Characterization of beta-Sitosterol for Potential Selective GR Modulation

文献类型： 外文期刊

第一作者： Leng, Yue

作者： Leng, Yue;Sun, Yonghai;Li, Tiezhu;Lv, Chengyu;Li, Zhuolin;Yuan, Cuiping;Zhang, Jie;Li, Tiezhu;Wang, Yongjun

作者机构：

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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