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An Algal Metabolite-Based PPAR-? Agonist Displayed Anti-Inflammatory Effect via Inhibition of the NF-?B Pathway.

ABSTRACT: In our previous study, a synthetic compound, (+)-(R,E)-6a1, that incorporated the key structures of anti-inflammatory algal metabolites and the endogenous peroxisome proliferator-activated receptor ? (PPAR-?) ligand 15-deoxy-?^12,14-prostaglandin J₂ (15d-PGJ₂), exerted significant PPAR-? transcriptional activity. Because PPAR-? expressed in macrophages has been postulated as a negative regulator of inflammation, this study was designed to investigate the anti-inflammatory effect of the PPAR-? agonist, (+)-(R,E)-6a1. Compound (+)-(R,E)-6a1 displayed in vitro anti-inflammatory activity in lipopolysaccharides (LPS)-stimulated murine RAW264.7 macrophages. Compound (+)-(R,E)-6a1 suppressed the expression of proinflammatory factors, such as nitric oxide (NO), inducible NO synthase (iNOS), cyclooxygenase-2 (COX-2), interleukin-6 (IL-6), and tumor necrosis factor-? (TNF-?), possibly by the inhibition of the nuclear factor-?B (NF-?B) pathway. In macrophages, (+)-(R,E)-6a1 suppressed LPS-induced phosphorylation of NF-?B, inhibitor of NF-?B ? (I?B?), and I?B kinase (IKK). These results indicated that PPAR-? agonist, (+)-(R,E)-6a1, exerts anti-inflammatory activity via inhibition of the NF-?B pathway.

SUBMITTER: Ju Z

PROVIDER: S-EPMC6627743 | biostudies-literature | 2019 May

REPOSITORIES: biostudies-literature

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An Algal Metabolite-Based PPAR-γ Agonist Displayed Anti-Inflammatory Effect via Inhibition of the NF-κB Pathway.

Ju Zhiran Z Su Mingzhi M Li Dandan D Hong Jongki J Im Dong-Soon DS Kim Suhkmann S Kim Eun La E Jung Jee H JH

Marine drugs 20190530 6

In our previous study, a synthetic compound, (+)-(R,E)-6a1, that incorporated the key structures of anti-inflammatory algal metabolites and the endogenous peroxisome proliferator-activated receptor γ (PPAR-γ) ligand 15-deoxy-∆12,14-prostaglandin J2 (15d-PGJ2), exerted significant PPAR-γ transcriptional activity. Because PPAR-γ expressed in macrophages has been postulated as a negative regulator of inflammation, this study was designed to inve ...[more]

PMID: 31151271

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An Algal Metabolite-Based PPAR-? Agonist Displayed Anti-Inflammatory Effect via Inhibition of the NF-?B Pathway.

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An Algal Metabolite-Based PPAR-γ Agonist Displayed Anti-Inflammatory Effect via Inhibition of the NF-κB Pathway.

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