Abstract

BackgroundCoptis chinensis (C. chinensis) contains various antioxidants, including berberine, epiberberlin, ferulic acid, magnoflorine, palmatine, and worenine, which have antibacterial, anti-inflammatory, haemostatic, hypotensive, and anticancer effects. In the present study, the melanogenesis-inhibiting effects of C. chinensis were investigated and the molecular mechanisms were elucidated.MethodsThe melanogenesis-inhibiting effect of C. chinensis was verified by measuring melanin contents, melanogenesis-related tyrosinase activities, and mRNA and protein expression levels of tyrosinase and microphthalmia-associated transcription factor (MITF). In addition, changes in miR-340 expression by C. chinensis were verified, and the activity of the miR-340 binding site of the target MITF gene was determined using luciferase reporter assays.ResultsAssays of melanin contents showed that C. chinensis had a skin-whitening effect and controlled mRNA and protein expression levels of tyrosinase. However, C. chinensis controlled protein levels of MITF without affecting mRNA levels. Determinations of miR-340 expression, which directly influences MITF translation, showed increased miR-340 mRNA levels in the presence of C. chinensis. Finally, luciferase reporter assays of the binding site on MITF showed that C. chinensis inhibits melanogenesis by directly controlling the miR-340–MITF axis.ConclusionsThe results of the present study verified the skin-whitening effect of C. chinensis and its molecular mechanisms and indicated that C. chinensis has high potential as an ingredient in skin-whitening cosmetics.

Highlights

  • Coptis chinensis (C. chinensis) contains various antioxidants, including berberine, epiberberlin, ferulic acid, magnoflorine, palmatine, and worenine, which have antibacterial, anti-inflammatory, haemostatic, hypotensive, and anticancer effects

  • The results of the present study verified the skin-whitening effect of C. chinensis and its molecular mechanisms and indicated that C. chinensis has high potential as an ingredient in skin-whitening cosmetics

  • The present study shows that C. chinensis extracts inhibit melanogenesis by decreasing tyrosinase activity (Fig. 2a) and expression (Fig. 2b, d)

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Summary

Introduction

Coptis chinensis (C. chinensis) contains various antioxidants, including berberine, epiberberlin, ferulic acid, magnoflorine, palmatine, and worenine, which have antibacterial, anti-inflammatory, haemostatic, hypotensive, and anticancer effects. MITF is a critical transcription factor for melanogenesis and is known to enhance the transcription of tyrosinase and its related proteins TRP-1 and TRP-2 (Buscà and Ballotti 2000; Saha et al 2006). Α-MSH is produced by melanocytes, Langerhans cells, fibroblasts, and endotheliocytes and, in keratinocytes following exposure to ultraviolet light (Chakraborty et al 1996). Modulation of intracellular signal transduction by α-MSH is recognized as an important target for the control of melanogenesis (Nasti and Timares 2015). Multiple studies report effective skin-whitening effects of treatments that modulate MITF expression, and the melanogenic gene tyrosinases, TRP-1 and TRP-2, have been implicated, control of tyrosinase activity and expression did not affect melanogenesis in isolation

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