一种肝脏类生物相容性氨基酸共聚物磁共振成像造影剂（英文）  

A Biocompatible Gadolinium(Ⅲ)-Poly(Aspartic Acid-Co-Phenylalanine) for Liver Magnetic Resonance Imaging Contrast Agent

作　　者：肖研[1] 湛游洋 薛蓉[1] 李晓晶[1] 裴奉奎[1] 冯江华[2] 占博涵 

机构地区：[1]中国科学院长春应用化学研究所,长春130022 [2]厦门大学电子科学系,厦门361005

出　　处：《波谱学杂志》2015年第2期273-282,共10页Chinese Journal of Magnetic Resonance

基　　金：The National Natural Science Foundation of China(20975097 and 21305134)

摘　　要：一种新型的以天门冬氨酸-苯丙氨酸共聚物为载体的大分子生物相容性材料(AP-EDA-DOTA-Gd)被制备出来作为磁共振成像造影剂.首先合成了天门冬氨酸-苯丙氨酸共聚物,之后利用乙二胺将1,4,7,10-四氮杂环十二烷-1,4,7,10-四乙酸(DOTA)连接到共聚物上,最后将钆离子通过配位的作用方式连接到DOTA上,最终得到大分子AP-EDA-DOTA-Gd.体外溶血性试验表明AP-EDA-DOTA-Gd具有较好的血液相容性.在p H=5.5的组织蛋白酶B的磷酸缓冲液中,AP-EDA-DOTA-Gd能够降解.APEDA-DOTA-Gd的体外弛豫效率(15.95 mmol–1·L·s–1)为目前临床应用的Gd-DOTA(5.59mmol–1·L·s–1)的2.9倍.大鼠肝脏成像实验结果表明,AP-EDA-DOTA-Gd对于肝组织的成像增强对比度为63.5±6.1%远高于Gd-DOTA(24.2±2.9%).A new biocompatible gadolinium （III）-macromolecule （AP-EDA-DOTA-Gd） was developed as a magnetic resonance imaging （MRI） contrast agent. Poly （aspartic acid-co- phenylalanine） was synthesized, modified via ethylenediamine, conjugated with 1,4,7,10- tetraazacyclododecane-1,4,7,10-tetraacetic acid （DOTA） and finally chelated gadolinium （III）, yielding gadolinium （III）-based macromolecule （AP-EDA-DOTA-Gd）. The hemolytic tests showed the hemocompatibility of this gadolinium （III）-based macromolecular conjugate.In vitro, AP-EDA-DOTA-Gd could be degraded, when it was incubated with cathepsin B in phosphate buffered solution （pH = 5.5）. TheT1-relaxivity （15.95 mmol–1·L·s–1） of AP-EDA-DOTA-Gd was 2.9 times of that （5.59 mmol–1·L·s–1） of the clinical MRI contrast agent （Gd-DOTA） at 1.5 T and 25℃. The liver enhancement of AP-EDA-DOTA-Gd was 63.5±6.1% during the maximum enhancement time （50-80 min）, which was much better than that of Gd-DOTA （24.2±2.9%, 10-30 min）. AP-EDA-DOTA-Gd was expected to be a potential liver MRI contrast agent.

关 键 词：MRI造影剂 钆大分子 肝脏 弛豫效率 

分 类 号：O482.53[理学—固体物理]