Folate-containing dextran ligand （FA-Dextran-DTPA） was synthesized by the incorporation of diethylenetriamine- pentaacetic acid （DTPA） and folate （FA） as a tumor-targeting group into dextran as a polymer carrier...Folate-containing dextran ligand （FA-Dextran-DTPA） was synthesized by the incorporation of diethylenetriamine- pentaacetic acid （DTPA） and folate （FA） as a tumor-targeting group into dextran as a polymer carrier. This ligand was further reacted with gadolinium chloride to make a dextran gadolinium complex FA-Dextran-DTPA-Gd. The ligand and its gadolinium complex were characterized by 1H-NMR, FTIR, UV-Vis, average particle sizes and zeta potential, as well. In vitro properties including relaxivity, cytotoxicity assay, cellular uptake assay, and magnetic resonance imaging （MRI） were also evaluated. Compared with Gd-DTPA, FA-Dextran-DTPA-Gd possessed obviously higher relaxation effectiveness and lower cytotoxicity to HeLa cells. FA-Dextran-DTPA-Gd had a high affinity to the H460 and MDA-MB-231 tumor cells and can be taken up selectively by these tumor cells. Moreover, FA-Dextran-DTPA-Gd showed enhanced signal intensities （SI） of MRI and enhanced the contrast of MR images of tumor cells. These results indicated that FA-Dextran-DTPA-Gd showed the potential as a tumor-targeting contrast agent in MRI.展开更多
基金financially supported by the National Natural Science Foundation of China(Nos.51173140 and 51373128)Wuhan Scientific and Technological Project(No.2013010501010131)+1 种基金Wuhan Science and Technology Innovation Team of Hi-tech Industrial Project,Hubei Province(No.2015070504020217)Innovation Fund for Post-graduate Education(Nos.CX2014058 and CX2013083),Wuhan Institute of Technology,China
文摘Folate-containing dextran ligand （FA-Dextran-DTPA） was synthesized by the incorporation of diethylenetriamine- pentaacetic acid （DTPA） and folate （FA） as a tumor-targeting group into dextran as a polymer carrier. This ligand was further reacted with gadolinium chloride to make a dextran gadolinium complex FA-Dextran-DTPA-Gd. The ligand and its gadolinium complex were characterized by 1H-NMR, FTIR, UV-Vis, average particle sizes and zeta potential, as well. In vitro properties including relaxivity, cytotoxicity assay, cellular uptake assay, and magnetic resonance imaging （MRI） were also evaluated. Compared with Gd-DTPA, FA-Dextran-DTPA-Gd possessed obviously higher relaxation effectiveness and lower cytotoxicity to HeLa cells. FA-Dextran-DTPA-Gd had a high affinity to the H460 and MDA-MB-231 tumor cells and can be taken up selectively by these tumor cells. Moreover, FA-Dextran-DTPA-Gd showed enhanced signal intensities （SI） of MRI and enhanced the contrast of MR images of tumor cells. These results indicated that FA-Dextran-DTPA-Gd showed the potential as a tumor-targeting contrast agent in MRI.
