Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | 배옥남 | - |
dc.date.accessioned | 2019-05-10T07:53:52Z | - |
dc.date.available | 2019-05-10T07:53:52Z | - |
dc.date.issued | 2009-01 | - |
dc.identifier.citation | BRITISH JOURNAL OF PHARMACOLOGY, v. 156, No. 2, Page. 328-337 | en_US |
dc.identifier.issn | 0007-1188 | - |
dc.identifier.uri | https://bpspubs.onlinelibrary.wiley.com/doi/abs/10.1111/j.1476-5381.2008.00028.x | - |
dc.identifier.uri | https://repository.hanyang.ac.kr/handle/20.500.11754/103869 | - |
dc.description.abstract | Inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) have been suggested as key components in various inflammatory diseases. Here we examined the effects of new quinolinedione derivatives, 6-(4-fluorophenyl)-amino-5,8-quinolinedione (OQ1) and 6-(2,3,4-trifluorophenyl)-amino-5,8-quinolinedione (OQ21) on activity and expression of iNOS and COX-2 to explore their anti-inflammatory properties. The effects of OQ1 and OQ21 were assessed on lipopolysaccharide (LPS)-induced iNOS and COX-2 in murine macrophage cell line (RAW264.7), along with isolated enzyme assays to measure enzyme inhibition. Nuclear factor-kappa B (NF kappa B) activation pathways were investigated to elucidate mechanisms underlying OQ-mediated suppression of the expression of iNOS and COX-2. In vivo anti-inflammatory activities of OQ compounds were evaluated in mouse ear oedema, induced by topical 12-O-tetradecanoylphorbol-13-acetate (TPA). LPS-induced NO production in RAW264.7 cells was inhibited by OQ1 and OQ21 through the attenuation of iNOS expression as well as iNOS activity. Down-regulation of iNOS followed blocking of NF kappa B activation, as assessed by inhibitory kappa B degradation and electrophoretic mobility shift assay for NF kappa B. Synthesis and accumulation of prostaglandin E-2 were also suppressed by OQ1 and OQ21. LPS-induced COX-2 expression and cellular COX-2 activities were attenuated by OQ1 and OQ21. Consistent with these results, OQ1 showed potent anti-inflammatory effects in mouse ear oedema induced by TPA. The novel quinolinedione derivatives, OQ1 and OQ21, showed potent anti-inflammatory activity through dual inhibitory effects on iNOS and COX-2, suggesting that OQ derivatives might provide a new therapeutic modality for chronic inflammatory diseases, refractory to conventional drug therapies. | en_US |
dc.description.sponsorship | This work was supported by the SRC/ERC Programme of MOST/KOSEF (R11-2007-107-01002-0). | en_US |
dc.language.iso | en_US | en_US |
dc.publisher | WILEY-BLACKWELL PUBLISHING | en_US |
dc.subject | iNOS | en_US |
dc.subject | cyclooxygenase-2 | en_US |
dc.subject | anti-inflammatory agent | en_US |
dc.subject | inflammation | en_US |
dc.subject | TPA-induced mouse ear oedema | en_US |
dc.subject | quinolinedione | en_US |
dc.title | Potent anti-inflammatory effects of two quinolinedione compounds, OQ1 and OQ21, mediated by dual inhibition of inducible NO synthase and cyclooxygenase-2 | en_US |
dc.type | Article | en_US |
dc.relation.volume | 156 | - |
dc.identifier.doi | 10.1111/j.1476-5381.2008.00028.x | - |
dc.relation.page | 328-337 | - |
dc.relation.journal | BRITISH JOURNAL OF PHARMACOLOGY | - |
dc.contributor.googleauthor | Lim, Kyung-Min | - |
dc.contributor.googleauthor | Lee, Joo-Young | - |
dc.contributor.googleauthor | Lee, Song-Mi | - |
dc.contributor.googleauthor | Bae, Ok-Nam | - |
dc.contributor.googleauthor | Noh, Ji-Yoon | - |
dc.contributor.googleauthor | Kim, Eun-Jin | - |
dc.contributor.googleauthor | Chung, Seung-Min | - |
dc.contributor.googleauthor | Chung, Jin-Ho | - |
dc.relation.code | 2009201482 | - |
dc.sector.campus | E | - |
dc.sector.daehak | COLLEGE OF PHARMACY[E] | - |
dc.sector.department | DEPARTMENT OF PHARMACY | - |
dc.identifier.pid | onbae | - |
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