Phytochemicals in the treatment of hyperpigmentation

Figures & data

Figure 1 Phytochemicals

Table 1 Overview of clinical studies of botanical extracts

Botanical component	Plant source	Depigmenting mechanism	Pigment disorder	Comparison	Major results	Limitations	Author, year
Aloesin	Aloe vera	Competitively inhibit tyrosinase, decrease DOPA oxidase	UV radiation hyperpigmentation	1) Vehicle control 2) Arbutin treated 3) Aloesin and arbutin treated	1) Aloesin treatment suppressed pigmentation by 34% 2) Arbutin by 43.5% 3) Cotreatment by 63.3% compared with the control 4) Aleosin treatment showed pigmentation suppression in a dose-dependent manner (P<0.05)	1) No between group comparison done	Choi et al,^Citation15 2002
Alpha-bisabolol	Chamomile	Inhibits alpha-MSH-induced melanogenesis by suppressing cAMP	UVA and UVB tanned skin (with solar simulator)	Vehicle cream	1) Significantly effective lightening as measured by spectrophotometer than vehicle control 2) No difference between groups detected by clinical evaluation	1) Lightening effect measured with spectrophotometer not detected in clinical evaluation 2) No description of clinical evaluation criteria	Lee et al,^Citation16 2010
Arbutin	Bearberry, California buckeye, cranberry, and blueberry	Inhibit tyrosinase, and DHICA polymerase	Solar lentigines	Vehicle control	The results of the clinical study demonstrated that arbutin provided a significant effect on overall skin lightening and moderate resolution of solar lentigines in Caucasian subjects	The test period for the study was from November to February, a period when complexion coloration generally lightens in the Northern Hemisphere	Boissy et al,^Citation20 2005
Ellagic acid	Green tea, strawberry, geranium, grapes, cherries, and walnuts	Copper chelation, decrease melanocyte proliferation	Melasma	1) Arbutin 2) Synthetic ellagic acid	Significant improvement in pigment density in all groups, with no statistical difference between them	Plant-derived ellagic acid not studied independently (treatment group received combination of synthetic and plant- derived ellagic acid)	Ertam et al,^Citation21 2008
Glabridin	Licorice	Inhibit tyrosinase	UVB-induced pigmentation	None	UVB-induced pigmentation and erythema in the skins of guinea pigs were inhibited by topical applications of 0.5% glabridin	Application on human skin and effects are unknown	Yokota et al,^Citation24 1998
Hesperidin	Citrus fruits	Inhibit tyrosinase, antioxidant of collagen	In vitro, human melanocytes	None	Photoprotective effect was obtained after hesperetin cream topical application when compared to the nontreatment group	Enhancers were added, and hesperidin was not studied independently	Huang et al,^Citation26 2010
		Induce melanin synthesis and tyrosinase activity	In vitro, human melanocytes	Control	Compared to control melanocytes, increased melanin production and tyrosinase activity 1.4- fold (P<0.01) and 1.1-fold (P<0.01), respectively	Conflicting results between studies	Usach et al,^Citation27 2015
Liquiritin	Licorice	Melanin dispersion, epidermal removal	Melasma	4% hydroquinone	Topical 4% liquiritin is significantly more effective than topical 2% liquiritin, and topical 2% liquiritin is also significantly more effective than 4% hydroquinone	Some patients used sunscreen while others did not. This factor was not considered in the analysis of the results	Zubair and Mujtaba,^Citation28 2009
Procyanidin	Pinus pinaster	Antioxidant and anti-inflammatory	Melasma	Placebo tablets containing starch	Treatment group with significantly improved Mexameter measurements and MASI scores compared with placebo	Procyanidin treatment was combined with vitamins A, C, and E and not studied independently	Handog et al,^Citation30 2009
Silymarin	Silybum marianum (standardized extract)	Inhibit L-DOPA oxidation activity of tyrosinase	Melasma	Vehicle control	1) All patients showed significant pigment improvement and lesion size reduction. 2) Effective in prevention of skin damage caused by UV sunlight	1) Patients advised to use sunscreen in addition to the treatment cream, possibly confounding the results of the stud	Altaei,^Citation33 2012

Note: Data from Fisk et al⁸ and Zhu and Gao.³

Abbreviations: cAMP, cyclic adenosine monophosphate; DOPA, 3,4-dihydroxyphenylalanine, DHICA, 5,6-dihydroxyindole-2-carboxylic acid; l-DOPA, l-3,4,-dihydroxyphenylalanine; MASI, Melasma Area and Severity Index; MSH, melanocyte-stimulating hormone; UV, ultraviolet; UVA, ultraviolet A; UVB, ultraviolet B.

Figure 2 Cosmeceutical mechanism of action for phytochemicals.

Abbreviation: l-DOPA, l-3,4,-dihydroxyphenylalanine; MSH, melanocyte-stimulating hormone.

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