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Molecules 2014, 19(10), 16609-16623; doi:10.3390/molecules191016609

Anti-Inflammatory Potential of Newly Synthesized 4-[(Butylsulfinyl)methyl]-1,2-benzenediol in Lipopolysaccharide-Stimulated BV2 Microglia

Department of Biochemistry, College of Korean Medicine, Dongeui University, Busan 614-052, Korea
Department of Microbiology, College of Medicine, Inje University, Busan 608-756, Korea
Division of Applied Life Science (BK21 Plus), Gyeongsang National University, Jinju 660-701, Korea
Department of Marine Life Sciences, Jeju National University, Jeju 690-756, Korea
Department of Chemistry and Chemistry Institute for Functional Materials, Pusan National University, Busan 609-735, Korea
Division of Applied Life Science, Gyeongsang National University, Jinju 660-701, Korea
Department of Urology, College of Medicine, Chungbuk National University, Cheongju 361-763, Korea
Anti-Aging Research Center & Blue-Bio Industry Regional Innovation Center, Dongeui University, Busan 614-714, Korea
These authors contributed equally to this work.
Author to whom correspondence should be addressed.
Received: 28 July 2014 / Revised: 4 October 2014 / Accepted: 8 October 2014 / Published: 15 October 2014
(This article belongs to the Collection Bioactive Compounds)
View Full-Text   |   Download PDF [1030 KB, uploaded 15 October 2014]   |  


In this study, we investigated the anti-inflammatory effects of newly synthesized 4-[(butylsulfinyl)methyl]-1,2-benzenediol (SMBD) in lipopolysaccharide (LPS)-stimulated BV2 microglia and the subsequent signaling events. Following stimulation with LPS, elevated production of nitric oxide (NO) and prostaglandin E2 (PGE2) was detected in BV2 cells; however, SMBD pretreatment inhibited the production of NO and PGE2 through suppressing gene expression of inducible NO synthase (iNOS) and cyclooxygenase-2 (COX-2), respectively, at non-toxic concentrations. LPS-stimulated gene expression and production of interleukin (IL)-1β and tumor necrosis factor (TNF)-α were also significantly reduced by SMBD. The anti-inflammatory effects of SMBD were associated with suppression of LPS-induced nuclear translocation of nuclear factor-kappa B (NF-κB), and phosphorylation of mitogen-activated protein kinases (MAPKs) and Akt, a phosphatidylinositol 3-kinase (PI3K) downstream effector. Therefore, the present results demonstrate that SMBD down-regulates inflammatory gene expression by inhibiting the activation of NF-κB through interference with the activation of MAPKs and PI3K/Akt signaling. Taken together, our data suggest that SMBD may have potential to be developed into an effective anti-inflammatory agent. View Full-Text
Keywords: 4-[(butylsulfinyl)methyl]-1,2-benzenediol; BV2 microglia; anti-inflammation; NF-κB; MAPKs; PI3K/Akt 4-[(butylsulfinyl)methyl]-1,2-benzenediol; BV2 microglia; anti-inflammation; NF-κB; MAPKs; PI3K/Akt

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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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Jo, G.-H.; Choi, I.-W.; Jeong, J.-W.; Kim, G.-Y.; Kim, J.; Suh, H.; Ryu, C.-H.; Kim, W.-J.; Choi, Y.H. Anti-Inflammatory Potential of Newly Synthesized 4-[(Butylsulfinyl)methyl]-1,2-benzenediol in Lipopolysaccharide-Stimulated BV2 Microglia. Molecules 2014, 19, 16609-16623.

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