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Molecules 2017, 22(11), 1977; doi:10.3390/molecules22111977

Anti-Inflammatory Potential of 1-Nitro-2-Phenylethylene

1
Laboratory of Inflammation Signaling, Department of Clinical Analysis, Faculty of Pharmacy, Federal University of Minas Gerais, Belo Horizonte 31270-901, MG, Brazil
2
Laboratory of Biological Activity, Faculty of Pharmaceutical Sciences, Federal University of Amazonas, Manaus 69067-005, AM, Brazil
3
Nucleus of Studies and Selection of Bioactive Molecules, Institute of Health Sciences, Federal University of Pará, Belém 66075-110, PA, Brazil
4
Department of Physiology and Biophysics, Institute of Biological Sciences, Federal University of Minas Gerais, Belo Horizonte 31270-901, MG, Brazil
5
Laboratory of Research in Drugs, Department of Biological Sciences and Health, Federal University of Amapá, Macapá 68903-419, AP, Brazil
*
Author to whom correspondence should be addressed.
Received: 4 September 2017 / Revised: 6 November 2017 / Accepted: 10 November 2017 / Published: 15 November 2017
(This article belongs to the Special Issue Anti-inflammatory Agents)
View Full-Text   |   Download PDF [1679 KB, uploaded 15 November 2017]   |  

Abstract

Inflammation is a reaction of the host to infectious or sterile stimuli and has the physiological purpose of restoring tissue homeostasis. However, uncontrolled or unresolved inflammation can lead to tissue damage, giving rise to a plethora of chronic inflammatory diseases, including metabolic syndrome and autoimmunity pathologies with eventual loss of organ function. Beta-nitrostyrene and its derivatives are known to have several biological activities, including anti-edema, vasorelaxant, antiplatelet, anti-inflammatory, and anticancer. However, few studies have been carried out regarding the anti-inflammatory effects of this class of compounds. Thereby, the aim of this study was to evaluate the anti-inflammatory activity of 1-nitro-2-phenylethene (NPe) using in vitro and in vivo assays. Firstly, the potential anti-inflammatory activity of NPe was evaluated by measuring TNF-α produced by human macrophages stimulated with lipopolysaccharide (LPS). NPe at non-toxic doses opposed the inflammatory effects induced by LPS stimulation, namely production of the inflammatory cytokine TNF-α and activation of NF-κB and ERK pathways (evaluated by phosphorylation of inhibitor of kappa B-alpha [IκB-α] and extracellular signal-regulated kinase 1/2 [ERK1/2], respectively). In a well-established model of acute pleurisy, pretreatment of LPS-challenged mice with NPe reduced neutrophil accumulation in the pleural cavity. This anti-inflammatory effect was associated with reduced activation of NF-κB and ERK1/2 pathways in NPe treated mice as compared to untreated animals. Notably, NPe was as effective as dexamethasone in both, reducing neutrophil accumulation and inhibiting ERK1/2 and IκB-α phosphorylation. Taken together, the results suggest a potential anti-inflammatory activity for NPe via inhibition of ERK1/2 and NF-κB pathways on leukocytes. View Full-Text
Keywords: 1-nitro-2-phenylethylene; anti-inflammatory activity; TNF-α production 1-nitro-2-phenylethylene; anti-inflammatory activity; TNF-α production
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Sugimoto, M.A.; de Jesus Amazonas da Silva, M.; Froede Brito, L.; dos Santos Borges, R.; Amaral, F.A.; de Araujo Boleti, A.P.; Ordoñez, M.E.; Carlos Tavares, J.; Pires Sousa, L.; Lima, E.S. Anti-Inflammatory Potential of 1-Nitro-2-Phenylethylene. Molecules 2017, 22, 1977.

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