Potent anti-inflammatory effects of two quinolinedione compounds, OQ1 and OQ21, mediated by dual inhibition of inducible NO synthase and cyclooxygenase-2
DC Field | Value | Language |
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dc.contributor.author | Lim, Kyung-Min | - |
dc.contributor.author | Lee, Joo-Young | - |
dc.contributor.author | Lee, Song-Mi | - |
dc.contributor.author | Bae, Ok-Nam | - |
dc.contributor.author | Noh, Ji-Yoon | - |
dc.contributor.author | Kim, Eun-Jin | - |
dc.contributor.author | Chung, Seung-Min | - |
dc.contributor.author | Chung, Jin-Ho | - |
dc.date.accessioned | 2021-06-23T16:03:50Z | - |
dc.date.available | 2021-06-23T16:03:50Z | - |
dc.date.created | 2021-01-21 | - |
dc.date.issued | 2009-01 | - |
dc.identifier.issn | 0007-1188 | - |
dc.identifier.uri | https://scholarworks.bwise.kr/erica/handle/2021.sw.erica/41464 | - |
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. | - |
dc.language | 영어 | - |
dc.language.iso | en | - |
dc.publisher | Wiley-Blackwell | - |
dc.title | Potent anti-inflammatory effects of two quinolinedione compounds, OQ1 and OQ21, mediated by dual inhibition of inducible NO synthase and cyclooxygenase-2 | - |
dc.type | Article | - |
dc.contributor.affiliatedAuthor | Bae, Ok-Nam | - |
dc.identifier.doi | 10.1111/j.1476-5381.2008.00028.x | - |
dc.identifier.scopusid | 2-s2.0-67650261357 | - |
dc.identifier.wosid | 000263352000012 | - |
dc.identifier.bibliographicCitation | British Journal of Pharmacology, v.156, no.2, pp.328 - 337 | - |
dc.relation.isPartOf | British Journal of Pharmacology | - |
dc.citation.title | British Journal of Pharmacology | - |
dc.citation.volume | 156 | - |
dc.citation.number | 2 | - |
dc.citation.startPage | 328 | - |
dc.citation.endPage | 337 | - |
dc.type.rims | ART | - |
dc.type.docType | Article | - |
dc.description.journalClass | 1 | - |
dc.description.isOpenAccess | N | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
dc.relation.journalResearchArea | Pharmacology & Pharmacy | - |
dc.relation.journalWebOfScienceCategory | Pharmacology & Pharmacy | - |
dc.subject.keywordPlus | NITRIC-OXIDE SYNTHASE | - |
dc.subject.keywordPlus | NF-KAPPA-B | - |
dc.subject.keywordPlus | PROSTAGLANDIN BIOSYNTHESIS | - |
dc.subject.keywordPlus | EXPERIMENTAL COLITIS | - |
dc.subject.keywordPlus | SELECTIVE INHIBITOR | - |
dc.subject.keywordPlus | ENDOTOXIC-SHOCK | - |
dc.subject.keywordPlus | IN-VIVO | - |
dc.subject.keywordPlus | MACROPHAGES | - |
dc.subject.keywordPlus | LIPOPOLYSACCHARIDE | - |
dc.subject.keywordPlus | ACTIVATION | - |
dc.subject.keywordAuthor | iNOS | - |
dc.subject.keywordAuthor | cyclooxygenase-2 | - |
dc.subject.keywordAuthor | anti-inflammatory agent | - |
dc.subject.keywordAuthor | inflammation | - |
dc.subject.keywordAuthor | TPA-induced mouse ear oedema | - |
dc.subject.keywordAuthor | quinolinedione | - |
dc.identifier.url | https://bpspubs.onlinelibrary.wiley.com/doi/10.1111/j.1476-5381.2008.00028.x | - |
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