SITOSTEROLS

US Previously Marketed

First approved in 1956

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/10796740 | https://www.ncbi.nlm.nih.gov/pubmed/12579296 | https://www.luckyvitamin.com/c-2091-beta-sitosterol | https://www.vitamart.ca/beta-sitosterol/ | https://www.webmd.com/vitamins-supplements/ingredientmono-939-beta-sitosterol.aspx | https://www.ncbi.nlm.nih.gov/pubmed/345413 | https://www.ncbi.nlm.nih.gov/pubmed/26199569

Beta-sitosterol is one of the main dietary phytosterols found in plants which have a similar skeleton as cholesterol. In human clinical trials, beta-sitosterol has been shown to have cholesterol-lowering effects and to relieve symptoms of benign prostatic hyperplasia. There has been a large amount of basic research conducted for potential applications of beta-sitosterol in a diverse range of conditions including cervical cancer, breast cancer, cystic fibrosis, and others. Beta-sitosterol is available over the counter as a natural health supplement and is marketed for a wide range of applications including headaches, tuberculosis, allergies, cancers, fibromyalgia, lupus, asthma, hair loss and many others.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Caspase-3 21 Target ID: P42574 Gene ID: 836.0 Gene Symbol: CASP3 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/12579296	Activator 1447
Protein kinase C alpha type 5 Target ID: P17252 Gene ID: 5578.0 Gene Symbol: PRKCA Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/28553226	Interacts 323

Conditions

Condition	Modality	Highest Phase	Product
Benign prostatic hyperplasia 28 Sources: https://www.ncbi.nlm.nih.gov/pubmed/10796740	Primary	Natural Metabolite	Unknown Approved Use Unknown
Breast cancer 432 Sources: https://www.ncbi.nlm.nih.gov/pubmed/12579296	Primary	Natural Metabolite	Unknown Approved Use Unknown
Sitosterolemia 2 Sources: https://clinicaltrials.gov/ct2/show/NCT00531128	Primary	Natural Metabolite	Unknown Approved Use Unknown
Cystic fibrosis 120 Sources: https://www.ncbi.nlm.nih.gov/pubmed/28553226	Primary	Natural Metabolite	Unknown Approved Use Unknown
Cervical cancer 40 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26199569	Primary	Natural Metabolite	Unknown Approved Use Unknown

PubMed

Title	Date	PubMed
Effect of β-sitosterol on the expression of HPV E6 and p53 in cervical carcinoma cells.	2015	26199569
Dietary supplements for benign prostatic hyperplasia: an overview of systematic reviews.	2012-11	22883375
Beta-sitosterol, a plant sterol, induces apoptosis and activates key caspases in MDA-MB-231 human breast cancer cells.	2003-02-13	12579296
Beta-sitosterols for benign prostatic hyperplasia.	2000	10796740
The influence of beta-sitosterol on biliary cholesterol saturation and bile acid kinetics in man.	1978	345413

Patents

Sample Use Guides

In Vivo Use Guide

Over 6 to 8 weeks beta-sitosterol supplementation of 12 g/day resulted in an average of 11% decrease in serum cholesterol and a 12% decrease in biliary cholesterol saturation.

Route of Administration: Oral

In Vitro Use Guide

Human cervical cancer cell lines, Caski and HeLa, were cultured in RPMI-1640 and supplemented with 10% foetal bovine serum and incubated at 37 deg-c in an atmosphere with 5% CO2. Cells were treated with 20 umol/L of beta-sitosterol for 48 hours and examined for changes by light microscopy, electron microscopy, and transmission electron microscopy. Changes in mRNA and protein expression were quantified using Real-Time qPCR and western blots. The treatment with beta-sitosterol reduced expression of PCNA, increased p53 mRNA, decreased the amount of HPV E6 transcripts. Cells treated with beta-sitosterol also exhibited loss of cell surface microvilli and increased electron density in the cell membrane.

Substance Class	Mixture Created by `admin` on `Mon Mar 31 18:38:30 GMT 2025` Edited by `admin` on `Mon Mar 31 18:38:30 GMT 2025`
Record UNII	G7V636VTDY
Record Status	`Validated (UNII)`
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Name

Type

Language

SITOSTEROLS

Common Name

English

SITOSTEROL

Preferred Name

English

Sitosterols [WHO-DD]

Common Name

English

Classification Tree Code System Code

DSLD

2794 (Number of products:1)