Berberine Derivatives with Different Pharmacological Activities via Structural Modifications

Mini Rev Med Chem. 2018;18(17):1424-1441. doi: 10.2174/1389557517666170321103139.


Berberine, a quaternary ammonium protoberberine alkaloid with an isoquinoline scaffold isolated from medicinal herbs, exhibits a wide spectrum of pharmacological activities. Berberine has been used in traditional Chinese medicine and Ayurvedic medicine. However, it has poor bioavailability, which seriously limits its application and development. The chemical transformation of natural products is an effective method to improve pharmacological activities. Researches have been carried out on the modification of berberine to obtain better pharmacological properties. In this paper, the structural modifications of berberine for different biological activities and its underlying mechanisms are reviewed.

Keywords: Berberine; bioavailability; chemical transformation; mechanisms; pharmacological activities; structural modification..

Publication types

  • Review

MeSH terms

  • Alzheimer Disease / drug therapy
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • Anti-Inflammatory Agents, Non-Steroidal / chemistry
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
  • Antimalarials / chemistry
  • Antimalarials / pharmacology*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Bacteria / drug effects
  • Berberine / analogs & derivatives
  • Berberine / chemistry
  • Berberine / pharmacology*
  • Humans
  • Medicine, Chinese Traditional
  • Molecular Structure
  • Neuroprotective Agents / chemistry
  • Neuroprotective Agents / pharmacology*
  • Plants, Medicinal / chemistry


  • Anti-Bacterial Agents
  • Anti-Inflammatory Agents, Non-Steroidal
  • Antimalarials
  • Antineoplastic Agents
  • Neuroprotective Agents
  • Berberine