Chinese Journal of Organic Chemistry ›› 2023, Vol. 43 ›› Issue (4): 1325-1340.DOI: 10.6023/cjoc202209037 Previous Articles     Next Articles



刘兴周a, 于明加a,*(), 梁建华a,b,*()   

  1. a 北京理工大学化学与化工学院 医药分子科学与制剂工程工信部重点实验室 北京 102488
    b 北京理工大学长三角研究院(嘉兴) 浙江嘉兴 314019
  • 收稿日期:2022-09-29 修回日期:2022-10-27 发布日期:2022-11-21
  • 通讯作者: 于明加, 梁建华
  • 基金资助:

Research Progress on the Synthesis of Protoberberine Skeleton and Its Anti-inflammatory Activity

Xingzhou Liua, Mingjia Yua(), Jianhua Lianga,b()   

  1. a Key Laboratory of Medical Molecule Science and Pharmaceutics Engineering, Ministry of Industry and Information Technology, School of Chemistry and Chemical Engineering, Beijing Institute of Technology, Beijing 102488
    b Yangtze Delta Region Academy of Beijing Institute of Technology, Jiaxing, Zhejiang 314019
  • Received:2022-09-29 Revised:2022-10-27 Published:2022-11-21
  • Contact: Mingjia Yu, Jianhua Liang
  • Supported by:
    National Natural Science Foundation of China(21878022)

The protoberberine alkaloids, exampled by berberine, have abundant biological activities, which show excellent anti-inflammatory effects in a variety of inflammatory diseases such as epilepsy and cardiovascular and cerebrovascular diseases. Due to the challenge in separation and purification of protoberberines from natural resource and intrinsic low bioavailability, many researchers have devoted to the discovery of new total synthesis methods or structural modification. The total synthesis, anti-inflammatory pathway and anti-inflammatory structure-activity relationships of protoberberine skeleton are summarized for the discovery of de novo protoberberine chemotypes with anti-inflammatory activity.

Key words: protoberberine alkaloids, berberine, total synthesis, anti-inflammatory pathway, structure-activity relationships