4-己基间苯二酚的美白功效及新作用机理探讨  

Skin brightening benefit of 4-hexylresorcinol in vivo and in vitro and its underlying mechanism

作　　者：顾学兰 张红 肖雪 周壮 瞿珏 施奕冰 Xuelan Gu;Hong Zhang;Xue Xiao;Zhuang Zhou;Jue Qu;Yibing Shi(Unilever Research&Development Center,Shanghai 200335,China)

机构地区：[1]联合利华上海研发中心,上海200335

出　　处：《日用化学工业（中英文）》2024年第12期1437-1446,共10页China Surfactant Detergent & Cosmetics

摘　　要：文章旨在系统评价4-己基间苯二酚(4-HR)的皮肤美白功效,并探索其新的作用机理。临床测试以祛斑美白化妆品功效原料研究技术指导原则为指南,开展了一项为期8周、安慰剂对照的人体测试研究,结果表明精华露中添加0.4%4-HR能显著提高皮肤ITA°值,降低皮肤黑色素含量。表面涂抹等量4-HR能明显提高体外重组3D黑素模型的表观亮度,显著减少黑色素含量。基于角质细胞的转录组学分析提示被4-HR影响表达的基因除参与皮肤发育过程、角质化过程,还影响氧化活性调控、细胞自噬功能等。进一步体外研究证明,4-HR能够抑制蓝光诱导的活性氧水平,减轻角质形成细胞的氧化应激反应。在人角质-黑素细胞共培养模型中,4-HR不仅能降低黑素含量,同时还能明显提高细胞自噬标记物LC3表达。加入自噬抑制剂氯喹后,4-HR对黑色素含量的抑制作用也随之显著降低。研究表明,添加0.4%4-HR的精华露具有良好的美白功效,4-HR可能以减轻氧化应激、调节细胞自噬功能的新作用机理而起到美白作用。4-Hexylresorcinol(4-HR),a potent tyrosinase inhibitor,has been used as an even-tone active ingredient for skin care application since 2007.While the skin brightening efficacy of 4-HR in Chinese population has not been thoroughly investigated and its significance in keratinocytes has not been fully raveled.This study aims to evaluate the skin brightening potential of 4-HR in vivo and in vitro and explore its new mechanism of action through transcriptome approach.The skin brightening effect of 0.4%4-HR in a facial serum was assessed in an 8-week,double-blinded,placebo-controlled,and randomized clinical study in 67 Chinese participants.ITA°,melanin index(MI)and visual grading were measured at baseline and 2,4 and 8 weeks after use.A pigmented living skin equivalent(pLSE)model constructed from Asian skin cells was utilized to assess the brightening efficacy of 0.4%4-HR by measuring the model’s brightness(L^(*)value)and melanin content.Then,transcriptomic analysis of 4-HR treated human epidermal keratinocytes was conducted,and the two in vitro models were adopted for hypothesis validation afterwards.In the clinical study,the result shows both 0.4%4-HR serum and placebo chassis can significantly improve all measures as compared to baseline at the 2,4,and 8 weeks.Furthermore,0.4%HR serum demonstrates a better performance in increasing ITA°as early as 2 weeks of application and decreasing MI value than the placebo group at Week 2.In the pLSE model,0.4%4-HR with topical application evidently increases L^(*)value by 15.88%and decreases melanin content by 47.61%compared to UVB group.RNA-sequencing analysis implies that 4-HR can regulate multiple biological processes including skin development,keratinocyte differentiation,oxidant activity and autophagy function.In the blue-light challenged human keratinocytes model,4-HR shows a significant ROS suppression capacity.In the keratinocytes-melanocytes co-culture model,4-HR prompts autophagy activity and decreases melanin content.Most importantly,the melanin inhibitory activit

关 键 词：皮肤美白 4-己基间苯二酚 自噬 氧化 转录学分析 

分 类 号：TQ658[化学工程—精细化工]