摘要
为了改善姜黄素(1)的水溶性及其肿瘤给药的靶向性,通过DCC/DMAP偶联法,分别将葡萄糖和1引入双端羧基化的聚乙二醇(PEG)链两端,构建了葡萄糖靶向聚乙二醇支载姜黄素[葡萄糖-聚乙二醇-姜黄素(4)],其结构经1H NMR和IR表征。用UV测定了4中1的含量及其在缓冲溶液中的稳定性。结果表明,当用PEG2000,PEG4000,PEG6000时,4中1的水溶解度分别为651.6μg.mL-1,533.3μg.mL-1,258.4μg.mL-1;4在pH 7.4的缓冲溶液中浸泡26h时,4中1的质量损失分别为19.05%,26.33%,49.96%,即PEG支载可显著改善1的水溶性和稳定性。
In order to improve the water-solubility and tumor-targeted of curcumin（1）,glucose and 1 were conjugated into chain segment of carboxylated PEG by DCC/DMAP crosslinking to construct Glu-PEG-1（4）.The sturctures were charactered by 1H NMR and IR.The content,water-solubility and stability of 1 in 4 were investigated by UV.The results showed that the water-solubility of 1,which was modified by PEG 2000,PEG 4000,PEG 6000,was 651.6 μg·mL-1,533.3 μg·mL-1 and 258.4 μg·mL-1,respectively,and the mass lose of 1 in buffer solution of pH 7.4 for 26 h was 19.05%,26.33% and 49.96%,respectively.After modified by PEG,the water-solubility and stability of 1 were obviously improved.
出处
《合成化学》
CAS
CSCD
北大核心
2011年第1期15-18,55,共5页
Chinese Journal of Synthetic Chemistry
基金
国家自然科学基金资助项目(30972423)
中央高校基本科研业务费专项资金资助项目(09029
DL10BB26)
