Enhanced Whitening Effect of the Formulations via Inhibition of Tyrosinase Activity by Combination of 4-n-Butylresorcinol, Licochalcone A and Glabridin at an Optimal Ratio

4-正丁基间苯二酚、光甘草查尔酮A和光甘草定以最佳比例组合,通过抑制酪氨酸酶活性增强配方的美白效果。

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Abstract

BACKGROUND: Companies launch tons of skin-whitening products to cater to the consumer market. Though skin-whitening cosmeceuticals are continuously developing, most cosmeceuticals are used alone, there is very little academic research conducting investigations into the effect of skin-whitening cosmeceutical combinations. OBJECTIVE: In this study, we aimed to screen out skin whitening agents and determine their optimal ratio to develop a formula with this combination. Further, to verify the skin whitening efficacy of blue light-induced in in vivo models with or without UV and clinical tests were performed. MATERIALS AND METHODS: Molecular docking simulations were used to screen out the best combination of skin whitening agents when combined in different ratios. In vitro tyrosinase activity and melanin content experiments helped to verify the best ratio combination. Clinical trials were also conducted to confirm the skin whitening efficacy on human skin. RESULTS: 4-n-butylresorcinol, licochalcone A, and glabridin exhibited stronger binding affinities to tyrosinase, and the best combination molar ratio is 5:1:1, which could inhibit both tyrosinase activity and melanin content in vitro. Further, the formulation containing this combination showed good skin whitening efficacy and could even prevent UVA and blue light-induced pigmentation. CONCLUSION: The 5:1:1 molar ratio of 4-n-butylresorcinol, licochalcone A, and glabridin was the best ratio that could inhibit both tyrosinase activity and melanin content. The formulation containing this ratio combination can enhance the skin whitening efficacy and also can prevent the UV and blue light induced skin pigmentation.

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