Discovery of Highly Potent Tyrosinase Inhibitor, T1, with Significant Anti-Melanogenesis Ability by zebrafish in vivo Assay and Computational Molecular Modeling

Chen, Wang Chuan; Tseng, Tien‐Sheng; Hsiao, Nai-Wan; Lin, Yun; Wen, Zhi Hong; Tsai, Chin Chuan; Lee, Yu Ching; Lin, Hui Hsiung; Tsai, Keng‐Chang

doi:10.1038/srep07995

Cited by 135 publications

(112 citation statements)

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“…Skin irritancy testing is usually performed on human keratinocytes [186]; human repeat insult patch testing (HRIPT, repeated applications of products on the skin, under an occlusive patch, in healthy adult volunteers) has also been developed to assess the dermal irritation or sensitization potency of a molecule. In vivo toxicity assays can be performed in zebrafish or mice [187].…”

Section: Further Development Of a Cosmetic Ingredientmentioning

confidence: 99%

Skin Whitening Cosmetics: Feedback and Challenges in the Development of Natural Skin Lighteners

et al. 2016

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Abstract:With the public's growing interest in skin whitening, lightening ingredients only used under dermatological supervision until recently, are more and more frequently incorporated into cosmetic formulas. The active agents that lighten skin tone are either natural or synthetic substances, and may act at various levels of melanogenesis. They are used to treat various skin pigmentation disorders or simply to obtain a lighter skin tone as whiter skin may be synonymous of wealth, health, youth, and/or beauty in different cultures. However, recent studies demonstrated the adverse effects of some of these ingredients, leading to their interdiction or restricted use under the European Directive and several other international regulations. After an overview of skin whitening practices and the associated risks, this article provides insight into the mechanisms involved in melanin synthesis and the biological assays available to attest the lightening activity of individual ingredients. The legislation dealing with the use of skin lighteners is then discussed. As traditional depigmenting agents such as hydroquinone and corticosteroids are of safety concern, the potential of natural extracts has been investigated more and more; finally, a synthesis of three years of research in our laboratory for such plant extracts will be given.

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Section: Further Development Of a Cosmetic Ingredientmentioning

confidence: 99%

Skin Whitening Cosmetics: Feedback and Challenges in the Development of Natural Skin Lighteners

et al. 2016

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“…9 All dienols ( 4a–4e ) possessed IC 50 values at µM levels (Table 2). Additionally, aliphatic linked dienols ( 4a–4d ) had IC 50 values statistically lower than KA itself.…”

Section: Resultsmentioning

confidence: 99%

“…9 Mushroom tyrosinase inhibition was determined by adding dienols in sample media (25 µL) to 96-well plates containing phosphate buffer (80 µL, pH = 6.8) and 125 µL substrate (0.5 mM L-DOPA) and incubated for 5 min at room temperature. 9 Mushroom tyrosinase (20 µL, 1250 U/mL, Sigma, Milwaukee, WI) in phosphate buffer (pH = 6.8) was added and incubated an additional 5 min at room temperature. The amount of dopachrome produced was measured using a microplate reader (Coulter, Boulevard Brea, CA) at 475 nm.…”

Section: Methodsmentioning

confidence: 99%

Biodegradable Kojic Acid-Based Polymers: Controlled Delivery of Bioactives for Melanogenesis Inhibition

et al. 2017

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Kojic acid (KA) is a naturally occurring fungal metabolite that is utilized as a skin-lightener and antibrowning agent owing to its potent tyrosinase inhibition activity. While efficacious, KA’s inclination to undergo pH-mediated, thermal-, and photodegradation reduces its efficacy, necessitating stabilizing vehicles. To minimize degradation, poly(carbonate-esters) and polyesters comprised of KA and natural diacids were prepared via solution polymerization methods. In vitro hydrolytic degradation analyses revealed KA release was drastically influenced by polymer backbone composition (e.g., poly(carbonate-ester) vs polyester), linker molecule (aliphatic vs heteroatom-containing), and release conditions (physiological vs skin). Tyrosinase inhibition assays demonstrated that aliphatic KA dienols, the major degradation product under skin conditions, were more potent then KA itself. All dienols were found to be less toxic than KA at all tested concentrations. Additionally, the most lipophilic dienols were statistically more effective than KA at inhibiting melanin biosynthesis in cells. These KA-based polymer systems deliver KA analogues with improved efficacy and cytocompatible profiles, making them ideal candidates for sustained topical treatments in both medical and personal care products.

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“…Chen et al [2] also screened 78 medicinal herbal plants and found out that the rhizome of GEB has a potential to inhibit tyrosinase activity. Although GEB has been used as an oriental medicinal remedy to treat neurodegenerative disorders, there is high possibility to use GEB as a tyrosinase inhibitor from these screening studies.…”

Section: Discussionmentioning

confidence: 99%

Inhibitory effect of Gastrodia elata Blume extract on alpha-melanocyte stimulating hormone-induced melanogenesis in murine B16F10 melanoma

Shim

Song

Choi³

et al. 2017

Nutr Res Pract

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BACKGROUND/OBJECTIVESGastrodia elata Blume (GEB), a traditional herbal medicine, has been used to treat a wide range of neurological disorders (e.g., paralysis and stroke) and skin problems (e.g., atopic dermatitis and eczema) in oriental medicine. This study was designed to investigate whether GEB extract inhibits melanogenesis activity in murine B16F10 melanoma.MATERIALS/METHODMurine B16F10 cells were treated with 0-5 mg/mL of GEB extract or 400 µg/mL arbutin (a positive control) for 72 h after treatment with/without 200 nM alpha-melanocyte stimulating hormone (α-MSH) for 24 h. Melanin concentration, tyrosinase activity, mRNA levels, and protein expression of microphthalmia-associated transcription factor (MITF), tyrosinase, tyrosinase-related protein (Trp)1, and Trp2 were analyzed in α-MSH-untreated and α-MSH-treated B16F10 cells.RESULTSTreatment with 200 nM α-MSH induced almost 2-fold melanin synthesis and tyrosinase activity along with increased mRNA levels and protein expression of MITF, tyrosinase, Trp1 and Trp2. Irrespective of α-MSH stimulation, GEB extract at doses of 0.5-5 mg/mL inhibited all these markers for skin whitening in a dose-dependent manner. While lower doses (0.5-1 mg/mL) of GEB extract generally had a tendency to decrease melanogenesis, tyrosinase activity, and mRNA levels and protein expression of MITF, tyrosinase, Trp1, and Trp2, higher doses (2-5 mg/mL) significantly inhibited all these markers in α-MSH-treated B16F10 cells in a dose-dependent manner. These inhibitory effects of the GEB extract at higher concentrations were similar to those of 400 µg/mL arbutin, a well-known depigmenting agent.CONCLUSIONSThese results suggest that GEB displays dose-dependent inhibition of melanin synthesis through the suppression of tyrosinase activity as well as molecular levels of MITF, tyrosinase, Trp1, and Trp2 in murine B16F10 melanoma. Therefore, GEB may be an effective and natural skin-whitening agent for application in the cosmetic industry.

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Discovery of Highly Potent Tyrosinase Inhibitor, T1, with Significant Anti-Melanogenesis Ability by zebrafish in vivo Assay and Computational Molecular Modeling

Cited by 135 publications

References 70 publications

Skin Whitening Cosmetics: Feedback and Challenges in the Development of Natural Skin Lighteners

Skin Whitening Cosmetics: Feedback and Challenges in the Development of Natural Skin Lighteners

Biodegradable Kojic Acid-Based Polymers: Controlled Delivery of Bioactives for Melanogenesis Inhibition

Inhibitory effect of Gastrodia elata Blume extract on alpha-melanocyte stimulating hormone-induced melanogenesis in murine B16F10 melanoma

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