Arbutin
Arbutin is a naturally occurring compound that has gained significant attention in the skincare industry for its skin-lightening properties. Derived from various plant sources, including bearberry, blueberry, and cranberry, arbutin is a glycosylated hydroquinone. It is often used in cosmetic products to address hyperpigmentation and uneven skin tone.
CHEMICAL COMPOSITION AND SOURCES
Arbutin is a glycoside, specifically a hydroquinone β-D-glucopyranoside. It is found in the leaves of certain plants, most notably the bearberry (Arctostaphylos uva-ursi), but also in other plants like pear trees and wheat. The compound can be extracted naturally or synthesized in laboratories for use in various products.
Mechanism of Action
The primary function of arbutin in skincare is to inhibit the enzyme tyrosinase. Tyrosinase is crucial in the production of melanin, the pigment responsible for skin color. By inhibiting this enzyme, arbutin reduces melanin production, leading to a lighter skin tone and the reduction of dark spots and hyperpigmentation.
Arbutin is metabolized in the body to become the urinary antiseptic, hydroquinone.
Types of Arbutin
There are two main types of arbutin used in skincare:
- Alpha-Arbutin: This is a more stable and water-soluble form of arbutin. It is considered more effective and is often preferred in cosmetic formulations due to its higher stability and efficacy in reducing hyperpigmentation.
- Beta-Arbutin: This is the naturally occurring form of arbutin. While it is effective, it is less stable compared to alpha-arbutin and may not be as potent in lower concentrations.
Benefits of Arbutin
Arbutin offers several benefits, particularly in the realm of skincare:
- Skin Lightening: Arbutin is widely used for its ability to lighten skin tone and reduce the appearance of dark spots, age spots, and freckles.
- Even Skin Tone: By reducing melanin production, arbutin helps in achieving a more uniform skin tone.
- Gentle on Skin: Unlike some other skin-lightening agents, arbutin is less likely to cause irritation, making it suitable for sensitive skin.
- Antioxidant Properties: Arbutin also exhibits antioxidant properties, which help in protecting the skin from damage caused by free radicals.
Applications in Skincare
Arbutin is incorporated into various skincare products, including:
- Serums: Concentrated serums with arbutin are popular for targeted treatment of hyperpigmentation.
- Creams and Lotions: These products often combine arbutin with other skin-beneficial ingredients to enhance overall skin health.
- Face Masks: Arbutin-infused masks provide a quick and effective way to deliver the compound to the skin.
Safety and Side Effects
Arbutin is generally considered safe for topical use. However, as with any skincare ingredient, it is essential to be aware of potential side effects:
- Skin Sensitivity: While rare, some individuals may experience mild irritation or allergic reactions. It is advisable to perform a patch test before using products containing arbutin.
- Sun Sensitivity: Arbutin can make the skin more sensitive to sunlight. It is crucial to use sunscreen when using arbutin-containing products to prevent sun damage.
Regulatory Status
Arbutin is approved for use in cosmetic products in many countries. However, the concentration of arbutin in products is often regulated to ensure safety. For instance, in the European Union, the use of hydroquinone, a related compound, is restricted, but arbutin is permitted in lower concentrations.
Comparison with Other Skin-Lightening Agents
Arbutin is often compared to other skin-lightening agents such as hydroquinone, kojic acid, and vitamin C. Here’s how it stacks up:
- Hydroquinone: While hydroquinone is a potent skin-lightening agent, it can cause irritation and is banned in some countries. Arbutin is a safer alternative with fewer side effects.
- Kojic Acid: Both arbutin and kojic acid inhibit tyrosinase, but arbutin is generally considered more stable and less irritating.
- Vitamin C: Vitamin C is an antioxidant that also helps in lightening the skin. It can be used in conjunction with arbutin for enhanced effects.
Arbutin (Uva Ursi, Pipsissewa, blueberry leaves, Pear fruit and skin & tree bark) is metabolized in the body to become the urinary antiseptic, hydroquinone.
A natural skin lightening/whitening agent. It works by slowly releasing hydroquinone through hydrolysis, which in turn blocks Tyrosinase activity and reduces the skin’s melanin (pigmentation) production. In cosmetics, this ingredient appears in two different forms: Alpha-Arbutin or Beta-Arbutin. It is claimed that Alpha Arbutin has a stronger inhibitory action than Beta Arbutin. Due to patenting concerns, most skin care products contain plant extracts that contain Arbutin (e.g. bearberry, pear, blueberry), rather than pure Arbutin. Used in a variety of cosmetics, particularly ones aimed at lightening the skin such as lotions, crèmes, serums, cleansers, and spot treatments.
ARTICLES/STUDIES
Bone Effects
- Arbutin suppresses osteosarcoma progression via miR-338-3p/MTHFD1L and inactivation of the AKT/mTOR pathway.
- Insights into Arbutin Effects on Bone Cells: Towards the Development of Antioxidant Titanium Implants.
- Veronica austriaca L. Extract and Arbutin Expand Mature Double TNF-alpha/IFN-gamma Neutrophils in Murine Bone Marrow Pool.
- Rosmarinic acid and arbutin suppress osteoclast differentiation by inhibiting superoxide and NFATc1 downregulation in RAW 264.7 cells.
Cancer
- Arbutin suppresses osteosarcoma progression via miR-338-3p/MTHFD1L and inactivation of the AKT/mTOR pathway.
- The Effect of Arbutin on The Expression of Tumor Suppressor P53, BAX/BCL-2 Ratio and Oxidative Stress Induced by Tert-Butyl Hydroperoxide in Fibroblast and LNcap Cell Lines.
- Capsaicin reverses the inhibitory effect of licochalcone A/beta-Arbutin on tyrosinase expression in b16 mouse melanoma cells.
- Inhibitory effects of alpha-arbutin on melanin synthesis in cultured human melanoma cells and a three-dimensional human skin model.
Hyperpigmentation
- Are Natural Ingredients Effective in the Management of Hyperpigmentation? A Systematic Review.
- Arbutin encapsulated micelles improved transdermal delivery and suppression of cellular melanin production.
- Analysis of the effects of hydroquinone and arbutin on the differentiation of melanocytes.
Tyrosinase Inhibitor
Immune System
- Role of Metabolism by Intestinal Bacteria in Arbutin-Induced Suppression of Lymphoproliferative Response in vitro.
- In vitro safety assessment of the strawberry tree (Arbutus unedo L.) water leaf extract and arbutin in human peripheral blood lymphocytes.
Neuroprotective
Arbutin attenuates hydrogen peroxide-induced oxidative injury through regulation of microRNA-29a in retinal ganglion cells. - optic nerve injury
Parkinson's Disease
Radioprotective
- Radioprotective Effect of Arbutin in Megavoltage Therapeutic X-irradiated Mice using Liver Enzymes Assessment. Arbutin is a strong radioprotector for reducing the radiation effect on the whole-body tissues by measuring ALP, ALT and AST enzyme activity levels.
- Comparative study on the photostability of arbutin and deoxy arbutin: sensitivity to ultraviolet radiation and enhanced photostability by the water-soluble sunscreen, benzophenone-4.
- Effects of Arbutin on Radiation-Induced Micronuclei in Mice Bone Marrow Cells and Its Definite Dose Reduction Factor.
Wound Healing
- Alpha-Arbutin Promotes Wound Healing by Lowering ROS and Upregulating Insulin/IGF-1 Pathway in Human Dermal Fibroblast.
- Arbutin and decrease of potentially toxic substances generated in human blood neutrophils.
Other Effects
- Action of tyrosinase on alpha and beta-arbutin; A kinetic study.
- The effect of arbutin on lipid peroxidation and antioxidant capacity in the serum of cyclosporine-treated rats.
- Alleviation effect of arbutin on oxidative stress generated through tyrosinase reaction with L-tyrosine and L-DOPA.
- Lipid composition determines the effects of arbutin on the stability of plant membranes.
- Anti-melanogenic effects of extracellular vesicles derived from plant leaves and stems in mouse melanoma cells and human healthy skin.
- The Efficacy of Umbelliferone, Arbutin, and N-Acetylcysteine to Prevent Microbial Colonization and Biofilm Development on Urinary Catheter Surface: Results from a Preliminary Study.
- Hypoglycemic activity of Pyrus biossieriana Buhse leaf extract and arbutin Inhibitory effects on alpha amylase and alpha glucosidase.