| RRC ID |
52261
|
| 著者 |
Nakashima KI, Ogiwara T, Hirai T, Tanaka T, Murata H, Kaburagi K, Fujii-Kuriyama Y, Hayashi H, Inoue M.
|
| タイトル |
Gerontoxanthone B from Maclura cochinchinensis var. gerontogea exhibits anti-inflammatory potential as an aryl hydrocarbon receptor agonist.
|
| ジャーナル |
Bioorg Med Chem
|
| Abstract |
The aryl hydrocarbon receptor (AhR) is a ligand-dependent transcriptional factor belonging to the basic helix-loop-helix-Per-Ahr/Arnt-Sim family. In this study, we evaluated the AhR agonistic activities of 12 xanthones isolated from the roots of M. cochinchinensis var. gerontogea using HepG2 cells transfected with pX4TK-Luc reporter plasmids. Gerontoxanthone B (GXB) showed the most potent activity at a concentration of 10μM, and the activity was inhibited by AhR antagonists such as GNF-351. GXB also increased cytochrome P450 1A1 mRNA and protein levels in HepG2 cells. Similar to the AhR agonist 2,3,7,8-tetrachlorodibenzo-p-dioxin, however, GXB suppressed the IL-1β-induced mRNA level of SAA1, an acute-phase response gene that is up-regulated AhR-dependently but XRE-independently. Thus, GXB shows XRE-dependent transcriptional activity and XRE-independent activity involving AhR.
|
| 巻・号 |
25(16)
|
| ページ |
4253-4258
|
| 公開日 |
2017-8-15
|
| DOI |
10.1016/j.bmc.2017.05.047
|
| PII |
S0968-0896(17)30263-8
|
| PMID |
28662965
|
| MeSH |
Anti-Inflammatory Agents, Non-Steroidal / chemistry
Anti-Inflammatory Agents, Non-Steroidal / isolation & purification
Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
Dose-Response Relationship, Drug
Hep G2 Cells
Humans
Maclura / chemistry*
Molecular Structure
Receptors, Aryl Hydrocarbon / agonists*
Structure-Activity Relationship
Tumor Cells, Cultured
Xanthones / chemistry
Xanthones / isolation & purification
Xanthones / pharmacology*
|
| IF |
3.073
|
| 引用数 |
2
|
| リソース情報 |
| ヒト・動物細胞 |
Hep G2(RCB1886) |
