title: Evaluation of amentoflavone isolated from Cnestis ferruginea Vahl ex DC (Connaraceae) on production of inflammatory mediators in LPS stimulated rat astrocytoma cell line (C6) and THP-1 cells.
abstract: BACKGROUND
  Cnestisferruginea (CF) Vahl ex DC (Connaraceae) is a shrub widely used in traditional African medicine for the treatment of various psychiatric illness and inflammatory conditions.
  
  
  OBJECTIVE
  This study was carried out to investigate the effect of amentoflavone isolated from methanolic root extract of CF on lipopolysaccharide (LPS)-induced neuroinflammatory cascade of events associated to the oxidative and nitrative stress, and TNF-α production in rat astrocytoma cell line (C6) and human monocytic leukemia cell line (THP-1), respectively.
  
  
  METHODS
  Rat astrocytoma cells (C6) were stimulated with LPS (10μg/ml) alone and in the presence of different concentrations of amentoflavone (0.1-3μg/ml) for 24h incubation period. Nitrite release, reactive oxygen species (ROS), malondialdehyde (MDA) and reduced-glutathione (GSH) in C6 cells were estimated; while the TNF-α level was estimated in THP-1 cell lysate. In vivo analgesic activity was evaluated using mouse writhing and hot plate tests while the anti-inflammatory effect was investigated using carrageenan-induced oedema test.
  
  
  RESULTS
  LPS (10μg/ml) significantly (P<0.05) stimulated C6 cells to release nitrite, ROS, MDA, and TNF-α generation while GSH was down regulated in comparison to control. However, amentoflavone significantly (P<0.05) attenuated nitrite, ROS, MDA and TNF-α generation and also up regulated the level of GSH. Amentoflavone per se did not have any significant effect on C6 and THP-1 cells. Amentoflavone (6.25-50mg/kg) significantly (P<0.05) reduced number of writhes and also increase pain threshold in hot plate test. It produced time course significant (P<0.05) decrease in oedema formation in rodents.
  
  
  CONCLUSIONS
  Findings in this study demonstrate the anti-neuroinflammatory and antinoceptive effects of amentoflavone which may suggest its beneficial roles in neuroinflammation associated disorders.
authors: Pharmacology Division, Central Drug Research Institute, Lucknow-226 001, Uttar Pradesh, India.
authors: I O
authors: IO
authors: Ishola
authors: J P
authors: JP
authors: Chaturvedi
authors: S
authors: S
authors: Rai
authors: N
authors: N
authors: Rajasekar
authors: O O
authors: OO
authors: Adeyemi
authors: R
authors: R
authors: Shukla
authors: T
authors: T
authors: Narender
mesh_terms: D019342:Acetic Acid; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000494:pharmacology* / Q000627:therapeutic use; D001254:Astrocytoma; D044946:Biflavonoids / Q000494:pharmacology* / Q000627:therapeutic use; D002351:Carrageenan; D002460:Cell Line; D045744:Cell Line, Tumor; D002470:Cell Survival; D031961:Connaraceae; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy; D005260:Female; D005978:Glutathione / Q000378:metabolism; D006358:Hot Temperature; D018836:Inflammation Mediators / Q000378:metabolism; D008070:Lipopolysaccharides; D008297:Male; D008315:Malondialdehyde / Q000378:metabolism; D051379:Mice; D009573:Nitrites / Q000378:metabolism; D010146:Pain / Q000188:drug therapy / Q000209:etiology; D008517:Phytotherapy; D018517:Plant Roots; D051381:Rats; D017207:Rats, Sprague-Dawley; D017382:Reactive Oxygen Species / Q000378:metabolism; D014409:Tumor Necrosis Factor-alpha / Q000378:metabolism
chemical_list: D000893:Anti-Inflammatory Agents; D044946:Biflavonoids; D018836:Inflammation Mediators; D008070:Lipopolysaccharides; D009573:Nitrites; D017382:Reactive Oxygen Species; D014409:Tumor Necrosis Factor-alpha; D008315:Malondialdehyde; D002351:Carrageenan; C011164:amentoflavone; D005978:Glutathione; D019342:Acetic Acid