Abstract
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.
Copyright © 2018 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Anti-Inflammatory Agents, Non-Steroidal / chemistry
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Anti-Inflammatory Agents, Non-Steroidal / isolation & purification
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Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
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Cell Survival / drug effects
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Depsides / chemistry
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Depsides / isolation & purification
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Depsides / pharmacology*
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Dose-Response Relationship, Drug
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Humans
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Lactones / chemistry
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Lactones / isolation & purification
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Lactones / pharmacology*
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Lichens / chemistry*
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Lipopolysaccharides / antagonists & inhibitors
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Lipopolysaccharides / pharmacology
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Macrophages / drug effects
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Molecular Docking Simulation
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Molecular Structure
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NF-kappa B / antagonists & inhibitors*
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NF-kappa B / metabolism
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PPAR gamma / agonists*
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PPAR gamma / metabolism
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Salicylates / chemistry
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Salicylates / isolation & purification
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Salicylates / pharmacology*
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Signal Transduction / drug effects
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Structure-Activity Relationship
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U937 Cells
Substances
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Anti-Inflammatory Agents, Non-Steroidal
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Depsides
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Lactones
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Lipopolysaccharides
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NF-kappa B
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PPAR gamma
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Salicylates
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lobaric acid