单甲氧基聚乙二醇修饰白藜芦醇的初步研究

Preparation of resveratrol modified with mPEG-5000

采用以琥珀酸酐和氯化亚砜活化的单甲氧基聚乙二醇,对白藜芦醇进行了化学修饰,以期改善其水溶性并增加其稳定性。通过官能团反应,白藜芦醇分子接上单甲氧基聚乙二醇分子,合成出一种枝化白藜芦醇单甲氧基聚乙二醇衍生物;对单甲氧基聚乙二醇端羟基依次进行羧基化、酰氯华等活化处理,通过酰氯与羟基的官能团反应合成出目标分子。应用透析方法分离纯化得到修饰产物,通过红外光谱分析、紫外光谱分析、HPLC分析,证实了产物与目标分子的结构相吻合。

A kind of monomethoxypolyethylene glycol was used to modify resveratrol and the optimal modification factors were got.A novel type branched macromolecule was synthesized from the resveratrol and the monomethoxypoly （ethylene glycol,（mPEG）.mPEG was activated by changing hydroxide teminal into acid chloride and carboxylation of mPEG was fulfilled before.The amino group was reserved so that it could be used as functional radical to modify resveratrol later.The mono-PEGylated product was isolated from the reaction mixture by the measure of dialyze.The PEGylated resveratrol showed better stability,and its dissolve trait was better enhanced.