半乳糖化壳聚糖-氟尿嘧啶偶合物的合成与表征  

Synthesis and Characterization of N-Galactosylated-Chitosan-5-Fluorouracil Acetic Acid Conjugate

作　　者：梁美好[1] 马臻[1] 王尊元[1] 沈正荣[1] 

机构地区：[1]浙江省医学科学院,杭州310013

出　　处：《中国药学杂志》2011年第21期1677-1680,共4页Chinese Pharmaceutical Journal

基　　金：浙江省自然科学基金(Y207790);浙江省科技厅青年基金项目(2006R20004)

摘　　要：目的合成肝靶向大分子前药半乳糖化壳聚糖-氟尿嘧啶偶合物(GC-FUA)。方法将乳糖酸以酰胺键偶合到壳聚糖(CS)上,得到半乳糖化壳聚糖(GC),再将经溴乙酸修饰的氟尿嘧啶(FUA)键合到GC上,得到目标产物GC-FUA,通过NMR和FT-IR对结构进行表征,并用1H-NMR测定乳糖酰基取代度(DSGC)和FUA取代度(DSFUA)。结果通过控制反应条件得到了乳糖酰基取代度不同的高分子载体GC,以及FUA取代度不同的偶合物GC-FUA。结论成功地合成了肝靶向大分子前药GC-FUA。OBJECTIVE To synthesize a liver-targeting prodrug named N-galactosylated-chitosan-5-fluorouracil acetic acid conjugate （GC-FUA）. METHODS Lactobionic acid was firstly coupled with chitosan （ CS）, and then reacted with 5-fluorouracil acetic acid （FUA） modified with bromoacetate. The structure was confirmed by NMR and FT-IR. The degrees of substitution （DS） of lacto- syl group and FUA moiety were calculated by 1H-NMR. RESULTS GC-FUA with different DS of lactosyl group and FUA moiety were synthesized via different reaction conditions. CONCLUSION The liver-targeting polymeric prodrug was obtained successfully.

关 键 词：壳聚糖 去唾液酸糖蛋白受体 5-氟尿嘧啶 大分子药物 

分 类 号：R914[医药卫生—药物化学]