DC Field | Value | Language |
---|---|---|
dc.contributor.author | Lee, Sunyoung | ko |
dc.contributor.author | Lee, Yonghyun | ko |
dc.contributor.author | Kim, Wooseong | ko |
dc.contributor.author | Nam, Joon | ko |
dc.contributor.author | Jeong, Seongkeun | ko |
dc.contributor.author | Yoo, Jin-Wook | ko |
dc.contributor.author | Kim, Min-Soo | ko |
dc.contributor.author | Moon, Hyung Ryong | ko |
dc.contributor.author | Jung, Yunjin | ko |
dc.date.accessioned | 2016-04-15T03:13:53Z | - |
dc.date.available | 2016-04-15T03:13:53Z | - |
dc.date.created | 2015-09-01 | - |
dc.date.created | 2015-09-01 | - |
dc.date.issued | 2015 | - |
dc.identifier.citation | DRUG DESIGN DEVELOPMENT AND THERAPY, v.9, pp.4227 - 4237 | - |
dc.identifier.issn | 1177-8881 | - |
dc.identifier.uri | http://hdl.handle.net/10203/204062 | - |
dc.description.abstract | In an inflammatory state where HOCl is generated, glycine readily reacts with HOCl to produce glycine chloramine, an anti-inflammatory oxidant. Colonic delivery of celecoxib elicits anticolitic effects in a trinitrobenzene sulfonic acid-induced rat colitis model. Glycine-bearing celecoxib derivatives were prepared and evaluated as a colon-specific mutual prodrug acting on nuclear factor-kappa B (NF kappa B), an anticolitic target. Glycylcelecoxib (GC), N-glycylaspart-1-ylcelecoxib (N-GA1C), and C-glycylaspart-1-ylcelecoxib (C-GA1C) were synthesized and their structures identified using infrared and proton nuclear magnetic resonance spectrometer. The celecoxib derivatives were chemically stable in pH 6.8 and 1.2 buffers. GC and C-GA1C were resistant to degradation in the small intestinal contents, while N-GA1C was substantially cleaved to release celecoxib. In contrast, all the celecoxib derivatives were degraded to liberate celecoxib in the cecal content. These results suggest that GC and C-GA1C could be delivered to and liberate celecoxib and glycine in the large intestine. In human colon carcinoma HCT116 and murine macrophage RAW264.7 cells, combined celecoxib-glycine chloramine treatment additively suppressed the production of proinflammatory NF kappa B target gene products. Collectively, our data suggest that C-GA1C is a potential colon-specific mutual prodrug acting against NF kappa B. | - |
dc.language | English | - |
dc.publisher | DOVE MEDICAL PRESS LTD | - |
dc.subject | INFLAMMATORY-BOWEL-DISEASE | - |
dc.subject | SELECTIVE CYCLOOXYGENASE-2 INHIBITORS | - |
dc.subject | EXPERIMENTAL COLITIS | - |
dc.subject | TAURINE CHLORAMINE | - |
dc.subject | 5-AMINOSALICYLIC ACID | - |
dc.subject | ACTIVATION | - |
dc.subject | ALPHA | - |
dc.subject | MECHANISM | - |
dc.subject | ROFECOXIB | - |
dc.subject | OXIDATION | - |
dc.title | Evaluation of glycine-bearing celecoxib derivatives as a colon-specific mutual prodrug acting on nuclear factor-kappa B, an anti-inflammatory target | - |
dc.type | Article | - |
dc.identifier.wosid | 000359300300001 | - |
dc.identifier.scopusid | 2-s2.0-84939806275 | - |
dc.type.rims | ART | - |
dc.citation.volume | 9 | - |
dc.citation.beginningpage | 4227 | - |
dc.citation.endingpage | 4237 | - |
dc.citation.publicationname | DRUG DESIGN DEVELOPMENT AND THERAPY | - |
dc.identifier.doi | 10.2147/DDDT.S88543 | - |
dc.contributor.nonIdAuthor | Lee, Sunyoung | - |
dc.contributor.nonIdAuthor | Kim, Wooseong | - |
dc.contributor.nonIdAuthor | Nam, Joon | - |
dc.contributor.nonIdAuthor | Jeong, Seongkeun | - |
dc.contributor.nonIdAuthor | Yoo, Jin-Wook | - |
dc.contributor.nonIdAuthor | Kim, Min-Soo | - |
dc.contributor.nonIdAuthor | Moon, Hyung Ryong | - |
dc.contributor.nonIdAuthor | Jung, Yunjin | - |
dc.description.isOpenAccess | Y | - |
dc.type.journalArticle | Article | - |
dc.subject.keywordAuthor | colon-specific drug delivery | - |
dc.subject.keywordAuthor | mutual prodrug | - |
dc.subject.keywordAuthor | celecoxib | - |
dc.subject.keywordAuthor | glycine chloramine | - |
dc.subject.keywordAuthor | nuclear factor kappa-B | - |
dc.subject.keywordPlus | INFLAMMATORY-BOWEL-DISEASE | - |
dc.subject.keywordPlus | SELECTIVE CYCLOOXYGENASE-2 INHIBITORS | - |
dc.subject.keywordPlus | EXPERIMENTAL COLITIS | - |
dc.subject.keywordPlus | TAURINE CHLORAMINE | - |
dc.subject.keywordPlus | 5-AMINOSALICYLIC ACID | - |
dc.subject.keywordPlus | ACTIVATION | - |
dc.subject.keywordPlus | ALPHA | - |
dc.subject.keywordPlus | MECHANISM | - |
dc.subject.keywordPlus | ROFECOXIB | - |
dc.subject.keywordPlus | OXIDATION | - |
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