与材料和波谱学研究.E-mail:yukc@163.com E-mail:yukc@163.com
  • 基金资助:

    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.

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

ZHOU Jin-Lan1, WAN Fu-Xian1, YU Kai-Chao1,2, DING Shang-Wu2   

  1. 1. Department of Chemistry, Huazhong University of Science and Technology, Wuhan 430074, China;
    2. Department of Chemistry and Center for Nanoscience and Nanotechnology, National Sun Yat-Sen University, Kaohsiung 804-24, Taiwan, China
  • Received:2004-12-01 Online:2005-08-10 Published:2005-08-10

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被引次数

9

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.

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

Abstract: 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, 1HNMR 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(Gd2·3a) 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.

Key words: Amphiphilicity, Dimeric contrast agent, Dimer-Gd(Ⅲ) complex, Relaxivity, Liver-selective MRI, Contrast enhancement

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