CAJ | 학술논문

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pH =5.5的组织蛋白酶B的磷酸缓冲液中，AP-EDA-DOTA-Gd能够降解．AP- EDA-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 (5.59 mmol–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%)．
일충신형적이천문동안산-분병안산공취물위재체적대분자생물상용성재료(AP-EDA-DOTA-Gd)피제비출래작위자공진성상조영제．수선합성료천문동안산-분병안산공취물，지후이용을이알장1，4，7，10-사담잡배십이완-1，4，7，10-사을산(DOTA)련접도공취물상，최후장구리자통과배위적작용방식련접도 DOTA 상，최종득도대분자AP-EDA-DOTA-Gd．체외용혈성시험표명AP-EDA-DOTA-Gd구유교호적혈액상용성．재pH =5.5적조직단백매B적린산완충액중，AP-EDA-DOTA-Gd능구강해．AP- EDA-DOTA-Gd적체외이예효솔(15.95 mmol–1×L×s–1)위목전림상응용적Gd-DOTA (5.59 mmol–1×L×s–1)적2.9배．대서간장성상실험결과표명，AP-EDA-DOTA-Gd대우간조직적성상증강대비도위63.5±6.1%원고우Gd-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.