β-sitosterol: benefits, dosage, contraindications

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β-sitosterol is a plant sterol. Phytosterols are bioactive compounds that are naturally present in the membranes of plant cells and whose chemical structure is similar to that of cholesterol. They are abundant in lipid-rich plant foods such as nuts, seeds, legumes, rice bran, wheat germ, peanuts, corn oil and soybean seeds. They are also found in plants such as the dwarf palm, ryegrass 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 shown that β-sitosterol has various biological activities such as analgesic, immunomodulatory, anticancer, anti-inflammatory, hypolipidemic, protective effects against respiratory diseases, wound-healing, and antidiabetic effects. The European Food Safety Authority (EFSA) has suggested that consumption of about 1.5 to 2.4 g/day of phytosterols and/or stanols reduces blood cholesterol levels, which lowers the risk of heart disease. Likewise, the FDA has concluded that β-sitosterol and other plant sterol esters may reduce the risk of coronary heart disease by lowering blood cholesterol levels.

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Phytosubstances


Indications

Scoring methodology

EFSA approval.

Several randomized, double-blind, controlled clinical trials (> 2), including a significant number of patients (>100), with consistently positive conclusions for the indication.
Several randomized, double-blind, controlled clinical trials (> 2), including a significant number of patients (>100), with positive conclusions for the indication.
One or more randomized studies, or several cohorts or epidemiological studies, with positive conclusions for the indication.
Clinical studies exist but are uncontrolled, with conclusions that may be positive or conflicting.
No clinical studies to date that can demonstrate the indication.


Hypercholesterolemia
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Oral intake of beta-sitosterol significantly reduces total cholesterol 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 moderately elevated cholesterol; however, this combination does not affect triglyceride levels or HDL cholesterol.

Posologie

posologieOral

posologie1500 - 3500 mg


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

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 (dwarf palm) taken twice daily improves hair quantity and quality in men with androgenetic alopecia. nn

Posologie

posologieOral

posologie100 mg


Synergies


Properties


Hypolipidemic

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Beta-sitosterol inhibits intestinal cholesterol absorption by a competitive effect within the limited space of mixed micelles, which reduces cholesterol absorption by about 50%. However, because the body has less cholesterol available, compensatory mechanisms come into play by 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. The reduction in cholesterol bioavailability by beta-sitosterol may also reduce the biosynthesis of testosterone and DHT. As a reminder, it is suggested that androgenetic alopecia involves increased hair follicle sensitivity to DHT, shortening their growth phase and reducing their size. For prostate hyperplasia, animal research suggests that beta-sitosterol may inhibit 5-alpha-reductase activity, although finasteride appears more potent. Laboratory studies suggest beta-sitosterol may have antiproliferative effects on the prostate, possibly 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 can inhibit the growth of human colon cancer cells in vitro. The mechanism of action involves membrane signaling, caspases, and inflammatory mediators.

Usages associés

Benign prostatic hyperplasia

Immunomodulatory

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Beta-sitosterol may have immunostimulatory effects. Mixtures of beta-sitosterol and its glycoside, sitosterolin, also appear to enhance T-cell proliferative responses in vitro. Beta-sitosterol may also moderate the immune suppression and inflammation observed in marathon runners after a race.


Hypoglycemic

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A study showed that oral treatment with beta-sitosterol decreases 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 understood and require further studies.


Wound healing

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Beta-sitosterol has an angiogenic effect. Indeed, beta-sitosterol improves the formation of new blood 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 the 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 impairment of locomotion. Other research has shown that the combination of beta-sitosterol and fluoxetine (an antidepressant drug) has a synergistic effect.


Safe dosage

Adults aged 18 years and older: 60 mg - 4000 mg

Beta-sitosterol is most commonly 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 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: weak 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 use

Avoid use due to lack of reliable and sufficient information. nn

Lactating woman: avoid

Avoid use due to lack of reliable and sufficient information. nn


Contraindications

Sitosterolemia: contraindicated

Taking beta-sitosterol may exacerbate sitosterolemia, a rare hereditary lipid storage disorder. People with this condition have increased absorption of cholesterol and beta-sitosterol from the diet, and decreased clearance of beta-sitosterol. Total body stores of beta-sitosterol increase substantially. High hepatic beta-sitosterol levels competitively inhibit cholesterol catabolism, thereby contributing to hypercholesterolemia. nnBeta-sitosterol and its glycoside, sitosterolin, are contraindicated in patients with sitosterolemia. nn