title: Attenuation of LPS-induced inflammation by ICT, a derivate of icariin, via inhibition of the CD14/TLR4 signaling pathway in human monocytes.
abstract: OBJECTIVE
  To evaluate the anti-inflammatory potential of ICT in LPS stimulated human innate immune cells.
  
  
  BACKGROUND
  3, 5, 7-Trihydroxy-4'-methoxy-8-(3-hydroxy-3- methylbutyl)-flavone (ICT) is a novel derivative of icariin, the major active ingredient of Herba Epimedii, an herb used in traditional Chinese medicine. We previously demonstrated its anti-inflammatory potential in a murine macrophage cell line as well as in mouse models.
  
  
  METHODS
  We measured TNF-α production by ELISA, TLR4/CD14 expression by flow cytometry, and NF-κB and MAPK activation by western blot all in LPS-stimulated PBMC, human monocytes, or THP-1 cells after treatment with ICT.
  
  
  RESULTS
  ICT inhibited LPS-induced TNF-α production in THP-1 cells, PBMCs and human monocytes in a dose-dependent manner. ICT treatment resulted in down-regulation of the expression of CD14/TLR4 and attenuated NF-κB and MAPK activation induced by LPS.
  
  
  CONCLUSIONS
  We illustrate the anti-inflammatory property of ICT in human immune cells, especially in monocytes. These effects were mediated, at least partially, via inhibition of the CD14/TLR4 signaling pathway.
authors: Department of Integrative Medicine, Huashan Hospital, Fudan University, 12 Middle Urumqi Road, Shanghai, 200040, China.
authors: Jinfeng
authors: J
authors: Wu
authors: Junmin
authors: J
authors: Zhou
authors: Xianghong
authors: X
authors: Chen
authors: Nicole
authors: N
authors: Fortenbery
authors: Erika A
authors: EA
authors: Eksioglu
authors: Sheng
authors: S
authors: Wei
authors: Jingcheng
authors: J
authors: Dong
mesh_terms: D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology / Q000627:therapeutic use*; D002460:Cell Line; D048049:Extracellular Signal-Regulated MAP Kinases / Q000276:immunology; D047309:Flavones / Q000494:pharmacology / Q000627:therapeutic use*; D005419:Flavonoids; D006801:Humans; D007249:Inflammation / Q000188:drug therapy* / Q000276:immunology; D018950:Lipopolysaccharide Receptors / Q000276:immunology*; D008070:Lipopolysaccharides; D009000:Monocytes / Q000187:drug effects / Q000276:immunology; D008517:Phytotherapy; D015398:Signal Transduction / Q000187:drug effects; D051197:Toll-Like Receptor 4 / Q000037:antagonists & inhibitors* / Q000276:immunology; D014409:Tumor Necrosis Factor-alpha / Q000276:immunology; D048051:p38 Mitogen-Activated Protein Kinases / Q000276:immunology
chemical_list: C558386:3,5,7-trihydroxy-4'-methoxy-8-(3-hydroxy-3-methylbutyl)flavone; D000894:Anti-Inflammatory Agents, Non-Steroidal; D047309:Flavones; D005419:Flavonoids; D018950:Lipopolysaccharide Receptors; D008070:Lipopolysaccharides; D051197:Toll-Like Receptor 4; D014409:Tumor Necrosis Factor-alpha; D048049:Extracellular Signal-Regulated MAP Kinases; D048051:p38 Mitogen-Activated Protein Kinases; C056599:icariin