Arbutin: Benefits, Dosage, Contraindications

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Arbutin is a β-glucoside of hydroquinone or phenolic heteroside. It naturally occurs in several plant species of the Ericaceae family. It can be found in the leaves of bearberry, blueberry, cinder heather, or cranberry. Alpha-arbutin has traditionally been used as a treatment for certain diseases, such as urinary tract infections. It is commonly used as an antioxidant and thus found in most anti-aging products. It is also used in cosmetics as a depigmenting agent due to its inhibitory action on tyrosinase, an enzyme responsible for melanin formation.

Other name(s) 

arbutoside

Family or group: 

Phytosubstances

Active ingredients:

Hydroquinone

D-glucose


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.


Urinary tract infections
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Arbutin, metabolized in the urinary tract, is used in the treatment of urinary tract infections. Indeed, Arbutin present in bearberry leaves (17%) acts as a urinary antiseptic due to its antibacterial properties. Other medicinal plant extracts rich in arbutin can relieve cystitis symptoms.

Posologie

posologieOral administration

posologie100 mg

populationAdults, Women


Properties


Dermatological Effect

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Particularly used as a skin lightening product, alpha-arbutin also appears to be very effective, at low concentrations, in treating skin issues such as dry skin, freckles, and acne scars.

Usages associés

Skin lightening

Antibacterial

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Arbutin is used for its antibacterial properties. Indeed, Arbutin is active against coliform bacilli, the main germs responsible for urinary tract infections. Arbutin is metabolized in the urinary tract (after hydrolysis by intestinal or skin bacteria), where it breaks down into glucose and hydroquinone, a substance very similar to phenol with anti-infectious actions.

Usages associés

Skin lightening, Urinary tract infections

Diuretic

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Arbutin is recognized for its natural diuretic properties. Some animal research shows that it can increase urine flow.

Usages associés

Urinary tract infections

Antioxidant

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Arbutin is commonly used as an antioxidant, and consequently in most anti-aging products to fight oxidative stress and cellular aging. Indeed, it has the same antioxidant activity as hydroquinone and an effective, long-lasting radical activity to fight oxidative stress.

Usages associés

Skin lightening

Anti-inflammatory

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In vitro, arbutin exhibits anti-inflammatory activity. It significantly reduces pro-inflammatory mediators such as TNF-alpha.

Usages associés

Urinary tract infections

Anticancer

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Methanolic extracts of Damiana, a small shrub with aromatic flowers rich in arbutin, show cytotoxic activity in vitro against several cancer cell lines.


Safety dosage

Adult from 18 years: 50 mg - 720 mg

Arbutin is primarily extracted from Bearberry. Dried leaves contain arbutin at concentrations ranging from 5 to 16%. These concentrations vary based on the time and place of plant harvest. Arbutin dosages depend on the preparations. For example, bearberry is generally expressed in weight ratio based on arbutin content. In one trial, capsules containing 20% arbutin for 3600 mg of bearberry/day were used, resulting in 720 mg of arbutin. Use should be short-term (3 to 5 days). Moreover, isolated hydroquinone is toxic at high doses (1 g).


Interactions

Médicaments

Urinary acidifiers: moderate interaction

Theoretically, taking arbutin with medications known to acidify urine may reduce its effectiveness for urinary tract infections. Some urinary acidifiers include potassium phosphate and other phosphate salts.


Precautions

Retinopathy: avoid

Hydroquinone inhibits melanin synthesis and could lead to retina thinning. Theoretically, arbutin could worsen retina thinning in patients with this condition.


Contraindications

Child up to 12 years: prohibited

Arbutin is contraindicated in children under 12 years. Hydroquinone may cause serious liver disorders.

Pregnant woman: prohibited

Arbutin may have oxytocic effects, increasing the speed of labor.

Breastfeeding woman: prohibited

Arbutin is contraindicated in breastfeeding women.