小檗碱作为一种生物碱具有重要的医用价值,已广泛的应用于消炎、降血脂、降血糖、抗癌等诸多方面,而大量药理研究进一步表明:对其结构进行修饰改造可以提高其生物活性,使其具有更加优秀的药用功效,更加易于临床使用.同时,大量小檗碱衍生物的合成可望进一步深入了解小檗碱作用于人体的生物机制,以便进一步扩展其应用范围.介绍了近年小檗碱结构修饰研究进展,重点介绍在其分子结构中N(7)、C(8)、C(9)、C(12)和C(13)位点的结构修饰方法.此外,还介绍了修饰后生物活性的变化,以及一些具有较好生物活性的小檗碱衍生物,旨在为进一步深入开展以药效机制为基础的小檗碱结构改造和创新药物研究提供重要的参考信息.%Berberine as an alkaloid has been widely applied in fields of anti-inflammatory anti-hyperlipidemia, anti-hypoglycemia and anti-cancer. A large number of pharmacological studies demonstrated that the structural modification of berberine could improve its biological activity with excellent medicinal efficacy in clinical applications. Meanwhile,the numerous syntheses of berberine derivatives are expected to help people further understand the biological mechanism of berberine on the human body,and extend the application ranges of berberine. By reviewing the research progress of structural modification of berberine,this paper focuses on the structural modification method for N(7),C(8),C(9),C(12)and C(13)sites in the molecular structures. Besides,the modified biological activity and the berberine derivatives with better bioactivity are introduced, providing systematic information for further studies on structural modification of berberine for developing new drug based on its pharmacodynamic mechanisms.
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