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10.5483/bmbrep.2018.51.6.064

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suck abstract from ncbi


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pmid29804558
      BMB+Rep 2018 ; 51 (6 ): 308-313
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  • Anti-inflammatory effects of a novel compound, MPQP, through the inhibition of IRAK1 signaling pathways in LPS-stimulated RAW 264 7 macrophages #MMPMID29804558
  • Kim BR ; Cho YC ; Cho S
  • BMB Rep 2018[Jun]; 51 (6 ): 308-313 PMID29804558 show ga
  • Small-molecule inhibitors are widely used to treat a variety of inflammatory diseases. In this study, we found a novel antiinflammatory compound, 1-[(2R,4S)-2-methyl-4-(phenylamino)-1,2,3,4-tetrahydroquinolin-1-yl]prop-2-en-1-one (MPQP). It showed strong anti-inflammatory effects in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages. These effects were exerted through the inhibition of the production of NO and pro-inflammatory cytokines, such as interleukin (IL)-6, IL-1?, and tumor necrosis factor-? (TNF-?). Furthermore, MPQP decreased the expression levels of inducible NO synthase (iNOS) and cyclooxygenase 2 (COX-2). Additionally, it mediated the inhibition of the phosphorylation of p38, c-Jun N-terminal kinase (JNK), the inhibitor of ?B? (I?B?), and their upstream kinases, I?B kinase (IKK) ?/?, mitogen-activated protein kinase kinase (MKK) 3/6, and MKK4. Furthermore, the expression of IL-1 receptor-associated kinase 1 (IRAK1) that regulates NF-?B, p38, and the JNK signaling pathways, was also increased by MPQP. These results indicate that MPQP regulates the IRAK1-mediated inflammatory signaling pathways by targeting IRAK1 or its upstream factors. [BMB Reports 2018; 51(6): 308-313].
  • |Animals [MESH]
  • |Anti-Inflammatory Agents/*pharmacology [MESH]
  • |Cyclooxygenase 2/metabolism [MESH]
  • |I-kappa B Proteins/metabolism [MESH]
  • |Inflammation/drug therapy [MESH]
  • |Interleukin-1 Receptor-Associated Kinases/*antagonists & inhibitors/metabolism [MESH]
  • |Lipopolysaccharides/pharmacology [MESH]
  • |MAP Kinase Kinase 4/metabolism [MESH]
  • |Macrophages/drug effects [MESH]
  • |Mice [MESH]
  • |NF-KappaB Inhibitor alpha/metabolism [MESH]
  • |NF-kappa B/metabolism [MESH]
  • |Nitric Oxide/biosynthesis/metabolism [MESH]
  • |Phosphorylation/drug effects [MESH]
  • |Quinolines/*pharmacology [MESH]
  • |RAW 264.7 Cells [MESH]
  • |Signal Transduction/drug effects [MESH]
  • |Small Molecule Libraries/*pharmacology [MESH]


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