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Mar. Drugs 2017, 15(1), 7; doi:10.3390/md15010007

The In Vitro and In Vivo Anti-Inflammatory Effects of a Phthalimide PPAR-γ Agonist

College of Pharmacy, Pusan National University, Busan 609-735, Korea
These authors equally contributed to this work.
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Authors to whom correspondence should be addressed.
Academic Editor: Peer B. Jacobson
Received: 25 October 2016 / Revised: 5 December 2016 / Accepted: 9 December 2016 / Published: 4 January 2017
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Abstract

Previously, the authors found that 4-hydroxy-2-(4-hydroxyphenethyl) isoindoline-1,3-dione (PD1) (a phthalimide analogue) bound to and activated peroxisome proliferator-activated receptor-γ (PPAR-γ). Since PPAR-γ suppresses inflammatory responses, the present study was undertaken to investigate the anti-inflammatory effects of PD1. In lipopolysaccharide (LPS)-stimulated murine RAW264.7 macrophages, PD1 suppressed the inductions of pro-inflammatory factors, including inducible nitric oxide synthase (iNOS), nitric oxide (NO), cyclooxygenase 2 (COX-2), tumor necrosis factor α (TNF-α), interleukin-1β (IL-1β), and interleukin-6 (IL-6). Concomitantly, PD1 enhanced the expressions of anti-inflammatory factors, such as arginase-1 and interleukin-10 (IL-10), and suppressed LPS-evoked nuclear factor kappa B (NF-κB) p65 subunit phosphorylation in macrophages. In addition, PPAR-γ activated by PD1 was intensively translocated to the nucleus. These observations suggest that the anti-inflammatory mechanism of PD1 involves inhibition of the NF-κB pathway. In a subsequent in vivo animal experiment conducted using a carrageenan-induced acute inflammatory rat paw edema model, intraperitoneal injection of PD1 significantly reduced paw swelling. Histological analysis of rat paw tissue sections revealed less infiltration of immune cells in PD1-pretreated animals. These findings suggest that PD1 be viewed as a lead compound for the development of novel anti-inflammatory therapeutics. View Full-Text
Keywords: anti-inflammatory effect; PPAR-γ agonist; phthalimide analogue; RAW264.7 macrophage; cytokines; NF-κB pathway; paw edema anti-inflammatory effect; PPAR-γ agonist; phthalimide analogue; RAW264.7 macrophage; cytokines; NF-κB pathway; paw edema
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MDPI and ACS Style

Su, M.; Cao, J.; Huang, J.; Liu, S.; Im, D.S.; Yoo, J.-W.; Jung, J.H. The In Vitro and In Vivo Anti-Inflammatory Effects of a Phthalimide PPAR-γ Agonist. Mar. Drugs 2017, 15, 7.

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