Structurally modified glycyrrhetinic acid derivatives as anti-inflammatory agents

Bioorg Chem. 2021 Feb:107:104598. doi: 10.1016/j.bioorg.2020.104598. Epub 2020 Dec 29.

Abstract

With the aim of finding new anti-inflammatory drugs, a series of new Glycyrrhetinic acid derivatives (1-34) have been designed and synthesized by structural modification, and their anti-inflammatory activities in vitro have been evaluated. The anti-inflammatory activities assay demonstrated that compound 5b suppressed the expression of pro-inflammatory cytokines including IL-6, TNF-α and NO, it also suppressed the expression of iNOS and COX-2 in LPS-induced RAW264.7 cells in a dose-dependent manner. Additionally, western blot results indicated that the suppressing effect of compound 5b on pro-inflammatory cytokines were correlated with the suppression of NF-κB and MAPK signaling pathways. The results attained in this study indicated that compound 5b had the potential to be developed into an anti-inflammation agent and it may be applied to the prevention and treatment of inflammatory diseases.

Keywords: Anti-inflammatory; Glycyrrhetinic acid; Structural modification; Synthesis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / chemical synthesis
  • Anti-Inflammatory Agents / chemistry
  • Anti-Inflammatory Agents / pharmacology*
  • Cell Survival / drug effects
  • Cells, Cultured
  • Cytokines / antagonists & inhibitors
  • Cytokines / biosynthesis
  • Dose-Response Relationship, Drug
  • Glycyrrhetinic Acid / chemical synthesis
  • Glycyrrhetinic Acid / chemistry
  • Glycyrrhetinic Acid / pharmacology*
  • Lipopolysaccharides / antagonists & inhibitors
  • Lipopolysaccharides / pharmacology
  • Mice
  • Molecular Structure
  • Nitric Oxide / antagonists & inhibitors
  • Nitric Oxide / biosynthesis
  • RAW 264.7 Cells
  • Structure-Activity Relationship

Substances

  • Anti-Inflammatory Agents
  • Cytokines
  • Lipopolysaccharides
  • Nitric Oxide
  • Glycyrrhetinic Acid