Phytochemicals in the treatment of hyperpigmentation |
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Phytochemicals in the treatment of hyperpigmentation

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Treating hyperpigmentation can be challenging and various modalities are needed to aid in the improvement of topical treatments. Cosmeceuticals are topical cosmetic-pharmaceutical hybrids containing biologically active ingredients that may improve the appearance of skin and are increasingly popular alternatives to standard agents. Among cosmeceuticals – plant-derived compounds known as phytochemicals, have been shown to have a multitude of cellular actions for various dermatological diseases.

The purpose of a review published in Botanics: Targets and Therapy was to examine the latest clinical studies using plant-derived compounds and their effectiveness in the management of hyperpigmentation disorders. 

Flavonoids are naturally occurring phenolic phytochemicals that possess a host of biological properties, in vitro. Some phytochemicals and their mechanisms of action on various dermatological conditions have been enlisted below(scroll to right for full table view in mobile browsers):


Plant Source

Pigment Disorder

Depigmenting Mechanism


Bearberry, California buckeye, cranberry and blueberry

Solar lentigines

Inhibit tyrosinase and DHICA polymerase


Candeia tree bark

Dark spots

Rich in natural α-bisabolol that acts on melanocytes receptors to reduce irritation reactions

Melanogenesis inhibition


Green vegetables, beans and cereal grains

hyperpigmented spots, fine lines and wrinkles, red blotchiness and skin sallowness (yellowing)

It is an amide of vitamin B3 (niacin) – has antipruritic, antimicrobial, vasoactive, photo-protective, sebostatic and lightening effects.

Controls the NFκB-mediated transcription of signalling molecules by inhibiting the nuclear poly (ADP-ribose) polymerase-1 (PARP-1)



UVA and UVB tanned skin (with solar simulator)

Inhibits alpha MSH-induced melanogenesis by suppressing cAMP



UVB-induced pigmentation

Inhibit tyrosinase

Aldavine 5x

Ascophyllum Nodosum Extract and Asparagopsis Armata Extract

Dark circles, rosacea, spider veins, sensitive/irritated skin, sun burn, razor burn and after laser treatment

Inhibits VEGF, PGE2, MMP-2 and angiogenesis

Lanachrys 2b

Chrysanthellum indicum

Reduces the appearance of under eye bags

Binds to alpha-2 receptor to activate lipolysis; scavenges free radicals


Pterocarpus Marsupium

Lightens skin tone and supports dyschromia management

Scavenges free radicals, exhibits good melanogenesis potential and protects from harmful UV rays 


Citrus fruits

Lightens skin tone, UV protection

Inhibit tyrosinase; antioxidant of collagen; inhibit tyrosinase activity


Silybum marianum (standardized extract)


Inhibit l-DOPA oxidation activity of tyrosinase

In summary, it was stated that a large variety of safe and effective skin-lightening botanicals exist as potential alternatives to current products, such as, hydroquinone. Natural extracts represent a large repository of ingredients for skin-lightening cosmeceuticals. Dermatologists and primary care physicians would benefit from familiarizing themselves with the evidence supporting or refuting the use of botanically derived products for hyperpigmentation treatment, as patients are becoming increasingly interested in natural alternatives.


  • Botanics: Targets and Therapy. 2016 Sept 16;6. doi: 10.2147/BTAT.S691132.
  • Inspiring ingredients. Available at: Accessed on 16 July 2020.
  • Aldavine™5x. Available at: Accessed on 16 July 2020.
  • PteroWhite® 90%. Available at: Accessed on 16 July 2020.
  • pTeroWhite®. Available at: Accessed on 16 July 2020.
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