The mechanisms of melanogenesis inhibition by glabridin: molecular docking, PKA/MITF and MAPK/MITF pathways

Glabridin is the main ingredient of hydrophobic fraction in licorice extract and has been shown to have anti-melanogenesis activity in skins. However, the underlying mechanism(s) remain not completely understood. The aim of this study is thus to elucidate the possible mechanisms related to the melan...

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Main Authors: Chunxing Pan, Xiaoying Liu, Yating Zheng, Zejun Zhang, Yongliang Li, Biao Che, Guangrong Liu, Lanyue Zhang, Changzhi Dong, Haji Akber Aisa, Zhiyun Du, Zhengqiang Yuan
Format: Article
Language:English
Published: Tsinghua University Press 2023-01-01
Series:Food Science and Human Wellness
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Online Access:http://www.sciencedirect.com/science/article/pii/S2213453022001185
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author Chunxing Pan
Xiaoying Liu
Yating Zheng
Zejun Zhang
Yongliang Li
Biao Che
Guangrong Liu
Lanyue Zhang
Changzhi Dong
Haji Akber Aisa
Zhiyun Du
Zhengqiang Yuan
author_facet Chunxing Pan
Xiaoying Liu
Yating Zheng
Zejun Zhang
Yongliang Li
Biao Che
Guangrong Liu
Lanyue Zhang
Changzhi Dong
Haji Akber Aisa
Zhiyun Du
Zhengqiang Yuan
author_sort Chunxing Pan
collection DOAJ
description Glabridin is the main ingredient of hydrophobic fraction in licorice extract and has been shown to have anti-melanogenesis activity in skins. However, the underlying mechanism(s) remain not completely understood. The aim of this study is thus to elucidate the possible mechanisms related to the melanogenesis suppression by glabridin in cultured B16 murine melanoma cells and in UVA radiation induced hyperpigmentation model of BALB/c mice as well. Molecular docking simulations revealed that between catalytic core residues and the compound. The treatment by glabridin significantly downregulated both transcriptional and/or protein expression of melanogenesis-related factors including melanocyte stimulating hormone receptor (MC1R), microphthalmia-associated transcription factor (MITF), tyrosinase (TYR), TYR-related protein-1 (TRP-1) and TRP-2 in B16 cells. Both PKA/MITF and MAPK/MITF signaling pathways were found to be involved in the suppression of melanogenesis by glabridin in B16 cells. Also in vivo glabridin therapy significantly reduced hyperpigmentation, epidermal thickening, roughness and inflammation induced by frequent UVA exposure in mice skins, thus beneficial for skin healthcare. These data further look insights into the molecular mechanisms of melanogenesis suppression by glabridin, rationalizing the application of the natural compound for skin healthcare.
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spelling doaj-art-8331b75f2dc14b1798c85a1e2984ce3b2025-02-03T05:15:36ZengTsinghua University PressFood Science and Human Wellness2213-45302023-01-01121212222The mechanisms of melanogenesis inhibition by glabridin: molecular docking, PKA/MITF and MAPK/MITF pathwaysChunxing Pan0Xiaoying Liu1Yating Zheng2Zejun Zhang3Yongliang Li4Biao Che5Guangrong Liu6Lanyue Zhang7Changzhi Dong8Haji Akber Aisa9Zhiyun Du10Zhengqiang Yuan11School of Biomedical and Pharmaceutical Sciences, Guangdong University of Technology, Guangzhou 510006, ChinaInfinitus(China) Company Ltd., Guangzhou 510663, ChinaSchool of Biomedical and Pharmaceutical Sciences, Guangdong University of Technology, Guangzhou 510006, ChinaSchool of Biomedical and Pharmaceutical Sciences, Guangdong University of Technology, Guangzhou 510006, ChinaFoshan Allen Conney Biological Technology Co., Ltd., Foshan 528225, ChinaInfinitus(China) Company Ltd., Guangzhou 510663, ChinaInfinitus(China) Company Ltd., Guangzhou 510663, ChinaSchool of Biomedical and Pharmaceutical Sciences, Guangdong University of Technology, Guangzhou 510006, ChinaUniversité Paris Diderot, Sorbonne Paris Cité, ITODYS, UMR 7086 CNRS, FranceThe Key Laboratory of Plant Resources and Chemistry of Arid Zone, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Ürümqi 830011, ChinaSchool of Biomedical and Pharmaceutical Sciences, Guangdong University of Technology, Guangzhou 510006, China; Corresponding authors at: School of Biomedical and Pharmaceutical Sciences, Guangdong University of Technology, Guangzhou 510006, ChinaSchool of Biomedical and Pharmaceutical Sciences, Guangdong University of Technology, Guangzhou 510006, China; Corresponding authors at: School of Biomedical and Pharmaceutical Sciences, Guangdong University of Technology, Guangzhou 510006, ChinaGlabridin is the main ingredient of hydrophobic fraction in licorice extract and has been shown to have anti-melanogenesis activity in skins. However, the underlying mechanism(s) remain not completely understood. The aim of this study is thus to elucidate the possible mechanisms related to the melanogenesis suppression by glabridin in cultured B16 murine melanoma cells and in UVA radiation induced hyperpigmentation model of BALB/c mice as well. Molecular docking simulations revealed that between catalytic core residues and the compound. The treatment by glabridin significantly downregulated both transcriptional and/or protein expression of melanogenesis-related factors including melanocyte stimulating hormone receptor (MC1R), microphthalmia-associated transcription factor (MITF), tyrosinase (TYR), TYR-related protein-1 (TRP-1) and TRP-2 in B16 cells. Both PKA/MITF and MAPK/MITF signaling pathways were found to be involved in the suppression of melanogenesis by glabridin in B16 cells. Also in vivo glabridin therapy significantly reduced hyperpigmentation, epidermal thickening, roughness and inflammation induced by frequent UVA exposure in mice skins, thus beneficial for skin healthcare. These data further look insights into the molecular mechanisms of melanogenesis suppression by glabridin, rationalizing the application of the natural compound for skin healthcare.http://www.sciencedirect.com/science/article/pii/S2213453022001185GlabridinMelanogenesisMolecular dockingPKA/MITF pathwayMAPK/ MITF pathway
spellingShingle Chunxing Pan
Xiaoying Liu
Yating Zheng
Zejun Zhang
Yongliang Li
Biao Che
Guangrong Liu
Lanyue Zhang
Changzhi Dong
Haji Akber Aisa
Zhiyun Du
Zhengqiang Yuan
The mechanisms of melanogenesis inhibition by glabridin: molecular docking, PKA/MITF and MAPK/MITF pathways
Food Science and Human Wellness
Glabridin
Melanogenesis
Molecular docking
PKA/MITF pathway
MAPK/ MITF pathway
title The mechanisms of melanogenesis inhibition by glabridin: molecular docking, PKA/MITF and MAPK/MITF pathways
title_full The mechanisms of melanogenesis inhibition by glabridin: molecular docking, PKA/MITF and MAPK/MITF pathways
title_fullStr The mechanisms of melanogenesis inhibition by glabridin: molecular docking, PKA/MITF and MAPK/MITF pathways
title_full_unstemmed The mechanisms of melanogenesis inhibition by glabridin: molecular docking, PKA/MITF and MAPK/MITF pathways
title_short The mechanisms of melanogenesis inhibition by glabridin: molecular docking, PKA/MITF and MAPK/MITF pathways
title_sort mechanisms of melanogenesis inhibition by glabridin molecular docking pka mitf and mapk mitf pathways
topic Glabridin
Melanogenesis
Molecular docking
PKA/MITF pathway
MAPK/ MITF pathway
url http://www.sciencedirect.com/science/article/pii/S2213453022001185
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