Effects of a Tetramethoxyhydroxyflavone on the Expression of Inflammatory Mediators in LPS-Treated Human Synovial Fibroblast and Macrophage Cells

  • Yoon, Do-Young (Division of Bioscience and Biotechnology, Konkuk University) ;
  • Cho, Min-Chul (Division of Bioscience and Biotechnology, Konkuk University) ;
  • Kim, Jung-Hee (Division of Bioscience and Biotechnology, Konkuk University) ;
  • Kim, Eun-Jin (Division of Bioscience and Biotechnology, Konkuk University) ;
  • Kang, Jeong-Woo (Division of Bioscience and Biotechnology, Konkuk University) ;
  • Seo, Eun-Hee (Division of Bioscience and Biotechnology, Konkuk University) ;
  • Shim, Jung-Hyun (Division of Bioscience and Biotechnology, Konkuk University) ;
  • Kim, Soo-Hyun (Institute of Biomedical Science and Technology, Konkuk University) ;
  • Lee, Hee-Gu (Korea Research Institute of Bioscience and Biotechnology) ;
  • Oh, Goo-Taeg (Division of Molecular Life Sciences, Ewha Womans University) ;
  • Hong, Jin-Tae (Department of Pharmacy, Chungbuk National University College of Pharmacy) ;
  • Park, Joo-Won (Department of Laboratory Medicine, Dankook University College of Medicine) ;
  • Kim, Jong-Wan (Department of Laboratory Medicine, Dankook University College of Medicine)
  • Published : 2008.04.30


The inhibitory effects of 5,6,3',5'-tetramethoxy 7,4'-hydroxyflavone (labeled as p7F) were elucidated on the productions of proinflammatory cytokines as well as inflammatory mediators in human synovial fibroblasts and macrophage cells. p7F inhibited IL-1${\beta}$ or TNF-${\alpha}$ induced expressions of inflammatory mediators (ICAM-1, COX-2, and iNOS). p7F also inhibited LPS-induced productions of nitric oxide and prostaglandin $E_2$ in RAW 264.7 cells. In order to investigate whether p7F would inhibit IL-1 signaling, p7F was added to the D10S Th2 cell line (which is responsive to only IL-1${\beta}$ and thus proliferates), revealing that p7F inhibited IL-1${\beta}$-induced proliferation of D10S Th2 cells in a dose-response manner. A flow cytometric analysis revealed that p7F reduced the intracellular level of free radical oxygen species in RAW 264.7 cells treated with hydrogen peroxide. p7F inhibited IkB degradation and NF-${\kappa}$B activation in macrophage cells treated with LPS, supporting that p7F could inhibit signaling mediated via toll-like receptor. Taken together, p7F has inhibitory effects on LPS-induced productions of inflammatory mediators on human synovial fibroblasts and macrophage cells and thus has the potential to be an anti-inflammatory agent for inhibiting inflammatory responses.


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