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dc.contributor.author배옥남-
dc.date.accessioned2019-05-10T07:53:52Z-
dc.date.available2019-05-10T07:53:52Z-
dc.date.issued2009-01-
dc.identifier.citationBRITISH JOURNAL OF PHARMACOLOGY, v. 156, No. 2, Page. 328-337en_US
dc.identifier.issn0007-1188-
dc.identifier.urihttps://bpspubs.onlinelibrary.wiley.com/doi/abs/10.1111/j.1476-5381.2008.00028.x-
dc.identifier.urihttps://repository.hanyang.ac.kr/handle/20.500.11754/103869-
dc.description.abstractInducible 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.sponsorshipThis work was supported by the SRC/ERC Programme of MOST/KOSEF (R11-2007-107-01002-0).en_US
dc.language.isoen_USen_US
dc.publisherWILEY-BLACKWELL PUBLISHINGen_US
dc.subjectiNOSen_US
dc.subjectcyclooxygenase-2en_US
dc.subjectanti-inflammatory agenten_US
dc.subjectinflammationen_US
dc.subjectTPA-induced mouse ear oedemaen_US
dc.subjectquinolinedioneen_US
dc.titlePotent anti-inflammatory effects of two quinolinedione compounds, OQ1 and OQ21, mediated by dual inhibition of inducible NO synthase and cyclooxygenase-2en_US
dc.typeArticleen_US
dc.relation.volume156-
dc.identifier.doi10.1111/j.1476-5381.2008.00028.x-
dc.relation.page328-337-
dc.relation.journalBRITISH JOURNAL OF PHARMACOLOGY-
dc.contributor.googleauthorLim, Kyung-Min-
dc.contributor.googleauthorLee, Joo-Young-
dc.contributor.googleauthorLee, Song-Mi-
dc.contributor.googleauthorBae, Ok-Nam-
dc.contributor.googleauthorNoh, Ji-Yoon-
dc.contributor.googleauthorKim, Eun-Jin-
dc.contributor.googleauthorChung, Seung-Min-
dc.contributor.googleauthorChung, Jin-Ho-
dc.relation.code2009201482-
dc.sector.campusE-
dc.sector.daehakCOLLEGE OF PHARMACY[E]-
dc.sector.departmentDEPARTMENT OF PHARMACY-
dc.identifier.pidonbae-
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COLLEGE OF PHARMACY[E](약학대학) > PHARMACY(약학과) > Articles
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