Beta-sitosterol: Benefits, Dosage, Contraindications

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Beta-sitosterol is a plant sterol. Phytosterols are bioactive compounds naturally found in the membranes of plant cells with a chemical structure similar to cholesterol. They are highly present in plant foods rich in lipids such as nuts, seeds, legumes, rice bran, wheat germ, peanuts, corn oil, and soybean oil. They also exist in plants such as saw palmetto, rye pollen, pygeum (African plum) and nettles. The average diet provides about 175-200 mg of β-sitosterol, but less than 5% is actually absorbed when consumed orally. Therefore, these plant sterols do not have atherogenic effects. Numerous in vitro and in vivo studies have demonstrated that β-sitosterol possesses various biological actions such as analgesic, immunomodulatory, anticancer, anti-inflammatory, hypolipidemic, protective against respiratory diseases, healing, and antidiabetic effects. The European Food Safety Authority (EFSA) suggested that consuming approximately 1.5 to 2.4 g/day of phytosterols and/or stanols reduces blood cholesterol levels, thereby diminishing the risk of heart disease. On the other hand, the FDA concluded that β-sitosterol and other plant sterol esters may reduce the risk of coronary heart disease by lowering blood cholesterol levels.

Other name(s) 

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Phytosubstances


Indications

Rating methodology

EFSA approval.

Several clinical trials (> 2) randomized controlled with double blind, including a significant number of patients (>100) with consistently positive outcomes for the indication.
Several clinical trials (> 2) randomized controlled with double blind, and including a significant number of patients (>100) with positive outcomes for the indication.
One or more randomized studies or multiple cohorts or epidemiological studies with positive outcomes for the indication.
Clinical studies exist but are uncontrolled, with conclusions that may be positive or contradictory.
Lack of clinical studies to date that can demonstrate the indication.


Hypercholesterolemia
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Oral intake of beta-sitosterol significantly reduces total cholesterol levels and low-density lipoprotein (LDL) cholesterol levels, but has little or no effect on high-density lipoprotein (HDL) cholesterol levels. Some preliminary clinical research shows that taking a combination of 8 g of soy protein and 2 g of beta-sitosterol per day for 40 days slightly reduces LDL cholesterol by 17 to 20 mg/dL from baseline in patients with moderate hypercholesterolemia; however, this combination does not affect triglyceride or HDL cholesterol levels.

Posologie

posologieOral

posologie1500 - 3500 mg


Benign prostatic hyperplasia
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Taking 60 to 130 mg of beta-sitosterol orally in 2 or 3 divided doses per day improves urinary symptoms, increases maximum urinary flow rate, and decreases post-void residual urinary volume, but does not affect prostate size. The optimal dose is 60 mg twice a day. This dose can be reduced to 30 mg twice a day when symptoms improve.

Posologie

posologieOral

posologie60 - 130 mg


Hair loss
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Preliminary clinical research shows that a combination of 50 mg beta-sitosterol and 200 mg saw palmetto extract taken twice daily improves the quantity and quality of hair in men with androgenetic alopecia.

Posologie

posologieOral

posologie100 mg


Synergies


Properties


Hypolipidemic

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Beta-sitosterol inhibits intestinal cholesterol absorption through a competitive effect at the limited space of mixed micelles, reducing cholesterol absorption by about 50%. However, since the body has less cholesterol, compensatory mechanisms come into play, increasing cholesterol synthesis in the liver.

Usages associés

Hypercholesterolemia

Antiandrogenic

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Inhibition of 5 alpha-reductase, which prevents the conversion of testosterone to dihydrotestosterone (DHT), may contribute to beta-sitosterol’s activity in androgenetic alopecia. Reduction in the bioavailability of cholesterol by beta-sitosterol can also reduce the biosynthesis of testosterone and DHT. It's suggested that androgenetic alopecia involves increased sensitivity of hair follicles to DHT, reducing their growth phase and size. For prostate hyperplasia, animal research suggests that beta-sitosterol may inhibit the activity of 5-alpha-reductase, although finasteride seems more potent. Laboratory research suggests that beta-sitosterol may have antiproliferative effects on the prostate, potentially by inhibiting growth factors. In animals, beta-sitosterol shrinks the prostate, but this has not been demonstrated in humans.

Usages associés

Benign prostatic hyperplasia, Hair loss

Anticancer

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There is preliminary evidence that beta-sitosterol may have anticancer effects. Beta-sitosterol may inhibit the growth of human colon cancer cells in vitro. The mechanism of action involves membrane signalization, caspases, and inflammatory mediators.

Usages associés

Benign prostatic hyperplasia

Immunomodulator

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Beta-sitosterol may have immunostimulant effects. Mixtures of beta-sitosterol and its glycoside, sitosteroline, also appear to enhance proliferative responses of T cells in vitro. Beta-sitosterol may also moderate the immune decline and inflammation seen in marathon runners after a race.


Hypoglycemic

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A study has shown that oral treatment with beta-sitosterol lowers fasting blood glucose and improves glucose tolerance by increasing fasting plasma insulin levels in hyperglycemic rats. The mechanisms of this increase are not yet well elucidated and require further studies.


Healing

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Beta-sitosterol has an angiogenic effect. Indeed, beta-sitosterol improves the formation of new vessels in a dose-dependent manner and promotes the expression of several proteins related to angiogenesis, including Von Willebrand factors, VEGF (Vascular Endothelial Growth Factor), and VEGF receptor.

Usages associés

Burns

Neurological

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An in vivo study conducted in mice showed that administration of beta-sitosterol reduces anxiety without the side effects of anxiolytic drugs and without altering locomotion. Other research has shown that the combination of beta-sitosterol and fluoxetine (an antidepressant drug) has a synergistic effect.


Safety dosage

Adult from 18 year(s): 60 mg - 4000 mg

Beta-sitosterol is most often used at doses of 60 to 130 mg per day for up to 18 months or at higher doses of 3 to 4 grams per day for 1 to 3 months.


Interactions

Médicaments

EZETIMIBE: moderate interaction

Ezetimibe inhibits the intestinal absorption of beta-sitosterol and reduces plasma concentrations in people with or without sitosterolemia. In people with mild to moderate hypercholesterolemia, ezetimibe reduces beta-sitosterol levels by 41%.

Pravastatin: minor interaction

There is evidence that pravastatin can lower blood levels of beta-sitosterol. Theoretically, this could occur with other HMG-CoA reductase inhibitors ("statins").


Precautions

Pregnant women: avoid

Avoid use due to lack of reliable and sufficient information.

Breastfeeding women: avoid

Avoid use due to lack of reliable and sufficient information.


Contraindications

Sitosterolemia: prohibited

The intake of beta-sitosterol may exacerbate sitosterolemia, a rare hereditary lipid storage disease. People with this condition show increased absorption of cholesterol and beta-sitosterol from the diet, and decreased clearance of beta-sitosterol. Total body reserves of beta-sitosterol increase significantly. High levels of hepatic beta-sitosterol competitively inhibit cholesterol catabolism, thereby contributing to hypercholesterolemia. Beta-sitosterol and its glycoside, sitosteroline, are contraindicated in patients with sitosterolemia.