title: α-Cyperone, isolated from the rhizomes of Cyperus rotundus, inhibits LPS-induced COX-2 expression and PGE2 production through the negative regulation of NFκB signalling in RAW 264.7 cells.
abstract: BACKGROUND
  The rhizomes of Cyperus rotundus (Cyperaceae) have been used in Asian traditional medicine for the treatment of several inflammatory diseases. However, the anti-inflammatory effects of α-cyperone, a major active compound of Cyperus rotundus, are poorly understood.
  
  
  METHODS
  PGE2 and cytokines released from cells were measured using an EIA assay kit. The expression of iNOS, COX-2, TNF-α, and IL-6 was measured by real-time RT-PCR and/or Western blot analysis. A luciferase assay was performed to measure the effect of α-cyperone on NFκB activity.
  
  
  RESULTS
  The n-hexane fraction of the 80% EtOH extract from the rhizomes of Cyperus rotundus was found to inhibit both NO and PGE2 production in RAW 264.7 cells. α-Cyperone isolated from the n-hexane fraction significantly inhibited PGE2 production by suppressing the LPS-induced expression of inducible COX-2 at both the mRNA and the protein levels. In contrast, α-cyperone had little effect on NO production and iNOS expression. Additionally, α-cyperone downregulated the production and mRNA expression of the inflammatory cytokine IL-6. Moreover, treatment with α-cyperone suppressed the transcriptional activity of NFκB and the nuclear translocation of the p65 NFκB subunit in LPS-induced RAW 264.7 cells.
  
  
  CONCLUSIONS
  The anti-inflammatory activity of α-cyperone is associated with the down-regulation of COX-2 and IL-6 via the negative regulation of the NFκB pathway in LPS-stimulated RAW 264.7 cells.
authors.affiliation: Department of Life & Nanopharmaceutical Science, Kyung Hee University, Dongdaemun-Gu, Hoegi-Dong 130-701, Seoul, Republic of Korea.
authors.forename: Seung-Hyun
authors.initials: SH
authors.lastname: Jung
authors.forename: Su Jung
authors.initials: SJ
authors.lastname: Kim
authors.forename: Bo-Gyu
authors.initials: BG
authors.lastname: Jun
authors.forename: Kyung-Tae
authors.initials: KT
authors.lastname: Lee
authors.forename: Seon-Pyo
authors.initials: SP
authors.lastname: Hong
authors.forename: Myung Sook
authors.initials: MS
authors.lastname: Oh
authors.forename: Dae Sik
authors.initials: DS
authors.lastname: Jang
authors.forename: Jung-Hye
authors.initials: JH
authors.lastname: Choi
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D015153:Blotting, Western; D002460:Cell Line; D051546:Cyclooxygenase 2 / Q000235:genetics / Q000378:metabolism*; D029786:Cyperus / Q000737:chemistry; D015232:Dinoprostone / Q000378:metabolism*; D004305:Dose-Response Relationship, Drug; D015536:Down-Regulation; D000431:Ethanol / Q000737:chemistry; D017930:Genes, Reporter; D006586:Hexanes / Q000737:chemistry; D007124:Immunoenzyme Techniques; D015850:Interleukin-6 / Q000378:metabolism; D008070:Lipopolysaccharides / Q000494:pharmacology*; D008264:Macrophages / Q000187:drug effects* / Q000201:enzymology; D055670:Medicine, Korean Traditional; D051379:Mice; D016328:NF-kappa B / Q000235:genetics / Q000378:metabolism*; D009281:Naphthalenes / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D052247:Nitric Oxide Synthase Type II / Q000378:metabolism; D008517:Phytotherapy; D010936:Plant Extracts / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D010946:Plants, Medicinal; D012333:RNA, Messenger / Q000378:metabolism; D060888:Real-Time Polymerase Chain Reaction; D020133:Reverse Transcriptase Polymerase Chain Reaction; D027343:Rhizome; D015398:Signal Transduction / Q000187:drug effects*; D012997:Solvents / Q000737:chemistry; D014162:Transfection; D014409:Tumor Necrosis Factor-alpha / Q000378:metabolism
chemical_list: D000893:Anti-Inflammatory Agents; D006586:Hexanes; D015850:Interleukin-6; D008070:Lipopolysaccharides; D016328:NF-kappa B; D009281:Naphthalenes; D010936:Plant Extracts; D012333:RNA, Messenger; D012997:Solvents; D014409:Tumor Necrosis Factor-alpha; C026385:n-hexane; D000431:Ethanol; D052247:Nitric Oxide Synthase Type II; C496317:Nos2 protein, mouse; C077623:Ptgs2 protein, mouse; D051546:Cyclooxygenase 2; D015232:Dinoprostone; C583938:alpha-cyperone