Abstract

BackgroundBletilla striata is the main medicine of many skin whitening classic formulas in traditional Chinese medicine (TCM) and is widely used in cosmetic industry recently. However, its active ingredients are still unclear and its fibrous roots are not used effectively. The aim of the present study is to discover and identify its potential anti-melanogenic active constituents by zebrafish model and molecular docking.MethodsThe antioxidant activities were evaluated by 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity, 2,2′-azino-bis-(3-ethylbenthiazoline-6-sulphonic acid) (ABTS) radical scavenging activity and ferric reducing antioxidant power (FRAP) assay. The anti-melanogenic activity was assessed by tyrosinase inhibitory activity in vitro and melanin inhibitory in zebrafish. The chemical profiles were performed by ultra-high-performance liquid chromatography combined with quadrupole time-of-flight tandem mass spectrometry (UPLC-Q-TOF-MS/MS). Meanwhile, the potential anti-melanogenic active constituents were temporary identified by molecular docking.ResultsThe 95% ethanol extract of B. striata fibrous roots (EFB) possessed the strongest DPPH, ABTS, FRAP and tyrosinase inhibitory activities, with IC50 5.94 mg/L, 11.69 mg/L, 6.92 mmol FeSO4/g, and 58.92 mg/L, respectively. In addition, EFB and 95% ethanol extract of B. striata tuber (ETB) significantly reduced the melanin synthesis of zebrafish embryos in a dose-dependent manner. 39 chemical compositions, including 24 stilbenoids were tentatively identified from EFB and ETB. Molecular docking indicated that there were 83 (including 60 stilbenoids) and 85 (including 70 stilbenoids) compounds exhibited stronger binding affinities toward tyrosinase and adenylate cyclase.ConclusionThe present findings supported the rationale for the use of EFB and ETB as natural skin-whitening agents in pharmaceutical and cosmetic industries.

Highlights

  • Bletilla striata is the main medicine of many skin whitening classic formulas in traditional Chinese medicine (TCM) and is widely used in cosmetic industry recently

  • B. striata is the main medicine of many skin whitening classic formulas in TCM [16] and it is widely used in cosmetic industry recently [17]

  • The research results given by Chen et al indicated that 95% ethanol extract of B. striata possessed higher tyrosinase inhibitory activity than those of its water extract with inhibition rate of 68.36% in vitro [18], while the result of Huang et al showed that the inhibitory activity of B. striata water extract on tyrosinase was stronger than that of 95% ethanol extract with inhibition rate of 62% in vitro [19]

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Summary

Introduction

Bletilla striata is the main medicine of many skin whitening classic formulas in traditional Chinese medicine (TCM) and is widely used in cosmetic industry recently. The dried tuber of B. striata, known as Baiji, firstly recorded in Shennong’s Classic of Materia Medica, has been widely used as a traditional Chinese medicine (TCM) for thousands of years in China. B. striata is the main medicine of many skin whitening classic formulas in TCM [16] and it is widely used in cosmetic industry recently [17]. Its active ingredients are still unclear and even some research results were contrary. The research results by Lu et al [20] and Linghu et al [21] demonstrated that both water and 95% ethanol extract of B. striata, especially its chloroform fractionation, could inhibit B16 cell growth and induce its apoptosis in a concentrationdependent manner

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