論文 - 詳細
| RRC ID | 44609 |
|---|---|
| 著者 | Gamo K, Shiraki T, Matsuura N, Miyachi H. |
| タイトル | Mechanism of peroxisome proliferator-activated receptor gamma (PPARγ) transactivation by hesperetin glucuronides is distinct from that by a thiazolidine-2,4-dione agent. |
| ジャーナル | Chem Pharm Bull (Tokyo) |
| Abstract |
Hesperidin, a flavanone glycoside present abundantly in citrus fruits, is predominantly metabolized to hesperetin-7-O-β-D-glucuronide (H7-OG) and hesperetin-3'-O-β-D-glucuronide (H3'-OG), which exhibit partial agonistic activity towards peroxisome proliferator-activated receptor gamma (PPARγ). Here, in order to understand the mechanism(s) of action of PPARγ transactivation elicited by hesperetin glucuronides, we compared the transactivation activities of PPARγ (ligand-binding domain (LBD)) mutants by hesperetin glucuronides and troglitazone, a thiazolidine-2,4-dione class PPARγ full agonist. The assay results indicated that the mechanisms of activation of PPARγ by hesperetin glucuronides and by troglitazone are distinct, probably due to a difference in the binding sites of these compounds on the PPARγ LBD. Flavanone-class PPARγ partial agonists, luteolin and hesperetin glucuronides, showed similar activation profiles of the PPARγ LBD mutants, even though they have different side chain functionalities. |
| 巻・号 | 62(5) |
| ページ | 491-3 |
| 公開日 | 2014-1-1 |
| DOI | 10.1248/cpb.c14-00021 |
| PII | DN/JST.JSTAGE/cpb/c14-00021 |
| PMID | 24789933 |
| MeSH | Animals Binding Sites / drug effects COS Cells Cells, Cultured Chlorocebus aethiops Hesperidin / chemical synthesis Hesperidin / chemistry Hesperidin / pharmacology* Humans Models, Molecular Molecular Structure PPAR gamma / agonists* PPAR gamma / genetics PPAR gamma / metabolism Structure-Activity Relationship Thiazolidinediones / chemical synthesis Thiazolidinediones / chemistry Thiazolidinediones / pharmacology* |
| 引用数 | 6 |
| WOS 分野 | CHEMISTRY, ANALYTICAL BIOCHEMICAL RESEARCH METHODS BIOCHEMISTRY & MOLECULAR BIOLOGY |
| オルトメトリクス指標 |
オルトメトリクス指標項目
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| 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 | COS-1(RCB0143) |