The synthesis and bioactivity of apigenin derivatives

Fitoterapia. 2024 Dec:179:106228. doi: 10.1016/j.fitote.2024.106228. Epub 2024 Sep 25.

Abstract

Background: Apigenin, a naturally occurring compound with a flavone core structure, is known for its diverse bioactivities, including anti-inflammation, anti-toxicant, anti-cancer and so on. There has been significant interest in the medicinal chemistry community. To address these challenges, researchers have developed various derivatives of apigenin to address challenges such as poor water-solubility and low intestinal absorption, aiming to enhance the pharmacological activities and pharmacokinetic properties of this compound.

Objective: In recent years, there has been a proliferation of apigenin derivatives with enhanced bioactivity. However, there is a lack of comprehensive reviews on the function-based modification of these derivatives. In this paper, we provide an overview of the apigenin derivatives with varying bioactivities and explored their structure activity relationships. And the functions of different groups of apigenin derivatives were also analyzed.

Conclusion: This review summarized the current achievements that could provide some clues for further study of apigenin-based drugs.

Keywords: Anti-bacterial activity; Anti-cancer; Anti-inflammatory; Apigenin; Biological activity; Synthesis.

Publication types

  • Review

MeSH terms

  • Animals
  • Anti-Inflammatory Agents* / chemistry
  • Anti-Inflammatory Agents* / pharmacology
  • Apigenin* / chemical synthesis
  • Apigenin* / chemistry
  • Apigenin* / pharmacology
  • Humans
  • Molecular Structure
  • Phytochemicals / pharmacology
  • Structure-Activity Relationship

Substances

  • Apigenin
  • Anti-Inflammatory Agents
  • Phytochemicals