文献类型： 外文期刊
作者： Leng, Yue 1 ; Sun, Yonghai 1 ; Lv, Chengyu 2 ; Li, Zhuolin 2 ; Yuan, Cuiping 2 ; Zhang, Jie 2 ; Li, Tiezhu 1 ; Wang, Yong 1 ;
作者机构： 1.Jilin Univ, Coll Food Sci & Engn, Changchun 130062, Peoples R China
2.Jilin Acad Agr Sci, Inst Agrofood Technol, Changchun 130033, Jilin, Peoples R China
关键词： Glucocorticoid receptor; beta-sitosterol; transactivation; transrepression; dissociate; molecular docking
期刊名称：PROTEIN AND PEPTIDE LETTERS （ 影响因子：1.156； 五年影响因子：1.054 ）
ISSN： 0929-8665
年卷期： 2021 年 28 卷 3 期
页码：
收录情况： SCI
摘要： Background: Although glucocorticoids (GCs) are characterized as powerful agents to treat inflammatory afflictions, they are accompanied by metabolic side effects which limit their usage. beta-Sitosterol, as a minor component found in extraction of vegetable oil, was reported to have anti-inflammatory effects in RAW 264.7 cells. Objective: To test whether beta-sitosterol has an effect to dissociate transrepression from transactivation as a selective novel GR binder, this work evaluated the dissociated characteristics of beta-sitosterol. Methods: The probable binding interaction between beta-sitosterol and GR was explored by molecular docking. The GR transcriptional activity of beta-sitosterol was assessed in the reporter gene assay. The ability of beta-sitosterol to modulate the transactivation and transrepression of GR was evaluated by real-time quantitative PCR analysis. Results and Discussion: In the present study, beta-sitosterol treatment cannot induce GR-mediated transactivation. beta-Sitosterol exerted a potential to inhibited the expression of GR target transrepressed gene without activating the expression of GR transactivation dependent gene. Molecular docking demonstrated that beta-Sitosterol was able to bind the ligand binding domain of GR but unable to induce GR activation. Conclusion: This work offers evidence that beta-sitosterol may serve as a selective GR modulator.
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