ATP-Binding Pocket-Targeted Suppression of Src and Syk by Luteolin Contributes to Its Anti-Inflammatory Action
DC Field | Value | Language |
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dc.contributor.author | Lee, Jeong-Oog | - |
dc.contributor.author | Jeong, Deok | - |
dc.contributor.author | Kim, Mi-Yeon | - |
dc.contributor.author | Cho, Jae Youl | - |
dc.date.available | 2018-05-09T08:53:24Z | - |
dc.date.created | 2018-04-17 | - |
dc.date.issued | 2015 | - |
dc.identifier.issn | 0962-9351 | - |
dc.identifier.uri | http://scholarworks.bwise.kr/ssu/handle/2018.sw.ssu/9827 | - |
dc.description.abstract | Luteolin is a flavonoid identified as a major anti-inflammatory component of Artemisia asiatica. Numerous reports have demonstrated the ability of luteolin to suppress inflammation in a variety of inflammatory conditions. However, its exact anti-inflammatory mechanism has not been fully elucidated. In the present study, the anti-inflammatory mode of action in activated macrophages of luteolin from Artemisia asiatica was examined by employing immunoblotting analysis, a luciferase reporter gene assay, enzyme assays, and an overexpression strategy. Luteolin dose-dependently inhibited the secretion of nitric oxide (NO) and prostaglandin E-2 (PGE(2)) and diminished the levels of mRNA transcripts of inducible NO synthase (iNOS), tumor necrosis factor( TNF-)-alpha, and cyclooxygenase-2 (COX-2) in lipopolysaccharide-(LPS-) and pam3CSK-treated macrophage-like RAW264.7 cells without displaying cytotoxicity. Luteolin displayed potent NO-inhibitory activity and also suppressed the nuclear translocation of NF-kappa B (p65 and p50) via blockade of Src and Syk, but not other mitogen-activated kinases. Overexpression of wild type Src and point mutants thereof, and molecular modelling studies, suggest that the ATP-binding pocket may be the luteolin-binding site in Src. These results strongly suggest that luteolin may exert its anti-inflammatory action by suppressing the NF-kappa B signaling cascade via blockade of ATP binding in Src and Syk. | - |
dc.publisher | HINDAWI PUBLISHING CORP | - |
dc.relation.isPartOf | MEDIATORS OF INFLAMMATION | - |
dc.subject | NF-KAPPA-B | - |
dc.subject | RAW 264.7 CELLS | - |
dc.subject | INFLAMMATORY RESPONSES | - |
dc.subject | ARTEMISIA PLANTS | - |
dc.subject | EPITHELIAL-CELLS | - |
dc.subject | CANCER CELLS | - |
dc.subject | TNF-ALPHA | - |
dc.subject | ACTIVATION | - |
dc.subject | INHIBITION | - |
dc.subject | EUPATILIN | - |
dc.title | ATP-Binding Pocket-Targeted Suppression of Src and Syk by Luteolin Contributes to Its Anti-Inflammatory Action | - |
dc.type | Article | - |
dc.identifier.doi | 10.1155/2015/967053 | - |
dc.type.rims | ART | - |
dc.identifier.bibliographicCitation | MEDIATORS OF INFLAMMATION | - |
dc.description.journalClass | 1 | - |
dc.identifier.wosid | 000358239100001 | - |
dc.identifier.scopusid | 2-s2.0-84937776460 | - |
dc.citation.title | MEDIATORS OF INFLAMMATION | - |
dc.contributor.affiliatedAuthor | Kim, Mi-Yeon | - |
dc.type.docType | Article | - |
dc.description.oadoiVersion | published | - |
dc.subject.keywordPlus | NF-KAPPA-B | - |
dc.subject.keywordPlus | RAW 264.7 CELLS | - |
dc.subject.keywordPlus | INFLAMMATORY RESPONSES | - |
dc.subject.keywordPlus | ARTEMISIA PLANTS | - |
dc.subject.keywordPlus | EPITHELIAL-CELLS | - |
dc.subject.keywordPlus | CANCER CELLS | - |
dc.subject.keywordPlus | TNF-ALPHA | - |
dc.subject.keywordPlus | ACTIVATION | - |
dc.subject.keywordPlus | INHIBITION | - |
dc.subject.keywordPlus | EUPATILIN | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
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