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Identification and characterization of ?-sitosterol target proteins.

ABSTRACT: ?-Sitosterol is the most abundant plant sterol in the human diet. It is also the major component of several traditional medicines, including saw palmetto and devil's claw. Although ?-sitosterol is effective against enlarged prostate in human clinical trials and has anti-cancer and anti-inflammatory activities, the mechanisms of action are poorly understood. Here, we report the identification of two new binding proteins for ?-sitosterol that may underlie its beneficial effects.

SUBMITTER: Lomenick B

PROVIDER: S-EPMC4567552 | biostudies-literature | 2015 Nov

REPOSITORIES: biostudies-literature

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Identification and characterization of β-sitosterol target proteins.

Lomenick Brett B Shi Heping H Huang Jing J Chen Chuo C

Bioorganic & medicinal chemistry letters 20150311 21

β-Sitosterol is the most abundant plant sterol in the human diet. It is also the major component of several traditional medicines, including saw palmetto and devil's claw. Although β-sitosterol is effective against enlarged prostate in human clinical trials and has anti-cancer and anti-inflammatory activities, the mechanisms of action are poorly understood. Here, we report the identification of two new binding proteins for β-sitosterol that may underlie its beneficial effects. ...[more]

PMID: 25804720

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Anti-Hepatocellular-Cancer Activity Exerted by β-Sitosterol and β-Sitosterol-Glucoside from Indigofera zollingeriana Miq.

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Isolation, characterization, and docking studies of campesterol and β-sitosterol from <i>Strychnos innocua</i> (Delile) root bark.

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Hippocampal gene expression profiling in mice treated with beta-sitosterol

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2021-05-18 | GSE134467 | GEO

β-sitosterol reduces anxiety and synergizes with established anxiolytic drugs in mice.

Project description:Anxiety and stress-related conditions represent a significant health burden in modern society. Unfortunately, most anxiolytic drugs are prone to side effects, limiting their long-term usage. Here, we employ a bioinformatics screen to identify drugs for repurposing as anxiolytics. Comparison of drug-induced gene-expression profiles with the hippocampal transcriptome of an importin α5 mutant mouse model with reduced anxiety identifies the hypocholesterolemic agent β-sitosterol as a promising candidate. β-sitosterol activity is validated by both intraperitoneal and oral application in mice, revealing it as the only clear anxiolytic from five closely related phytosterols. β-sitosterol injection reduces the effects of restraint stress, contextual fear memory, and c-Fos activation in the prefrontal cortex and dentate gyrus. Moreover, synergistic anxiolysis is observed when combining sub-efficacious doses of β-sitosterol with the SSRI fluoxetine. These preclinical findings support further development of β-sitosterol, either as a standalone anxiolytic or in combination with low-dose SSRIs.

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Imperatorin and β-sitosterol have synergistic activities in alleviating collagen-induced arthritis.

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