DC Field | Value | Language |
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dc.contributor.author | Jeong-Hyung Lee | - |
dc.contributor.author | Haeng Sun Jung | - |
dc.contributor.author | P M Giang | - |
dc.contributor.author | X Jin | - |
dc.contributor.author | Sangku Lee | - |
dc.contributor.author | P T Son | - |
dc.contributor.author | Dongho Lee | - |
dc.contributor.author | Young-Soo Hong | - |
dc.contributor.author | Kyeong Lee | - |
dc.contributor.author | Jung Joon Lee | - |
dc.date.accessioned | 2017-04-19T09:04:00Z | - |
dc.date.available | 2017-04-19T09:04:00Z | - |
dc.date.issued | 2006 | - |
dc.identifier.issn | 0022-3565 | - |
dc.identifier.uri | 10.1124/jpet.105.092486 | ko |
dc.identifier.uri | https://oak.kribb.re.kr/handle/201005/7259 | - |
dc.description.abstract | Nuclear factor-κB (NF-κB) and the signaling pathways that regulate its activity have become a focal point for intense drug discovery and development efforts. NF-κB regulates the transcription of a large number of genes, particularly those involved in immune, inflammatory, and antiapoptotic responses. In our search for NF-κB inhibitors from natural resources, we identified cardamomin, 2′,4′-dihydroxy-6′-methoxychalcone, as an inhibitor of NF-κB activation from Alpinia conchigera Griff (Zingiberaceae). In present study, we demonstrated the effect of cardamomin on NF-κB activation in lipopolysaccharide (LPS)-stimulated RAW264.7 cells and LPS-induced mortality. This compound significantly inhibited the induced expression of NF-κB reporter gene by LPS or tumor necrosis factor (TNF)-α in a dose-dependent manner. LPS-induced production of TNF-α and NO as well as expression of inducible nitric-oxide synthase and cyclooxygenase-2 was significantly suppressed by the treatment of cardamomin in RAW264.7 cells. Also, cardamomin inhibited not only LPS-induced degradation and phosphorylation of inhibitor κBα (IκBα) but also activation of inhibitor κB (IκB) kinases and nuclear translocation of NF-κB. Further analyses revealed that cardamomin did not directly inhibit IκB kinases, but it significantly suppressed LPS-induced activation of Akt. Moreover, cardamomin suppressed transcriptional activity and phosphorylation of Ser536 of RelA/p65 subunit of NF-κB. However, this compound did not inhibit LPS-induced activation of extracellular signal-regulated kinase and stress-activated protein kinase/c-Jun NH 2-terminal kinase, but significantly impaired activation of p38 mitogen-activated protein kinase. We also demonstrated that pretreatment of cardamomin rescued C57BL/6 mice from LPS-induced mortality in conjunction with decreased serum level of TNF-α. Together, cardamomin could be valuable candidate for the intervention of NF-κB-dependent pathological condition such as inflammation. | - |
dc.publisher | Amer Soc Pharmacology Experimental Therapeutics | - |
dc.title | Blockade of nuclear factor-κB signaling pathway and anti-inflammatory activity of cardamomin, a chalcone analog from Alpinia conchigera | - |
dc.title.alternative | Blockade of nuclear factor-κB signaling pathway and anti-inflammatory activity of cardamomin, a chalcone analog from Alpinia conchigera | - |
dc.type | Article | - |
dc.citation.title | Journal of Pharmacology and Experimental Therapeutics | - |
dc.citation.number | 1 | - |
dc.citation.endPage | 278 | - |
dc.citation.startPage | 271 | - |
dc.citation.volume | 316 | - |
dc.contributor.affiliatedAuthor | Jeong-Hyung Lee | - |
dc.contributor.affiliatedAuthor | Haeng Sun Jung | - |
dc.contributor.affiliatedAuthor | Sangku Lee | - |
dc.contributor.affiliatedAuthor | Dongho Lee | - |
dc.contributor.affiliatedAuthor | Young-Soo Hong | - |
dc.contributor.affiliatedAuthor | Kyeong Lee | - |
dc.contributor.affiliatedAuthor | Jung Joon Lee | - |
dc.contributor.alternativeName | 이정형 | - |
dc.contributor.alternativeName | 정행선 | - |
dc.contributor.alternativeName | Giang | - |
dc.contributor.alternativeName | Jin | - |
dc.contributor.alternativeName | 이상구 | - |
dc.contributor.alternativeName | Son | - |
dc.contributor.alternativeName | 이동호 | - |
dc.contributor.alternativeName | 홍영수 | - |
dc.contributor.alternativeName | 이경 | - |
dc.contributor.alternativeName | 이정준 | - |
dc.identifier.bibliographicCitation | Journal of Pharmacology and Experimental Therapeutics, vol. 316, no. 1, pp. 271-278 | - |
dc.identifier.doi | 10.1124/jpet.105.092486 | - |
dc.description.journalClass | Y | - |
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