National Engineering Research Center for Biomaterials, Sichuan University, Chengdu 610064, PR China.
Macromol Biosci. 2009 Dec 8;9(12):1227-36. doi: 10.1002/mabi.200900231.
Liver-imaging probes are prepared through the conjugation of Gd chelates and galactosyl moieties to peptide dendrimers. The dendritic probes possessing highly controlled structures and a single molecular weight have a two-fold increase in T(1) relaxivity to 9.1 x 10(3) (Gd M)(-1) s(-1) compared to Gd-DTPA. No obvious cytotoxicity of this multifunctional dendritic agent is discovered in vitro. The dendrimer bearing galactosyl moieties leads to a much-higher hepatocyte-cell uptake in vitro and provides good signal-intensity enhancement (35%) of mouse liver in vivo especially at 60 min after intravenous injection. In comparison, non-targeting Gd dendrimers provide only an 11% enhancement of imaging contrast at the same time point. Overall, the dendrimers bearing galactosyl moieties may be used as liver-imaging probes.
肝脏成像探针通过将 Gd 螯合物和半乳糖基部分连接到肽树枝状大分子上来制备。与 Gd-DTPA 相比，具有高度可控结构和单一分子量的树枝状探针的 T(1)弛豫率提高了一倍，达到 9.1 x 10(3)(Gd M)(-1) s(-1)。体外未发现这种多功能树枝状试剂有明显的细胞毒性。带有半乳糖基部分的树枝状聚合物导致体外肝细胞摄取率大大提高，并在体内（特别是静脉注射后 60 分钟）提供良好的信号强度增强（35%）。相比之下，在相同时间点，非靶向 Gd 树枝状聚合物仅提供 11%的成像对比度增强。总的来说，带有半乳糖基部分的树枝状聚合物可用作肝脏成像探针。
