【摘要】 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。更多还原

【Abstract】 Poly( aspartic acid-co-leucine) was synthesized,modified via ethylenediamine,conjugated with1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid(DOTA) and finally chelated with gadolinium ?,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 D2 O. 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 were65. 1% ± 5. 2% and 21. 3% ± 4. 9%,for PL-A2-DOTA-Gd and Gd-DOTA,respectively.更多还原