摘要
为提高小檗碱的水溶性以及降糖活性,对其C-9位进行了结构修饰,合成了6个9-O-小檗碱酯类衍生物(3a~3f),其中3b~3d和3f为新化合物,其结构经~1H NMR,IR和HR-MS (ESI)表征。选用人肝癌细胞(HepG2)建立胰岛素抵抗模型(HepG2-IR),通过MTT法研究了3a~3f的体外降糖活性。结果表明:3a~3f均具有不同程度的降糖活性,其中化合物3a(IC_(50)=0. 044±0. 97 mg·L~(-1))在低浓度0. 08 mg·L~(-1)时,对HepG2-IR细胞葡萄糖消耗量为3. 5 mM,优于小檗碱(2. 75 mM)。
In order to improve the water solubility and hypoglycemic activity of berberine,six berberine derivatives( 3a ~ 3f) were synthesized by structural modifications. Among them,3b ~ 3d and 3f were new compounds. The structures were characterized by ~1H NMR,IR and HR-MS( ESI). The in vitro hypoglycemic activities of 3a ~ 3f in establishing insulin resistance model( HepG2-IR) by Human hepatoma cell( HepG2) were determined by MTT method. The results showed that 3a ~ 3f had different levels of hypoglycemic activity,compound 3a( IC50= 0. 044 + 0. 68 mg·L~(-1)) consumed 3. 5 mM glucose for HepG2-IR cells at low concentration of 0. 08 mg·L~(-1),which was better than berberine( 2. 75 mM).
引文
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