Liver-targeting macromolecular MRI contrast agents  

作　　者：鄢国平 卓仁禧 徐勉懿 李丽云 唐岳枫 

出　　处：《Science China Chemistry》2001年第4期344-352,共9页中国科学（化学英文版）

基　　金：Acknowledgements The authors would like to thank Mr. Cao Guoqiang and Mr. Cao Wei (Department of Nuclear Medicine of Wuhan Union Hospital) for their assistance in the biodistribution experiment, Profs. Zheng Congyi and Mr. Qu Sanfu (College of Life Scien

摘　　要：Macromolecular ligands with liver-targeting group (pyridoxamine, PM) PHEA-DTPA-PM and PAEA-DTPA-PM were prepared by the incorporation of different amount of diethylenetria-minepentaacetic acid monopyridoxamine group (DTPA-PM) into poly-α, β-[N-(2-hydroxyethyl)-L-aspartamide] (PHEA) and poly-α, β-[N-(2-aminoethyl)-L-aspartamide] (PAEA). The macromolecular ligands thus obtained were further complexed with gadolinium chloride to give macromolecular MRI contrast agents with different Gd(III) contents. These macromolecular ligands and their gadolinium complexes were characterized by1H NMR, IR, UV and elementary analysis. Relaxivity studies showed that these polyaspartamide gadolinium complexes possess higher relaxation effectiveness than that of the clinically used Gd-DTPA. Magnetic resonance imaging of the liver in rats and experimental data of biodistribution in mice indicate that these macromolecular MRI contrast agents containing pyridoxamine exhibit liver-targeting property.Macromolecular ligands with liver-targeting group (pyridoxamine, PM) PHEA-DTPA-PM and PAEA-DTPA-PM were prepared by the incorporation of different amount of diethylenetria-minepentaacetic acid monopyridoxamine group (DTPA-PM) into poly-cc, p-[N-(2-hydroxyethyl)-L-aspartamide] (PHEA) and poly-α, β-[N-(2-aminoethyl)-L-aspartamide] (PAEA). The macromolecular ligands thus obtained were further complexed with gadolinium chloride to give macromolecular MRI contrast agents with different Gd(Ⅲ) contents. These macromolecular ligands and their gadolinium complexes were characterized by 1H NMR, 1R, UV and elementary analysis. Relaxivity studies showed that these polyaspartamide gadolinium complexes possess higher relaxation effectiveness than that of the clinically used Gd-DTPA. Magnetic resonance imaging of the liver in rats and experimental data of biodistribution in mice indicate that these macromolecular MRI contrast agents containing pyridoxamine exhibit liver-targeting property.

关 键 词：POLYASPARTAMIDE gadolinium complexes magnetic resonance imaging (MRI) RELAXIVITY liver-targeting 

分 类 号：O657.2[理学—分析化学]