Abstract

Controlling unwanted hyperpigmentation is a major challenge in dermatology and cosmetology, and safe and efficacious antimelanogenic agents are deemed useful for this purpose. p-Coumaric acid is a natural metabolite contained in many edible plants, and its antioxidant activities in reducing oxidative stress and inflammatory reactions have been demonstrated in various experimental models. p-Coumaric acid has the optimal structure to be a competitive inhibitor of tyrosinase that catalyzes key reactions in the melanin biosynthetic pathway. Experimental evidence supports this notion as it was found to be a more potent inhibitor of tyrosinase, especially toward human enzymes, than other well-known tyrosinase inhibitors such as arbutin and kojic acid. p-Coumaric acid inhibited melanin synthesis in murine melanoma cells, human epidermal melanocytes, and reconstituted three-dimensional human skin models. Ex-vivo skin permeation experiments and in-vivo efficacy tests for p-coumaric acid confirmed its efficient transdermal delivery and functional efficacy in reducing erythema development and skin pigmentation due to ultraviolet radiation exposure. Human studies further supported its effectiveness in hypopigmentation and depigmentation. These findings suggest that p-coumaric acid has good potential to be used as a skin-lightening active ingredient in cosmetics. Future studies are needed to extensively examine its safety and efficacy and to develop an optimized cosmetic formulation for the best performance in skin lightening.

Highlights

  • Melanin synthesis is an important topic in medical and cosmetic industries owing to its relevance to photo-protection, carcinogenesis processes, and skin pigmentation disorders [1,2,3,4,5]

  • This review focused on the antimelanogenic properties of p-coumaric acid to extensively examine its potential as an active ingredient in cosmetics

  • P-coumaric acid has a unique chemical structure, and many of its biochemical properties are suitable for its use as a skin-lightening cosmetic ingredient. p-Coumaric acid inhibited the catalytic activity of tyrosinase in vitro, especially toward human tyrosinase, more effectively than other structurally similar compounds, especially when L-tyrosine was used as the substrate. p-Coumaric acid inhibited tyrosinase gene expression stimulated by α-MSH

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Summary

Introduction

Melanin synthesis is an important topic in medical and cosmetic industries owing to its relevance to photo-protection, carcinogenesis processes, and skin pigmentation disorders [1,2,3,4,5]. Hydroquinone is primarily used as a pharmacotherapy agent, and a combination drug including retinoid is used, but it can cause adverse effects such as skin irritation, allergy, mutations, and cancer [10]. Various active ingredients such as arbutin and kojic acid have been used to control skin pigmentation [11,12,13]. P-coumaric acid was found to be a potent and selective inhibitor of human tyrosinase [18]. Considering the need for natural skin lightening agents in cosmetics, it is of interest to scrutinize recent literature on the biological activities of p-coumaric acid. This review focused on the antimelanogenic properties of p-coumaric acid to extensively examine its potential as an active ingredient in cosmetics

Skin and Pigmentation
Melanin Synthetic Pathway and Its Regulation
Literature
Comparison of p-Coumaric Acid and Other Tyrosinase Inhibitors
Skin and Cell Membrane Permeability of p-Coumaric Acid
11. Protective Effects of p-Coumaric Acid against UV
Findings
12. Conclusions and Future Directions
Full Text
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