Methyl-2-acetylamino-3-(4-hydroxyl-3,5-dimethoxybenzoylthio)propanoate suppresses melanogenesis through ERK signaling pathway mediated MITF proteasomal degradation

Ha, Ji Hoon; Jeong, Yoon; Xuan, Song Hua; Lee, Jae-Young; Park, Jino; Park, Soo Nam

doi:10.1016/j.jdermsci.2018.04.011

Cited by 15 publications

(13 citation statements)

References 59 publications

(73 reference statements)

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“…As to the human sources, data on inhibition of human recombinant or purified tyrosinase [9,207], human melanoma cells [130,136], normal human melanocytes [208][209][210][211], or human skin models consisting of reconstructed three-dimensional human epidermis [212][213][214][215] have been published (Figure 21). The results of clinical trials have also been reported for well recognized skin depigmenting agents [216,217] such as thiamidol, that, as stated also above, is one of the most striking examples of a pigmentation inhibitor exhibiting significant higher activity on human than on mushroom tyrosinase [9,218]. This nicely exemplifies the differential effects of tyrosinase inhibitors on the human and mushroom enzymes, likely due to the presence of additional amino acids in the hydrophobic substrate-binding pocket of mushroom tyrosinase [218].…”

Section: Human and Animal Tyrosinase Phenolic Inhibitorsmentioning

confidence: 53%

“…( Figure 21). The results of clinical trials have also been reported for well recognized skin depigmenting agents [216,217] such as thiamidol, that, as stated also above, is one of the most striking examples of a pigmentation inhibitor exhibiting significant higher activity on human than on mushroom tyrosinase [9,218]. This nicely exemplifies the differential effects of tyrosinase inhibitors on the human and mushroom enzymes, likely due to the presence of additional amino acids in the hydrophobic substrate-binding pocket of mushroom tyrosinase [218].…”

Section: Human and Animal Tyrosinase Phenolic Inhibitorsmentioning

confidence: 53%

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Natural and Bioinspired Phenolic Compounds as Tyrosinase Inhibitors for the Treatment of Skin Hyperpigmentation: Recent Advances

2019

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One of the most common approaches for control of skin pigmentation involves the inhibition of tyrosinase, a copper-containing enzyme which catalyzes the key steps of melanogenesis. This review focuses on the tyrosinase inhibition properties of a series of natural and synthetic, bioinspired phenolic compounds that have appeared in the literature in the last five years. Both mushroom and human tyrosinase inhibitors have been considered. Among the first class, flavonoids, in particular chalcones, occupy a prominent role as natural inhibitors, followed by hydroxystilbenes (mainly resveratrol derivatives). A series of more complex phenolic compounds from a variety of sources, first of all belonging to the Moraceae family, have also been described as potent tyrosinase inhibitors. As to the synthetic compounds, hydroxycinnamic acids and chalcones again appear as the most exploited scaffolds. Several inhibition mechanisms have been reported for the described inhibitors, pointing to copper chelating and/or hydrophobic moieties as key structural requirements to achieve good inhibition properties. Emerging trends in the search for novel skin depigmenting agents, including the development of assays that could distinguish between inhibitors and potentially toxic substrates of the enzyme as well as of formulations aimed at improving the bioavailability and hence the effectiveness of well-known inhibitors, have also been addressed.

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Section: Human and Animal Tyrosinase Phenolic Inhibitorsmentioning

confidence: 53%

Section: Human and Animal Tyrosinase Phenolic Inhibitorsmentioning

confidence: 53%

Natural and Bioinspired Phenolic Compounds as Tyrosinase Inhibitors for the Treatment of Skin Hyperpigmentation: Recent Advances

2019

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“…Melanin content was determined using a previously described method . B16F1 melanoma cells were cultured in 6‐well plates (1 × 10 5 cells/well).…”

Section: Methodsmentioning

confidence: 99%

Antimelanogenic and Antimigration Properties of the Ethyl Acetate Fraction of Calendula officinalis Flowers on Melanoma Cells

Xuan

Park

2019

Photochem & Photobiology

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Calendula officinalis L., commonly known as marigold, is not only cultivated for ornamental purposes but is also used as a traditional medicinal herb. Its flowers have been used to treat various skin diseases, including rashes, burns, cuts and bruises, since ancient times. However, to our knowledge, the impact of C. officinalis L. on melanoma and its mechanism have not been clarified. The aim of this work was to investigate the chemical characterization and antimelanogenic and antimigration activities of the ethyl acetate fraction of C. officinalis flowers (EFC), as well as elucidate the potential mechanism. The obtained results showed that EFC markedly decreased α‐MSH‐induced melanin production and the cell migration ability of melanoma cells in a dose‐dependent manner. Additionally, EFC significantly inhibited the activity and expression of matrix metalloproteinase 2 (MMP‐2) via suppressing the mitogen‐activated protein kinase (MAPK) signaling pathway. Taken together, the present study demonstrated that C. officinalis flowers can be used as a natural source of antimelanogenisis and antimigration regent to treatment or prevent skin diseases.

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“…White spotting is caused by a frameshift mutation of KIT in the Arabian camel (Holl et al, 2017). Furthermore, melanogenesis is additionally regulated by a number of key genes, which control melanocytes to further generate melanin, such as the key melanogenic enzyme genes TYR and DCT (Hearing, 2011;Yasumoto et al, 1997), and critical melanosomal protein PMEL (Chen et al, 2018;Ji et al, 2018). In addition, KIT has a critical influence on melanin deposition.…”

Section: Introductionmentioning

confidence: 99%

KIT is involved in melanocyte proliferation, apoptosis and melanogenesis in the Rex Rabbit

Chen

Zhao

et al. 2020

PeerJ

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Background Melanocytes play an extremely important role in the process of skin and coat colors in mammals which is regulated by melanin-related genes. Previous studies have demonstrated that KIT is implicated in the process of determining the color of the coat in Rex rabbits. However, the effect of KIT on the proliferation and apoptosis of melanocytes and melanogenesis has not been clarified. Methods The mRNA and protein expression levels of KIT were quantified in different coat colored rabbits by qRT-PCR and a Wes assay. To identify whether KIT functions by regulating of melanogenesis, KIT overexpression and knockdown was conducted in melanocytes, and KIT mRNA expression and melanin-related genes TYR, MITF, PMEL and DCT were quantified by qRT-PCR. To further confirm whether KIT influences melanogenesis in melanocytes, melanin content was quantified using NaOH lysis after overexpression and knockdown of KIT. Melanocyte proliferation was estimated using a CCK-8 assay at 0, 24, 48 and 72 h after transfection, and the rate of apoptosis of melanocytes was measured by fluorescence-activated cell sorting. Results KITmRNA and protein expression levels were significantly different in the skin of Rex rabbits with different color coats (P < 0.05), the greatest levels observed in those with black skin. The mRNA expression levels of KIT significantly affected the mRNA expression of the pigmentation-related genes TYR, MITF, PMEL and DCT (P < 0.01). Melanin content was evidently regulated by the change in expression patterns of KIT (P < 0.01). In addition, KIT clearly promoted melanocyte proliferation, but inhibited apoptosis. Conclusions Our results reveal that KIT is a critical gene in the regulation of melanogenesis, controlling proliferation and apoptosis in melanocytes, providing additional evidence for the mechanism of pigmentation of animal fur.

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Methyl-2-acetylamino-3-(4-hydroxyl-3,5-dimethoxybenzoylthio)propanoate suppresses melanogenesis through ERK signaling pathway mediated MITF proteasomal degradation

Abstract: These results clearly demonstrate that MAHDP suppresses the expression of melanogenic enzymes through ERK phosphorylation-mediated MITF proteasomal degradation, and suggest that MAHDP may be efficient as a therapeutic agent for hyperpigmentation.

Cited by 15 publications

References 59 publications

Natural and Bioinspired Phenolic Compounds as Tyrosinase Inhibitors for the Treatment of Skin Hyperpigmentation: Recent Advances

Natural and Bioinspired Phenolic Compounds as Tyrosinase Inhibitors for the Treatment of Skin Hyperpigmentation: Recent Advances

Antimelanogenic and Antimigration Properties of the Ethyl Acetate Fraction of Calendula officinalis Flowers on Melanoma Cells

KIT is involved in melanocyte proliferation, apoptosis and melanogenesis in the Rex Rabbit

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