Structurally modified glycyrrhetinic acid derivatives as anti-inflammatory agents

[Display omitted] •34 glycyrrhetinic acid derivatives were obtained by four structural modification methods.•The anti-inflammatory activity of compound 5b was significantly higher than glycyrrhetinic acid.•MAPK and NF-κB signaling pathways were involved in the anti-inflammatory process of compound 5b. 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.