Synthesis of Lathyrol PROTACs and Evaluation of Their Anti-Inflammatory Activities

J Nat Prod. 2023 Apr 28;86(4):767-781. doi: 10.1021/acs.jnatprod.2c00912. Epub 2023 Mar 31.

Abstract

Lathyrol is a core scaffold structure of many lathyrane diterpenoids with potent anti-inflammatory activity isolated from Euphorbia lathyrism. It was chosen as a framework to design and synthesize a series of proteolysis targeting chimeras. A total of 15 derivatives were obtained. Compound 13 exhibited inhibitory activity on LPS-induced NO production in RAW264.7 cells (IC50 = 5.30 ± 1.23 μM) with low cytotoxicity. Furthermore, compound 13 significantly degraded v-maf musculoaponeurotic fibrosarcoma oncogene homologue F (MAFF) protein, a target of lathyrane diterpenoid, concentration- and time-dependently. The mechanism of action of 13 is related to activating the Keap1/Nrf2 pathway. It also inhibited the expression of NF-κB, blocked the nuclear translocation of NF-κB, and activated autophagy in LPS-induced RAW264.7 cells. Based on the results obtained, compound 13 might be a promising anti-inflammatory agent.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / chemistry
  • Anti-Inflammatory Agents / pharmacology
  • Kelch-Like ECH-Associated Protein 1 / metabolism
  • Lipopolysaccharides / pharmacology
  • Mice
  • NF-E2-Related Factor 2 / metabolism
  • NF-kappa B* / metabolism
  • Nitric Oxide
  • Proteolysis Targeting Chimera*
  • RAW 264.7 Cells

Substances

  • lathyrane
  • NF-kappa B
  • Kelch-Like ECH-Associated Protein 1
  • Proteolysis Targeting Chimera
  • Lipopolysaccharides
  • NF-E2-Related Factor 2
  • Anti-Inflammatory Agents
  • Nitric Oxide