Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | 남태규 | - |
dc.date.accessioned | 2019-05-22T06:49:25Z | - |
dc.date.available | 2019-05-22T06:49:25Z | - |
dc.date.issued | 2018-06 | - |
dc.identifier.citation | MED CHEM COMM, v. 9, No. 8, Page. 1305-1310 | en_US |
dc.identifier.issn | 2040-2503 | - |
dc.identifier.uri | https://pubs.rsc.org/en/content/articlehtml/2018/md/c8md00156a | - |
dc.identifier.uri | https://repository.hanyang.ac.kr/handle/20.500.11754/105580 | - |
dc.description.abstract | Inflammatory bowel disease (IBD) is an inflammatory disease of the gastrointestinal tract with complex pathogenesis. Here, we synthesized 6-heteroarylamino analogues to inhibit TNF-alpha-induced adhesion of monocytes to colon epithelial cells which are implicated in the initial inflammation process of IBD. The best analogue, 16a, showed IC50 = 0.29 mu M, which is about five orders of magnitude better than that of 5-aminosalicylic acid (5-ASA), a positive control. Oral administration of 6f and 16a dramatically ameliorated 2,4,6-trinitrobenzenesulfonic acid (TNBS)-induced colon inflammation in rat. The ameliorating effects were accompanied by a high level of recovery in colon and body weights and in the myeloperoxidase (MPO) level. Consistently, the compounds suppressed the expression of intercellular adhesion molecule-1 (ICAM-1) and monocyte chemoattractant protein 1 (MCP-1). Moreover, they significantly suppressed the expression of pro-inflammatory cytokines such as TNF-alpha, IL-1 beta, and IL-6 while increasing the level of IL-10, an anti-inflammatory cytokine. | en_US |
dc.description.sponsorship | This work was supported by a grant of the Korean Health Technology R&D Project, Ministry of Health & Welfare, Republic of Korea (HI15C0542). | en_US |
dc.language.iso | en_US | en_US |
dc.publisher | ROYAL SOC CHEMISTRY | en_US |
dc.subject | INTESTINAL INFLAMMATION | en_US |
dc.subject | THERAPEUTIC TARGETS | en_US |
dc.subject | CROHNS-DISEASE | en_US |
dc.subject | IBD | en_US |
dc.subject | PATHOGENESIS6-AMINO-2,4,5-TRIMETHYLPYRIDIN-3-OLS | en_US |
dc.subject | IL-10 | en_US |
dc.subject | ASSAY | en_US |
dc.subject | RAT | en_US |
dc.title | Synthesis and evaluation of 6-heteroarylamino-2,4,5-trimethylpyridin-3-ols as inhibitors of TNF-alpha-induced cell adhesion and inflammatory bowel disease | en_US |
dc.type | Article | en_US |
dc.relation.no | 8 | - |
dc.relation.volume | 9 | - |
dc.identifier.doi | 10.1039/c8md00156a | - |
dc.relation.page | 1305-1310 | - |
dc.relation.journal | MEDCHEMCOMM | - |
dc.contributor.googleauthor | Park, Sang Won | - |
dc.contributor.googleauthor | Banskota, Suhrid | - |
dc.contributor.googleauthor | Gurung, Pallavi | - |
dc.contributor.googleauthor | Jin, You Jin | - |
dc.contributor.googleauthor | Kang, Han-eol | - |
dc.contributor.googleauthor | Chaudhary, Chhabi Lat | - |
dc.contributor.googleauthor | Lee, Sang Yeul | - |
dc.contributor.googleauthor | Jeong, Byeong-Seon | - |
dc.contributor.googleauthor | Kim, Jung-Ae | - |
dc.contributor.googleauthor | Nam, Tae-gyu | - |
dc.relation.code | 2018011695 | - |
dc.sector.campus | E | - |
dc.sector.daehak | COLLEGE OF PHARMACY[E] | - |
dc.sector.department | DEPARTMENT OF PHARMACY | - |
dc.identifier.pid | tnam | - |
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