Current development and structure-activity relationship study of berberine derivatives

Bioorg Med Chem. 2024 Oct 1:112:117880. doi: 10.1016/j.bmc.2024.117880. Epub 2024 Aug 17.

Abstract

Berberine is a quaternary ammonium isoquinoline alkaloid derived from traditional Chinese medicines Coptis chinensis and Phellodendron chinense. It has many pharmacological activities such as hypoglycemic, hypolipidemic, anti-tumor, antimicrobial and anti-inflammatory. Through structural modifications at various sites of berberine, the introduction of different groups can change berberine's physical and chemical properties, thereby improving the biological activity and clinical efficacy, and expanding the scope of application. This paper reviews the research progress and structure-activity relationships of berberine in recent years, aiming to provide valuable insights for the exploration of novel berberine derivatives.

Keywords: Berberine; Biological activities; Structural modification; Structure-activity relationships.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology
  • Berberine* / analogs & derivatives
  • Berberine* / chemistry
  • Berberine* / pharmacology
  • Humans
  • Hypoglycemic Agents / chemical synthesis
  • Hypoglycemic Agents / chemistry
  • Hypoglycemic Agents / pharmacology
  • Molecular Structure
  • Structure-Activity Relationship

Substances

  • Berberine
  • Hypoglycemic Agents
  • Antineoplastic Agents