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Molecules 2016, 21(4), 508;

1-(2,3-Dibenzimidazol-2-ylpropyl)-2-methoxybenzene Is a Syk Inhibitor with Anti-Inflammatory Properties

Department of Genetic Engineering, Sungkyunkwan University, Suwon 16419, Korea
Department of Pharmacy, Sunchon National University, Suncheon 57922, Korea
Medical College, Qingdao University, Qingdao 266071, China
Jiangsu Collaborative Innovation Center of Regional Modern Agriculture & Environmental Protection/Jiangsu Key Laboratory for Eco-Agricultural Biotechnology around Hongze Lake, Huaiyin Normal University, Huaian 223300, China
College of Pharmacy and Yonsei Institute of Pharmaceutical Sciences, Yonsei University, Incheon 21983, Korea
Department of Physiology, College of Veterinary Medicine, Chonbuk National University, Iksan 54596, Korea
These authors are equally contributed to this work.
Authors to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 4 March 2016 / Revised: 12 April 2016 / Accepted: 14 April 2016 / Published: 18 April 2016
(This article belongs to the Section Medicinal Chemistry)
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Inflammation is the protective action of our bodies against external pathogens by recognition of pathogen-associated molecular patterns (PAMPs) via pattern recognition receptors (PRRs). Proper regulation of inflammatory responses is required to maintain our body’s homeostasis, as well as there are demands to develop proper acute or chronic inflammation. In this study, we elucidated the regulatory mechanism of NF-κB-mediated inflammatory responses by a novel compound, 1-(2,3-dibenzimidazol-2-ylpropyl)-2-methoxybenzene (DBMB). We found that DBMB suppressed inflammatory mediators, nitric oxide (NO) and prostaglandin E2 (PGE2), reacted to exposure to a number of toll like receptor (TLR) ligands. Such observations occurred following to decreased mRNA expression of several pro-inflammatory mediators, and such diminished mRNA levels were caused by inhibited transcriptional factor nuclear factor (NF)-κB, as evaluated by luciferase reporter assay and molecular biological approaches. To find the potential targets of DBMB, we screened phosphorylated forms of NF-κB signal molecules: inhibitor of κBα (IκBα), IκB kinase (IKK)α/β, Akt, 3-phosphoinositide dependent protein kinase-1 (PDK1), p85, and spleen tyrosine kinase (Syk). We found that DBMB treatment could suppress signal transduction through these molecules. Additionally, we conducted in vitro kinase assays using immunoprecipitated Syk and its substrate, p85. Consequently, we could say that DBMB clearly suppressed the kinase activity of Syk kinase activity. Together, our results demonstrate that synthetic DBMB has an effect on the inflammatory NF-κB signaling pathway and suggest the potential for clinical use in the treatment of inflammatory diseases. View Full-Text
Keywords: 1-(2,3-dibenzimidazol-2-ylpropyl)-2-methoxybenzene; inflammatory responses; NF-κB; Syk 1-(2,3-dibenzimidazol-2-ylpropyl)-2-methoxybenzene; inflammatory responses; NF-κB; Syk

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Kim, E.; Son, Y.-J.; Yang, Y.; Shen, T.; Kim, I.; Aravinthan, A.; Kim, J.-H.; Cho, J.Y. 1-(2,3-Dibenzimidazol-2-ylpropyl)-2-methoxybenzene Is a Syk Inhibitor with Anti-Inflammatory Properties. Molecules 2016, 21, 508.

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