半乳糖化季铵壳聚糖衍生物的设计、合成和表征

Design,synthesis and characterization of N-trimethyl chitosan derivatives having pendant galactose residues

目的合成和表征半乳糖化季铵壳聚糖衍生物作为潜在的肝靶向基因载体。方法以天然聚合物壳聚糖为原料,首先制备季铵化壳聚糖,然后在其2-NH2上和乳糖酸反应,或与乳糖反应,用KBH4还原,制备得到未见文献报道的半乳糖化季铵壳聚糖衍生物。分别用FTIR,1H NMR,13C NMR和元素分析对其进行了表征。结果与结论半乳糖化季铵壳聚糖衍生物有望作为潜在的肝靶向基因载体。

OBJECTIVE To synthesize and characterize N-trimethyl chitosan derivatives having pendant galactose residues for potential gene delivery carriers for hepatocyte-targeting. METHOD Firstly, a water-soluble N-trimethyl chitosan derivatives （TMCS） was prepared. To give galactosylated N-trimethyl chitosan （Gal-TMCS） , lactobionic acid was added and galactose group was introduced into the amino groups of TMCS. Lactosaminated N-trimethyl chitosan （Lac-TMCS） was prepared by reaction of TMCS and α-lactose,followed by reaction with KBH4. RESULTS FFIR, ^1H NMR, ^13C NMR and elemental analysis characterized the chemical structures of N-trimethyl chitosan derivatives having pendant galactose residues. CONCLUSION may be used as potential gene delivery carriers for hepatocyte-targeting.