WEKO3
アイテム
Two Types of PPARγ Ligands Identified in the Extract of Artemisia campestris
http://hdl.handle.net/2241/0002002427
http://hdl.handle.net/2241/00020024270c8f9698-1944-428e-bef6-f25c3cd2454a
名前 / ファイル | ライセンス | アクション |
---|---|---|
Chemistry_3-2-647.pdf (3.4 MB)
|
Item type | Journal Article(1) | |||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
公開日 | 2022-01-07 | |||||||||||||||||
タイトル | ||||||||||||||||||
言語 | en | |||||||||||||||||
タイトル | Two Types of PPARγ Ligands Identified in the Extract of Artemisia campestris | |||||||||||||||||
言語 | ||||||||||||||||||
言語 | eng | |||||||||||||||||
資源タイプ | ||||||||||||||||||
資源 | http://purl.org/coar/resource_type/c_6501 | |||||||||||||||||
タイプ | journal article | |||||||||||||||||
アクセス権 | ||||||||||||||||||
アクセス権 | open access | |||||||||||||||||
アクセス権URI | http://purl.org/coar/access_right/c_abf2 | |||||||||||||||||
著者 |
Hasegawa, Tokio
× Hasegawa, Tokio
× Osaka, Mayo
× 宮前, 友策× Nishino, Katsutoshi
× 礒田, 博子× 川田, 清和× Neffati, Mohamed
× Irie, Kazuhiro
× Nagao, Masaya
|
|||||||||||||||||
抄録 | ||||||||||||||||||
内容記述タイプ | Abstract | |||||||||||||||||
内容記述 | The 70% ethanol extract of Artemisia campestris was screened to find PPARγ ligands using the PPARγ ligand-responsive chimera luciferase reporter system. Capillartemisin B was identified as a PPARγ ligand that stimulated lipid accumulation in 3T3-L1 cells. By further purification of PPARγ ligands from a large-scale preparation of the methanol extract of Artemisia campestris, we isolated and identified eupatilin and santaflavone as PPARγ ligands. Weak PPARγ ligand activity of eupatilin or santaflavone in reporter assay was enhanced by a PPARγ antagonist, GW9662, suggesting that santaflavone or eupatilin and GW9662 bound simultaneously to the multiple sub-pockets of the PPARγ ligand-binding domain (LBD) and cooperatively activated PPARγ. Docking simulation suggested that eupatilin binds to the Ω-pocket but not to the AF-2 pocket of Y-shaped PPARγ LBD where artepillin C that differs from capillartemisin B at the C-5′ position without hydroxy group binds. Eupatilin or santaflavone with or without GW9662 did not stimulate lipid accumulation in differentiated 3T3-L1 cells, suggesting that binding of each compound alone or with GW9662 to the Ω-pocket which stimulated the PPARγ-responsive reporter expression was not enough to stimulate lipid accumulation. The PPARγ ligands found in this study have a potential to design the fragment-based drug design of a novel PPARγ ligand that cover the Y-shaped PPARγ LBD. | |||||||||||||||||
言語 | en | |||||||||||||||||
書誌情報 |
en : Chemistry 巻 3, 号 2, p. 647-657, 発行日 2021-05 |
|||||||||||||||||
ISSN | ||||||||||||||||||
収録物識別子タイプ | EISSN | |||||||||||||||||
収録物識別子 | 2624-8549 | |||||||||||||||||
DOI | ||||||||||||||||||
関連タイプ | isIdenticalTo | |||||||||||||||||
識別子タイプ | DOI | |||||||||||||||||
関連識別子 | https://doi.org/10.3390/chemistry3020045 | |||||||||||||||||
権利 | ||||||||||||||||||
言語 | en | |||||||||||||||||
権利情報 | © 2021 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https:// creativecommons.org/licenses/by/ 4.0/). | |||||||||||||||||
著者版フラグ | ||||||||||||||||||
値 | publisher | |||||||||||||||||
出版者 | ||||||||||||||||||
言語 | en | |||||||||||||||||
出版者 | MDPI |