licorice, bearberry, oranges, green tea

Hyper Intelligence

The long list of ingredients available for treating hyperpigmentation reads partially like a science textbook, and partially like a nature encyclopedia. But thanks to skincare experts, all of the terms make sense when placed into a treatment context.

“There are many stages involved in the formation of pigmentation, and therefore a combination of ingredients that intervene at various stages of melanogenesis are necessary to achieve the desired results,” explains G.M. Collins’ Asquith. Adds GlyMed Plus’ Roberts, “Tyrosinase inhibitors would be key to control pigmentation and brighten/lighten existing pigmentation, and they’re powerful antioxidants. There are many botanical types of tyrosinase inhibitors, and each works in a different capacity to either block production of tyrosine or reduce other aspects of the equation.”

Here are the ingredients you’re most likely to see listed on the packaging of hyperpigmentation products. Some botanical ingredients are listed by their common plant names; others by their less easily recognizable extract names.

1-Methylhydantoin-2 IMIDE is a natural amino acid derivative that inhibits melanosome transfer, interfering in another process of melanogenesis.
Achromaxyl is a fermented and hydrolyzed protein that inhibits tyrosinase activity.
Alpha arbutin is a botanical that “prevents hyperproduction of melanin and further activation of tyrosinase, thus blocking melanin synthesis for better control over skin tone and brown spots,” says Dasha Saian, operations manager for SAIAN.
Alpha hydroxy acids work to peel off stained parts of the skin, though stains return.
Arginine, a natural amino acid, can hasten repair of sun-damaged tissue.
Azelic acid “is a dicarboxylic acid that has minimal effect on normal pigmentation and the greatest effect on heavily pigmented melanocytes, making it very effective in treating post-inflammatory hyperpigmentation (PIH) and darker skin of color,” says Roberts. "It inhibits tyrosinase as well as DNA synthesis and mitochondrial activity in hyperactive melanocytes. Azelic acid may be the most thoroughly researched and studied compound next to hydroquinone.”
Bearberry inhibits tyrosinase activity and may lead to a direct reduction of melanin.
Bellis daisy is a wildflower that decreases tyrosinase synthesis, reduces keratinocyte production and blocks the binding and transfer of melanocytes.
Diacetyl boldine is an extract from the bark of the Chilean boldo tree that works at the tyrosinase level to reduce and control pigmentation. “Diacetyl boldine is encapsulated into microliposomes to make it more effective at reaching its target in the skin, more resistant to degradation and more consistent in its results,” says Pevonia’s Jurist.
Glycolic acid helps remove the uppermost layers of the skin via exfoliation, providing a more even appearance.
Grape seed contains proanthocyanidins, which help lighten UV-induced hyperpigmentation.
Green tea contains polyphenols that may interfere with pigment transfer, and provides UV protection, too.
Hexapeptide is a skin-lightening peptide (see In the Pipeline on page 56 for more on peptides for treating hyperpigmentation).
Hydroquinone (see next page)
Kojic acid “effectively exfoliates the skin and helps reduce the dark pigmentation,” notes Saian. Roberts adds, “It works by decreasing the number of melanosomes that are generated, which leads to less transferred pigment.”
L-ascorbic acid 2-glucoside is a botanical that inhibits tyrosinase activity. “It interacts with the copper ions and converts the dopaquinone back to L-Dopa, preventing melanin formation,” says Roberts.
Lactic acid exfoliates and hastens cell turnover, and helps ward off adult acne.
Licorice root (extracts include licochalcone and glabriden) inhibits tyrosinase and functions as an anti-inflammatory. “Licorice root and its derivatives, such as licochalcone, are strong antioxidants with brightening effects,” says Mark Lees. Adds Roberts, “Licorice has the ability to absorb UVA and UVB rays; some claims say it’s more powerful than kojic acid and 75 times more effective than ascorbic acid.”
Magnesium ascorbyl phosphate (MAP) is a vitamin C derivative. “It’s popular in Japan, but vitamin C acids often cause irritant problems,” Lees says.
Mulberry root extracts are anti-inflammatory, and potent inhibitors of tyrosinase.
Mushroom extract and white willow bark extract decrease melanin production and inflammatory response from triggers.
Norwegian kelp extract interrupts the communication between the melanocyte and keratinocyte, and increases controlled exfoliation, helping to remove pigmented areas.
Oligopeptide-34 decreases the MITF gene expression, resulting in a reduced level of tyrosinase. “Oligopeptide-68 is one of the most effective skin brightening ingredients,” says Lees. “Due to its biomimetic liposomic time-release peptide delivery system, identical to the skin’s own structure and composition, it’s capable of rapidly equalizing skin tone and reducing unwanted hyperpigmentation.”
Pidobenzone is a melanin suppressant. “It makes no lightening claim, though it’s pretty effective,” Lees notes.
Retinol triggers cell division to promote more rapid turnover and exfoliation.
Rosemary has an inhibitory effect on carnosic acid and tyrosinase activity.
Stone crop suppresses melanin and offers UV protection.
Sulforawhite activates the proteasome system, which is responsible for breaking down the lipofuscin.
Turmeric oil is a natural astringent and antioxidant.
Tetrahydrocurcumin (THC) inhibits tyrosinase activity.
Vitamin C “Once the spots reveal themselves, reach for topical products that are high in vitamin C, which has been shown to be effective in reducing hyperpigmentation and providing powerful antioxidant protection,” advises Jeff Murad, VP of product development at Murad.
Yellow dock is a natural astringent with acne-banishing properties. It also inhibits tyrosinase activity.