CAJ | 학술논문

将天冬氨酸与亮氨酸反应,合成了天冬氨酸-亮氨酸共聚物(PL),通过乙二胺将钆-1,4,7,10-四氮杂环十二烷-1,4,7,10-四乙酸(Gd-DOTA)连接到PL上,制备了大分子磁共振成像造影剂PL-A2-DOTA-Gd,通过核磁碳谱、凝胶色谱等方法对其结构进行了表征,利用细胞毒性实验、溶血性实验、体外弛豫效率测定以及体内动物磁共振成像等方法对其性能进行了评估。研究表明,PL-A2-DOTA-Gd的细胞毒性远低于临床应用的造影剂Gd-DOTA,且其弛豫效率(15.3 L/(mmol·s))是Gd-DOTA(5.8 L/(mmol·s))的2.6倍。大分子磁共振成像造影剂PL-A2-DOTA-Gd具有良好的血液相容性,对昆明小鼠的肝脏信号的增强效果约为Gd-DOTA的3.1倍,且能在较长时间内保持良好稳定的增强效果。
장천동안산여량안산반응,합성료천동안산-량안산공취물(PL),통과을이알장구-1,4,7,10-사담잡배십이완-1,4,7,10-사을산(Gd-DOTA)련접도PL상,제비료대분자자공진성상조영제PL-A2-DOTA-Gd,통과핵자탄보、응효색보등방법대기결구진행료표정,이용세포독성실험、용혈성실험、체외이예효솔측정이급체내동물자공진성상등방법대기성능진행료평고。연구표명,PL-A2-DOTA-Gd적세포독성원저우림상응용적조영제Gd-DOTA,차기이예효솔(15.3 L/(mmol·s))시Gd-DOTA(5.8 L/(mmol·s))적2.6배。대분자자공진성상조영제PL-A2-DOTA-Gd구유량호적혈액상용성,대곤명소서적간장신호적증강효과약위Gd-DOTA적3.1배,차능재교장시간내보지량호은정적증강효과。
Poly ( aspartic acid-co-leucine) was synthesized, modified via ethylenediamine, conjugated with 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) and finally chelated with gadoliniumⅢ, yielding PL-A2-DOTA-Gd. The T1-relaxivity (15. 3 mmol-1 ·L·s-1 ) of PL-A2-DOTA-Gd was 2. 6 times than that of Gd-DOTA (5. 8 mmol-1·L·s-1) in D2O. The results of magnetic resonance imaging experiments showed significant enhancement in the rat liver after intravenous administration of PL-A2-DOTA-Gd, which persisted longer than Gd-DOTA. The mean percentage enhancements of liver parenchyma were 65. 1%±5. 2%and 21. 3%±4. 9%, for PL-A2-DOTA-Gd and Gd-DOTA, respectively.