4‐n‐butylresorcinol, a highly effective tyrosinase inhibitor for the topical treatment of hyperpigmentation

Kolbe, Ludger; Mann, Tobias; Gerwat, Wolfram; Batzer, Jan; Ahlheit, S.; Scherner, Cathrin; Wenck, Horst; Stäb, Franz

doi:10.1111/jdv.12051

Cited by 133 publications

(146 citation statements)

References 24 publications

(26 reference statements)

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“…3A, B). In addition, the 3D spheroids treated with vit (1, 3 µM), koj (300, 500 µM), cocoon (100, 500 ppm), and HQ (1, 5 µM), known as depigmentation agents, [9][10][11] had ca. 2-fold lower EGFP expression than that of the untreated control (Figs.…”

Section: Resultsmentioning

confidence: 99%

“…Melanin synthesis is mainly regulated by tyrosinase, which is the inhibition target of vit, Arb, koj, cocoon, and HQ, used as cosmetic and medical materials with depigmentation agents. [9][10][11] To investigate the depigmenting efficacy as shown by a combination of automated fluorescence microscopy and tyrosinase promoter-based fluorescent assay in 3D culture, images were acquired with an automated IN Cell Analyzer 1000 for the purpose of time-lapse acquisition in Ultra-Low Attachment 96-well plates. A combination assay using the IN Cell Analyzer 1000 makes potentially more efficient use of cost, time, and accuracy for the screening of skin-whitening ingredients, resulting in increased assay robustness.…”

Section: Resultsmentioning

confidence: 99%

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Development of Tyrosinase Promoter-Based Fluorescent Assay for Screening of Anti-melanogenic Agents

Lee

et al. 2015

Biological & Pharmaceutical Bulletin

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For screening of skin-whitening ingredients that modulate inhibition of melanogenesis, tyrosinase promoter-based assay using a three-dimensional (3D) spheroid culture technique is a beneficial tool to improve the accuracy of raw material screening in cosmetics through mimicking of the in vivo microenvironment. Although the advantages of high-throughput screening (HTS) are widely known, there has been little focus on specific cell-based promoter assays for HTS in identifying skin-whitening ingredients that inhibit accumulation of melanin. The aim of this study was therefore to develop a large-scale compatible assay through pTyr-EGFP, an enhanced green fluorescent protein (EGFP)-based tyrosinase-specific promoter, to seek potential melanogenesis inhibitors for cosmetic use. Herein, a stably transfected human melanoma cell line expressing EGFP under the control of a 2.2-kb fragment derived from the tyrosinase gene was generated. Spontaneous induction of the tyrosinase promoter by 3D spheroid culture resulted in increased expression of EGFP, providing a significant correlation with the tyrosinase mRNA level, and subsequent inhibition of tyrosinase activity. Importantly, the pTyr-EGFP system provided successful tracking of the changes in the live image and real-time monitoring. Thus tyrosinase promoter-based fluorescent assay using a 3D spheroid culture can be useful as a screening system for exploring the efficiency of anti-melanogenesis ingredients.Key words three-dimensional spheroid culture; tyrosinase promoter; fluorescent assay; high-throughput screening (HTS)Created with the purpose of mimicking in vivo environments, three-dimensional (3D) cultures have been shown to differ remarkably in the optimal cell growth, morphology, and differentiation compared with two-dimensional (2D) adherent cultures. Moreover, 3D cultures like spheroid cultures may come closer to the physiological interactions with neighboring cells and the extracellular matrix, providing valuable advanced tools for the evaluation of effectiveness. Particularly, therapeutic screening in 3D spheroid culture offers high potential for discovering drugs and biological relevances. 1)Recently, a biosensor was developed using 3D spheroid cultures and bioelectronically characterized by measuring physiological alterations after drug treatment. [2][3][4] In the cosmetic field, such large-scale screens often utilize the enhanced green fluorescent protein (EGFP) gene as a reporter to allow sensitive, rapid, and convenient quantitation of gene expression. 5)Although using 2D adherent cultures of melanin-producing cells is a useful method for the screening of skin-whitening ingredients, its utility is limited due to the time-consuming, laborious process, which only results in endpoint, static data with low sensitivity which requires multistep cell viability 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay for quantification. 6) We therefore developed a method to automatically monitor the activity of a tyrosinase promoter cloned upstream ...

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Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Development of Tyrosinase Promoter-Based Fluorescent Assay for Screening of Anti-melanogenic Agents

Lee

et al. 2015

Biological & Pharmaceutical Bulletin

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“…Another example of newers is 4-n-butylresorcinol, which has been shown a higher inhibitory capacity on human tyrosinase activity than hydroquinone, arbutin and kojic acid [12]. Another potent tyrosinase inhibitor, decapeptide-12 has been recently shown very effective with a marked improvement of PIH after 8-week therapy.…”

Section: Pigmentary Disordersmentioning

confidence: 99%

Treatment of Hyperpigmentation in Darker Skins

Yaylı¹

2015

Pigmentary Disorders

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“…4-n-Butylresorcinol is now considered the most effective topical depigmenting agent 75 . Unlike vitiligo, the depigmentation caused by chemicals does not usually respond to psoralens with UV rays.…”

Section: Chemical Depigmentationmentioning

confidence: 99%

Disorders of Pigmentation of the Skin - Hypotheses Underlying Interventions by Multiple Systems of Medicine:Is there a Role for Integrated Medicine?

Arianayagam

Ryan

2016

Current Science

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Biomedicine has not provided a complete explanation with fully effective therapies for disorders of pigmentation. Biomedicine emphasizes the role of melanocyte for protection from UV rays and as a determinant of skin colour. These important properties acquired a genetic basis much later than other functions, many relating to cell contact as in the keratinocyte -melanocyte unit, or as with the synapses of the neurological system. There are other roles, biochemical and mechanical, of melanocyte. Management that is inclusive of a maximally holistic approach justifies the use of diverse herbals, yoga and concern for cultural awareness provided by integrated medicine. Vitiligo provides a model which demonstrates that Ayurveda has a richer view of its presentations, possibly a stronger line on its pathogenesis, and a huge range of herbals, many now backed by studies from ethnobotanical laboratories, awaiting research into the many possible mechanisms by which they may act in the wide and complex field of melanocyte biochemistry.

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4‐n‐butylresorcinol, a highly effective tyrosinase inhibitor for the topical treatment of hyperpigmentation

Abstract: Background Hyperpigmentary disorders like melasma, actinic and senile lentigines are a major cosmetic concern.

Cited by 133 publications

References 24 publications

Development of Tyrosinase Promoter-Based Fluorescent Assay for Screening of Anti-melanogenic Agents

Development of Tyrosinase Promoter-Based Fluorescent Assay for Screening of Anti-melanogenic Agents

Treatment of Hyperpigmentation in Darker Skins

Disorders of Pigmentation of the Skin - Hypotheses Underlying Interventions by Multiple Systems of Medicine:Is there a Role for Integrated Medicine?

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