論文 - 詳細
| RRC ID | 78496 |
|---|---|
| 著者 | Sekiguchi M, Fujinami Y, Takado K, Kimoto Y, Higashimura Y. |
| タイトル | Activity difference of three labdane diterpenoids on human constitutive androstane receptor. |
| ジャーナル | Biosci Biotechnol Biochem |
| Abstract |
The constitutive androstane receptor (CAR) regulates enzyme transcription related to drug metabolism; therefore, natural compound clarification in food that interacts with CAR is significant for drug development. We revealed that 13-epimanool, which is a compound found in the common sage, is bound to hCAR based on differential scanning fluorometry (DSF) measurements using recombinant hCAR protein. Similar labdane diterpenoids were examined, which revealed that manool and sclareol, which were both natural compounds contained in herbs, are bound to hCAR. They exhibited different effects for CAR activity in the luciferase assay despite the structural similarity. Manool was a partial agonist, 13-epimanool was a weak partial agonist, and sclareol was an antagonist. The activity of hCAR may be regulated by slight differences in the bound compound. |
| 巻・号 | 87(11) |
| ページ | 1310-1315 |
| 公開日 | 2023-10-25 |
| DOI | 10.1093/bbb/zbad113 |
| PII | 7242540 |
| PMID | 37580155 |
| MeSH | Constitutive Androstane Receptor* Diterpenes* / pharmacology Humans Receptors, Cytoplasmic and Nuclear |
| IF | 1.516 |
| 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 | X(Twitter) |
| 各媒体での言及数の合計 | 2 |
| 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 | Hep G2(RCB1886) |