将肿瘤靶向基团5-(4-氨基苯基)-10,15,20-三(4-磺酸苯基)卟啉钠(APTSPP)与二乙三胺五乙酸(DTPA)分别键接在葡聚糖侧链上,再与钆Gd(III)离子配合,从而研制出一种新型含卟啉基葡聚糖大分子磁共振成像造影剂(APTSPP-Dextran-DTPA-Gd).对所合成的配体及钆配合物分别进行了核磁共振氢谱、紫外可见光谱、傅里叶变换红外光谱等结构表征,分析了钆配合物在水溶液中的粒径分布和Zeta电位,测试了钆配合物的体外弛豫率与新西兰大白兔体内肿瘤磁共振成像性能.与Gd-DTPA相比,所得钆配合物具有较高的弛豫率,对VX2肿瘤有良好的磁共振成像性能与靶向性,能对磁共振成像的对比度与清晰度有较好的提高.
The macromolecular ligand containing porphyrin groups(APTSPP-Dextran-DTPA)were synthesizedby the incorporation of water-soluble 5-(4′-aminophenyl)-10, 15, 20-tris(4′-sulfonatophenyl) porphyrintrisodium salt(APTSPP) and diethylenetriamine-pentaacetic acid(DTPA) to dextran. Dextran gadoliniumcomplex APTSPP-Dextran-DTPA-Gd was further prepared by the reaction of APTSPP-Dextran-DTPA. Theligand and gadolinium complex was characterized by Nuclear magnetic resonance hydrogen spectroscopy,Fourier transform infrared spectroscopy, and Ultraviolet spectroscopy. The relaxivity, magnetic resonanceimaging, average particle sizes and Zeta potential were evaluated in vitro and in vivo. Compared withGd-DTPA, the dextran gadolinium complex APTSPP-Dextran-DTPA-Gd shows high relaxation effectiveness andgood imaging performance, which improves the contrast and resolution of magnetic resonance imaging.