論文 - 詳細
| RRC ID | 1311 |
|---|---|
| 著者 | Ban HS, Suzuki K, Lim SS, Jung SH, Lee S, Ji J, Lee HS, Lee YS, Shin KH, Ohuchi K. |
| タイトル | Inhibition of lipopolysaccharide-induced expression of inducible nitric oxide synthase and tumor necrosis factor-alpha by 2'-hydroxychalcone derivatives in RAW 264.7 cells. |
| ジャーナル | Biochem Pharmacol |
| Abstract |
In cultures of the murine macrophage cell line RAW 264.7, effects of four 2'-hydroxychalcone derivatives, 2'-hydroxy-4'-methoxychalcone (compound 1), 2',4-dihydroxy-4'-methoxychalcone (compound 2), 2',4-dihydroxy-6'-methoxychalcone (compound 3) and 2'-hydroxy-4,4'-dimethoxychalcone (compound 4), on lipopolysaccharide (LPS)-induced production of nitric oxide (NO) and tumor necrosis factor (TNF)-alpha were examined. Compounds 1, 2 and 3 at 3-30microM inhibited the production with almost the same potency. Compound 4 showed no inhibitory activity. Compounds 1, 2 and 3 at 3-30microM inhibited the LPS-induced expression of inducible nitric oxide synthase (iNOS) and TNF-alpha mRNA. To clarify the mechanism involved, effects of compounds 1, 2 and 3 on the activation of nuclear factor (NF)-kappaB and activator protein-1 (AP-1) were examined. Both the LPS-induced activation of NF-kappaB and AP-1 were blocked by compounds 1, 2 and 3 at 3-30microM. Moreover, the three compounds at such concentrations inhibited the LPS-induced IkappaB degradation and the phosphorylation of c-jun N-terminal kinase (JNK) and c-jun. These findings suggest that the inhibition of the LPS-induced production of NO and TNF-alpha by the 2'-hydroxychalcone derivatives is due to the inhibition of NF-kappaB and AP-1 activations. |
| 巻・号 | 67(8) |
| ページ | 1549-57 |
| 公開日 | 2004-4-15 |
| DOI | 10.1016/j.bcp.2003.12.016 |
| PII | S0006295203009559 |
| PMID | 15041472 |
| MeSH | Animals Cell Line Chalcone / analogs & derivatives* Chalcone / pharmacology* Chalcones Drug Interactions Gene Expression / drug effects I-kappa B Proteins / metabolism JNK Mitogen-Activated Protein Kinases Lipopolysaccharides / pharmacology* Macrophages / drug effects* Macrophages / metabolism Mice Mitogen-Activated Protein Kinases / metabolism NF-KappaB Inhibitor alpha NF-kappa B / metabolism Nitrates / metabolism Nitric Oxide Synthase / biosynthesis* Nitric Oxide Synthase Type II Phosphorylation RNA, Messenger / biosynthesis RNA, Messenger / drug effects Signal Transduction Transcription Factor AP-1 / metabolism Tumor Necrosis Factor-alpha / biosynthesis* |
| IF | 4.96 |
| 引用数 | 73 |
| WOS 分野 | PHARMACOLOGY & PHARMACY |
| オルトメトリクス指標 |
オルトメトリクス指標項目
|
| 各媒体での言及数の合計 | 0 |
| 過去6か月間でのオルトメトリクス指標の変動値 | 0.0 |
| リソース情報 | |
| ヒト・動物細胞 | RAW 264(RCB0535) |