論文 - 詳細
| RRC ID | 19209 |
|---|---|
| 著者 | Kotani H, Tanabe H, Mizukami H, Makishima M, Inoue M. |
| タイトル | Identification of a naturally occurring rexinoid, honokiol, that activates the retinoid X receptor. |
| ジャーナル | J Nat Prod |
| Abstract |
Screening of a total of 86 crude drugs for retinoid X receptor (RXR) ligands demonstrated that the methanol extract of the bark of Magnolia obovata markedly activated the transcriptional activity of RXRalpha in luciferase reporter assays. Thereafter, honokiol (1) was isolated as a constituent able to activate RXR selectively as a natural rexinoid, but not RARalpha. The activity of 1 was more potent than those of phytanic acid and docosahexaenoic acid, both of which are known to be natural RXR agonists. Honokiol (1) is capable of activating a RXR/LXR heterodimer, resulting in the induction of ATP-binding cassette transporter A1 mRNA and protein expression in RAW264.7 cells, as well as an increase in [(3)H]cholesterol efflux from peritoneal macrophages. These effects of 1 were enhanced synergistically in the presence of an LXR agonist, 22(R)-hydroxycholesterol. The results obtained demonstrate that 1, a newly identified natural rexinoid, regulates the functions of RXR/LXR heterodimer and abrogates foam cell formation by the induction of ABCA1 via activation of the RXR/LXR heterodimer. |
| 巻・号 | 73(8) |
| ページ | 1332-6 |
| 公開日 | 2010-8-27 |
| DOI | 10.1021/np100120c |
| PMID | 20695472 |
| MeSH | ATP Binding Cassette Transporter 1 ATP-Binding Cassette Transporters / drug effects ATP-Binding Cassette Transporters / genetics Animals Bexarotene Biphenyl Compounds / chemistry Biphenyl Compounds / pharmacology* Cholesterol / metabolism Humans Ligands Lignans / chemistry Lignans / pharmacology* Macrophages / drug effects Magnolia / chemistry* Male Mice Mice, Inbred Strains Molecular Structure Plant Bark / chemistry Plants, Medicinal / chemistry* Receptors, Retinoic Acid Retinoic Acid Receptor alpha Retinoid X Receptors / agonists* Tetrahydronaphthalenes / chemistry |
| IF | 3.782 |
| 引用数 | 56 |
| WOS 分野 | CHEMISTRY, MEDICINAL PHARMACOLOGY & PHARMACY PLANT SCIENCES |
| オルトメトリクス指標 |
オルトメトリクス指標項目
|
| 最多言及媒体 | Patent(IFI CLAIMS) |
| 各媒体での言及数の合計 | 1 |
| 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 | 293(RCB1637) |