Arbutin: benefits, dosage, contraindications

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

Other name(s) 

arbutoside

Family or group: 

Phytosubstances

Active ingredients:

Hydroquinone

D-glucose


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.


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

Posologie

posologieOral administration

posologie100 mg

populationAdults, Women


Properties


Dermatological effect

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Used particularly as a skin lightening product, alpha-arbutin also appears to be very effective, at low concentrations, in the treatment of skin problems 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 colibacilli, 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-infective actions.

Usages associés

Skin lightening, Urinary tract infections

Diuretic

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Arbutin is recognized for its natural diuretic properties. Some animal studies indicate 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 combat oxidative stress and cellular aging. Indeed, it exhibits the same antioxidant activity as hydroquinone and a sustained radical-scavenging activity effective in fighting oxidative stress.

Usages associés

Skin lightening

Anti-inflammatory

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In vitro, arbutin has 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.


Safe dosage

Adults aged 18 years and over: 50 mg - 720 mg

Arbutin is mainly extracted from bearberry. The dried leaves contain arbutin at concentrations ranging from 5 to 16%. These concentrations vary depending on the time and place of the plant harvest. Arbutin dosages depend on the preparations. For example, bearberry is generally expressed as a weight ratio based on arbutin content. In one trial, capsules containing 20% arbutin were used for 3600 mg of bearberry/day, which yields 720 mg of arbutin. Use should be for a short duration (3 to 5 days). Furthermore, isolated hydroquinone is toxic at high doses (1 g).


Interactions

Médicaments

Urinary acidifiers: moderate interaction

Theoretically, taking arbutin with medications known to acidify the 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 thinning of the retina. Theoretically, arbutin could worsen retinal thinning in patients with this condition.


Contraindications

Children up to 12 years: prohibited

Arbutin is contraindicated in children under 12 years of age. Hydroquinone can cause serious liver disorders.

Pregnancy: prohibited

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

Breastfeeding: prohibited

Arbutin is contraindicated in breastfeeding women.