Characterization of β-Sitosterol for Potential Selective GR Modulation

Author(s): Yue Leng, Yonghai Sun, Chengyu Lv, Zhuolin Li, Cuiping Yuan, Jie Zhang, Tiezhu Li*, Yongjun Wang*

Journal Name: Protein & Peptide Letters

Volume 28 , Issue 3 , 2021


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Abstract:

Background: Although glucocorticoids (GCs) are characterized as powerful agents to treat inflammatory afflictions, they are accompanied by metabolic side effects which limit their usage. β-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 β-sitosterol has an effect to dissociate transrepression from transactivation as a selective novel GR binder, this work evaluated the dissociated characteristics of β-sitosterol.

Methods: The probable binding interaction between β-sitosterol and GR was explored by molecular docking. The GR transcriptional activity of β-sitosterol was assessed in the reporter gene assay. The ability of β-sitosterol to modulate the transactivation and transrepression of GR was evaluated by real-time quantitative PCR analysis.

Results and Discussion: In the present study, β-sitosterol treatment cannot induce GR-mediated transactivation. β-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 β-Sitosterol was able to bind the ligand binding domain of GR but unable to induce GR activation.

Conclusion: This work offers evidence that β-sitosterol may serve as a selective GR modulator.

Keywords: Glucocorticoid receptor, β-sitosterol, transactivation, transrepression, dissociate, molecular docking.

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Article Details

VOLUME: 28
ISSUE: 3
Year: 2021
Page: [276 - 281]
Pages: 6
DOI: 10.2174/0929866527666200813204833
Price: $95

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