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Open AccessFeature PaperArticle

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

1
College of Pharmacy, Pusan National University, Busan 46241, Korea
2
College of Pharmacy, Kyunghee University, Seoul 02447, Korea
3
Center for Proteome Biophysics, Department of Chemistry, Pusan National University, Busan 46241, Korea
*
Author to whom correspondence should be addressed.
Mar. Drugs 2019, 17(6), 321; https://doi.org/10.3390/md17060321
Received: 10 May 2019 / Revised: 23 May 2019 / Accepted: 25 May 2019 / Published: 30 May 2019
(This article belongs to the Collection Marine Drugs in the Management of Metabolic Diseases)
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 investigate the anti-inflammatory effect of the PPAR-γ 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-α (TNF-α), possibly by the inhibition of the nuclear factor-κB (NF-κB) pathway. In macrophages, (+)-(R,E)-6a1 suppressed LPS-induced phosphorylation of NF-κB, inhibitor of NF-κB α (IκBα), and IκB kinase (IKK). These results indicated that PPAR-γ agonist, (+)-(R,E)-6a1, exerts anti-inflammatory activity via inhibition of the NF-κB pathway. View Full-Text
Keywords: PPAR-γ agonist; 15d-PGJ2; anti-inflammatory; NF-κB pathway PPAR-γ agonist; 15d-PGJ2; anti-inflammatory; NF-κB pathway
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Ju, Z.; Su, M.; Li, D.; Hong, J.; Im, D.-S.; Kim, S.; Kim, E.L.; Jung, J.H. An Algal Metabolite-Based PPAR-γ Agonist Displayed Anti-Inflammatory Effect via Inhibition of the NF-κB Pathway. Mar. Drugs 2019, 17, 321.

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