氨基酸衍生的寡聚DTPA酯钆(Ⅲ)配合物对大鼠肝区的MRI弛豫增强  

MRI Relaxation Enhancement of Gadolinium Complexes with Oligo-DTPA-ester Ligands Derived from Amino Acids

作　　者：万福贤[1] 周锦兰[2] 俞开潮[2] 李丽云[3] 

机构地区：[1]山东农业大学化学与材料科学学院,泰安271018 [2]华中科技大学化学系,武汉430074 [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：《华中科技大学学报（医学版）》2005年第6期685-688,共4页Acta Medicinae Universitatis Scientiae et Technologiae Huazhong

基　　金：国家自然科学基金资助项目(No.20275011)

摘　　要：目的寻求高弛豫效能和肝胆道选择性造影剂。方法通过L-N,N-双羟乙基氨基酸与二乙三胺五乙酸(DTPA)双酸酐共聚,合成了由6种氨基酸衍生的线型寡聚DTPA酯钆(Ⅲ)配合物。测试了它们的纵向弛豫速率(R1),并对其中R1较高的聚[L-苯丙氨酸-N,N双(Gd-DTPA乙酯)]作了动物急性毒性测试和T1加权活体成像对比实验。结果含寡聚DTPA酯钆(Ⅲ)配合物比Gd-DTPA的R1要高,对肝区水质子的T1加权像信号具有更高的增强效能、更长的持续增强时间,而且无毒。结论由氨基酸衍生的线型寡聚DTPA酯钆(Ⅲ)配合物有作为新型磁共振成像用造影剂目标分子的应用前景。Objective To develop a new generation of MRI contrast agent with high relaxivity, low toxicity as well as liver selectivity. Methods Six oligo-DTPA-ester Gd^Ⅲ complexes were synthesized by copolymerization of diethylenetriamine pentaacetic dianhydride with 6 L-N, N-bis （2-hydroxethyl） amino acids, respectively. Their longitudinal relaxation rate was measured. One of them, the phenylalanine derivative, with the highest relaxivity, was chosen for the acute toxicity and T1-weighted imaging test. Results There was no toxicity for this new oligomeric Gd^Ⅲ complex, and it exhibited the highly enhanced MRI signal intensity and the prolonged signal duration in the rat liver compared to Gd-DTPA. Coneiusion This new oligomeric Gaduliniuum （Ⅲ） complex is promising to be used as a new series of potential MRI contrast agents.

关 键 词：磁共振成像 寡聚体造影剂 钆(Ⅲ)配合物 氨基酸 T-弛豫增强 

分 类 号：R445.2[医药卫生—影像医学与核医学] R981.9[医药卫生—诊断学]