Abstract

Growing scientific evidence indicates that Achillea biebersteinii is a valuable source of active ingredients with potential cosmetic applications. However, the data on its composition and pharmacological properties are still insufficient. This study aims to optimize the extraction procedure of the plant material, evaluate its phytochemical composition, and compare anti-tyrosinase potential of A. biebersteinii extracts obtained by various methods. In order to identify compounds responsible for the tyrosinase inhibitory activity of A. biebersteinii, the most active anti-tyrosinase extract was fractionated by column chromatography. The fractions were examined for their skin lightening potential by mushroom and murine tyrosinase inhibitory assays and melanin release assay. HPLC-ESI-Q-TOF-MS/MS analysis of the total extract revealed the presence of several phenolic acids, flavonoids, flavonoid glucosides, and carboxylic acid. Among them, fraxetin-8-O-glucoside, quercetin-O-glucopyranose, schaftoside/isoschaftoside, gmelinin B, 1,3-dicaffeoylquinic acid (1,3-DCQA), and ferulic acid were found in the fractions with the highest skin lightening potential. Based on obtained qualitative and quantitative analysis of the fractions, it was assumed that the caffeoylquinic acid derivatives and dicaffeoylquinic acid derivatives are more likely responsible for mushroom tyrosinase inhibitory activity of A. biebersteinii extracts and fractions. Ferulic acid was proposed as the most active murine tyrosinase inhibitor, responsible also for the reduced melanin release from B16F10 murine melanoma cells.

Highlights

  • Nowadays, the ingredients used in cosmetic formulations are required to perform multiple functions and protect the skin from the harmful effects of the environmental factors

  • Even if the DCQA derivatives were proved to exhibit the strongest tyrosinase inhibitory properties in the previously published articles, interestingly, our study showed that fraction 12 was found to be active even if it did not contain the DCQA derivatives, but simple organic and phenolic acids

  • Achillea biebersteinii extracts and fractions were confirmed as a source of potential cosmetic ingredients with significant skin lightening properties and antioxidant activity

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Summary

Introduction

The ingredients used in cosmetic formulations are required to perform multiple functions and protect the skin from the harmful effects of the environmental factors. Excessive exposure to UVR carries a significant health risk, including the development of skin cancer, as well as cause esthetic problems such as pigmentation disorders. Uneven skin pigmentation is caused by the dysregulation of the melanogenesis process by UVR, inflammation, hormonal imbalance, or several chemical compounds, including medicines [1]. In response to oxidative stress, keratinocytes are known to secrete α-melanocyte-stimulating hormone (α-MSH) that induce melanogenesis by the surrounding melanocytes, thereby preventing the UVR-induced damage [4]. The main benefits of plant extracts used in skin care products are antioxidant properties, antimicrobial activity, and inhibition of tyrosinase, leading to the reduction of hyperpigmentation disorders [7,8]

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