Lobaric acid and pseudodepsidones inhibit NF-κB signaling pathway by activation of PPAR-γ
| Autor: | Jabrane Azelmat, Xavier Barbeau, Patrick Lagüe, Normand Voyer, Claudia Carpentier, Daniel Grenier, Katy Vaillancourt |
|---|---|
| Rok vydání: | 2018 |
| Předmět: |
Lipopolysaccharides
Lichens Cell Survival Clinical Biochemistry Pharmaceutical Science Peroxisome proliferator-activated receptor Lobaric acid Pharmacology Depsides 01 natural sciences Biochemistry Lactones Structure-Activity Relationship Drug Discovery Humans Structure–activity relationship Secretion Molecular Biology chemistry.chemical_classification Dose-Response Relationship Drug Molecular Structure U937 cell 010405 organic chemistry Chemistry Macrophages Anti-Inflammatory Agents Non-Steroidal Organic Chemistry NF-kappa B U937 Cells Salicylates 0104 chemical sciences Molecular Docking Simulation PPAR gamma Nf κb signaling 010404 medicinal & biomolecular chemistry Dose–response relationship Docking (molecular) Molecular Medicine Signal Transduction |
| Zdroj: | Bioorganic & Medicinal Chemistry. 26:5845-5851 |
| ISSN: | 0968-0896 |
| DOI: | 10.1016/j.bmc.2018.10.035 |
| Popis: | Herein we report the anti-inflammatory activity of lobaric acid and pseudodepsidones isolated from the nordic lichen Stereocaulon paschale. Lobaric acid (1) and three compounds (2, 7 and 9) were found to inhibit the NF-κB activation and the secretion of pro-inflammatory cytokines (IL-1β and TNF-α) in LPS-stimulated macrophages. Inhibition and docking simulation experiments provided evidence that lobaric acid and pseudodepsidones bind to PPAR-γ between helix H3 and the beta sheet, similarly to partial PPAR-γ agonists. These findings suggest that lobaric acid and pseudodepsidones reduce the expression of pro-inflammatory cytokines by blocking the NF-κB pathway via the activation of PPAR-γ. |
| Databáze: | OpenAIRE |
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