4.7 Article

Structurally modified glycyrrhetinic acid derivatives as anti-inflammatory agents

Journal

BIOORGANIC CHEMISTRY
Volume 107, Issue -, Pages -

Publisher

ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2020.104598

Keywords

Synthesis; Glycyrrhetinic acid; Structural modification; Anti-inflammatory

Funding

  1. National Natural Science Funding of China [81960626]
  2. Inner Mongolia Natural Science Foundation [2020BS08013]

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A series of new Glycyrrhetinic acid derivatives were designed and synthesized to find new anti-inflammatory drugs. Compound 5b showed strong anti-inflammatory activity by suppressing the expression of pro-inflammatory cytokines and regulating NF-kappa B and MAPK signaling pathways.
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-alpha 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-kappa B 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.

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