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1. 武汉工程大学材料科学与工程学院,武汉,430074
2. 华中科技大学同济医学院附属协和医院PET中心,武汉,430022
纸质出版日期:2014-2-20,
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李倩, 韩林, 鄢国平, 涂园园, 袁辉, 邹头君, 邵春桃, 刘慧芳. 含磺胺嘧啶基团的葡聚糖钆配合物的研究[J]. 高分子学报, 2014,(2):263-269.
Qian Li, Lin Han, Guo-ping Yan, Yuan-yuan Tu, Hui Yuan, Tou-jun Zou, Chun-tao Shao, Hui-fang Liu. Studies on Dextran Gadolinium Complex Containing Sulfadiazine Groups[J]. Acta Polymerica Sinica, 2014,(2):263-269.
李倩, 韩林, 鄢国平, 涂园园, 袁辉, 邹头君, 邵春桃, 刘慧芳. 含磺胺嘧啶基团的葡聚糖钆配合物的研究[J]. 高分子学报, 2014,(2):263-269. DOI: 10.3724/SP.J.1105.2014.13288.
Qian Li, Lin Han, Guo-ping Yan, Yuan-yuan Tu, Hui Yuan, Tou-jun Zou, Chun-tao Shao, Hui-fang Liu. Studies on Dextran Gadolinium Complex Containing Sulfadiazine Groups[J]. Acta Polymerica Sinica, 2014,(2):263-269. DOI: 10.3724/SP.J.1105.2014.13288.
将具有肿瘤靶向性的磺胺嘧啶(SD)、二乙三胺五乙酸(DTPA)与葡聚糖(dextran)大分子侧链羟基偶联,合成葡聚糖大分子配体(SD-Dextran-DTPA),再与金属钆离子Gd3+配合,从而制备肿瘤靶向性葡聚糖大分子钆配合物(SD-Dextran-DTPA-Gd).对所合成的配体及钆配合物进行FTIR、UV和1H-NMR等结构表征,测试了配体及钆配合物在水溶液中的粒径分布和zeta电位、钆配合物的体外弛豫率、细胞摄取与T1加权磁共振成像性能.与小分子钆-二乙三胺五乙酸(Gd-DTPA)相比,SD-Dextran-DTPA-Gd具有较高的弛豫率,对肺癌细胞系H460、乳腺癌细胞系MDA-MB-231和T40D均有较好的亲和性,可被肿瘤细胞较好地摄取,并能获得较好的肿瘤细胞磁共振成像.
Sulfadiazine-containing dextran ligand (SD-Dextran-DTPA) was synthesized by the incorporation of diethylenetriaminepentaacetic acid (DTPA) and sulfadiazine (SD) as a tumor-targeting group into dextran. This ligand was further reacted with gadolinium chloride to produce tumor-targeting macromolecule gadolinium complex (SD-Dextran-DTPA-Gd). Experimental data of 1H-NMR
IR
UV
average particle sizes and zeta potential evidenced the formation of the dextran ligand and gadolinium complex. In vitro properties including the relaxivity
cell uptake assay and magnetic resonance imaging were also evaluated. In the aqueous solutions
the average diameter of the dextran ligand SD-Dextran-DTPA and complex SD-Dextran-DTPA-Gd increased when the concentration of their solutions decreased. Compared with Gd-DTPA
this tumor-targeting dextran gadolinium complex SD-Dextran-DTPA-Gd possessed obviously higher relaxation effectiveness due to a slowly tumbling system and an increase in rotational correlation time. The cell uptake assay indicated that SD-Dextran-DTPA-Gd had a high affinity to the H460
MDA-MB-231 and T40D tumor cells and can be taken up selectively by these tumor cells. Magnetic resonance imaging (MRI) tests showed that SD-Dextran-DTPA-Gd possessed the relaxation effectiveness higher than that of Gd-DTPA and can enhance the contrast of MR images of the tumor cells. Moreover
the T1 signal intensities of the MDA-MB-231 cell suspensions were obviously higher than those of the H460 and T40D cell suspensions. Therefore SD-Dextran-DTPA-Gd has shown the potential as a tumor-targeting contrast agent in MRI.
磁共振成像造影剂肿瘤靶向葡聚糖磺胺嘧啶细胞摄取二乙三胺五乙酸
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