• Journal of the Society of Cosmetic Scientists of Korea
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• v.33 no.2
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• pp.69-77
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• 2007

We examined the depigmentation effect on Korean traditional citrus 17 species. With B16 melanoma cells, we have seen inhibition of the tyrosinase and melanin formation, which eventually were dose dependently decreased by three citrus fruits, immature Citrus unshiu, Citrus hassaku, and Citrus sinensis ${\times}$ reticulata as compared with positive control. Also, we examined expression of tyrosinase, DOPAchrome tautomerase (TRP-2), and DHICA oxidase (TRP-1) which affect melanin synthesis. Especially, immature Citrus unshiu decreased the protein levels of tyrosinase and TRP-1. In conclusion, immature Citrus unshue showed the strongest activity in all the experiments mentioned above and we expect that it can be used for preventing UV-induced pigmentation.

• Korean Journal of Food Science and Technology
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• v.53 no.2
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• pp.160-164
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• 2021

This study investigated various physiological activities to examine the applicability of the functional materials of Allium tuberosum root extract. The A. tuberosum root extract showed a low cytotoxicity against murine melanoma B16F10 cells. It also showed high DPPH radical scavenging activity (ID50, 6.2 ㎍/mL), inhibited tyrosinase activity (ID50, 115.4 ㎍/mL), and decreased melanin content (ID50, 31.5 ㎍/mL). Treatment of B16F10 cells with A. tuberosum root extract suppressed the protein expression of tyrosinase in a dose-dependent manner. These findings suggest that A. tuberosum root extract inhibits melanin synthesis by suppressing intracellular tyrosinase expression. Additionally, A. tuberosum root extract inhibited elastase with an ID50 value of 145.1 ㎍/mL and contained isoquercitrin. These results indicate that A. tuberosum root extract is an appropriate natural material.

• Proceedings of the Plant Resources Society of Korea Conference
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• 2023.04a
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• pp.56-56
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• 2023

The cone of Pinus rigida × Pinus taeda (PRT), a plant in the Pinaceae family, has long been used in traditional medicine to treat hemostasis, bruises, and burns. Previous research has shown that regulating oxidation-reduction reactions in reactive oxygen species can help inhibit melanogenesis, the process of melanin synthesis, which is a common target for addressing hyperpigmentation. Inhibiting tyrosinase is also known to be effective in this regard. Based on these findings, we conducted an investigation into the inhibitory effect of the ethyl acetate fraction of PRT (ERT) on melanogenesis in B16 F10 cells. We know that the expression levels of melanin biosynthesis-related proteins, including tyrosinase, TRP-1, and TRP-2, are regulated by MITF (microphthalmia-associated transcription factor) and cAMP, with cAMP affecting the activity of protein kinase A (PKA). PKA can reduce melanogenesis, and CREB reduces the phosphorylation of melanin-producing enzymes. In addition, the MAPK signaling pathway, composed of ERK, JNK, p38, and other factors, is also known to play a role in the inhibition of melanogenesis in melanocytes. Our immunoblotting results showed that ERT inhibited the expression of melanin production-related proteins (tyrosinase, TRP-1, TRP-2, and MITF) that were significantly increased by a-MSH treatment to promote melanin production. Furthermore, the phosphorylation levels of factors related to cAMP/PKA/CREB and MAPK signaling pathways were significantly reduced without affecting the total form. In conclusion, we believe that treatment with ERT can inhibit melanin synthesis by modulating the phosphorylation of cAMP/PKA/CREB and MAPK signaling pathways at the cellular level. These findings suggest the potential of ERT as a raw material for functional cosmetics and pharmaceuticals, thanks to its antioxidant activity and ability to inhibit melanogenesis. We thought that these findings of ERT as a natural plant resource will inspire further research and development in this area.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.39 no.4
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• pp.289-294
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• 2013

To develop a new whitening agent for cosmetics, we investigated the inhibitory effects of biochanin A on melanogenesis. The biochanoin A is an active component in the extracts of Dalbergia odorifera T. Chen. It reduced melanin contents of B16F1 melanoma cells in a dose-dependent manner and decreased to about 48% at a concentration 10 ${\mu}g/mL$. It also inhibited the expression in microphthalmia associated transcription factor (MITF), Tyrosinase, Tyrosinase related protein 1 (Trp-1), and Tyrosinase related protein 2 (Trp-2) in melanocytes. The results suggested that biochanin A has considerable potential as a cosmetics ingredient with a whitening effect.

• Journal of Marine Bioscience and Biotechnology
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• v.14 no.1
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• pp.25-32
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• 2022

The desire to be light skinned is universal among women. Asia has a long history of using skincare formulations as whitening agents. There is an imperative need to develop novel cosmetics from herbal sources due to several unpleasant side effects and high costs. As a result, this study aims to investigate the effect of Ceylon black tea extracts on melanogenesis. Five different Ceylon black tea extracts were prepared and examined for total phenolic content (TPC), total flavonoid content (TFC), DPPH radical scavenging activity, and tyrosinase inhibitory activity. Furthermore, B16F10 melanoma cells were treated with these extracts and tested for cytotoxicity and protein suppression levels. According to the results of this study, the highest TPCs were obtained from ethanol and acetone extractions (240.303 ± 1.389 ㎍/g and 240.202 ± 4.700 ㎍/g, respectively), whereas the highest TFC was obtained from acetone extraction (57.484 ± 0.413 ㎍/g). Ceylon black tea extracted with ethanol exhibited the highest inhibitory activity on tyrosinase with an IC₅₀ value of 0.277 ± 0.017 mg/mL and the highest DPPH radical scavenging activity with an EC₅₀ value of 0.009 ± 0.000 mg/mL. Furthermore, western blot results revealed that tyrosinase, TRP-1, TRP-2, and MITF protein expression levels were dose-dependently suppressed, indicating the applicability of Ceylon black tea extract as a novel melanogenesis inhibitor.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.31 no.4 s.54
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• pp.305-310
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• 2005

To obtain effective and safe depigmenting agents, we investigated the effects of Scirpi rhizoma, a medicine among Chinese herbs, on melanogenesis. Dried S. rhizoma was refluxed with 70% aqueous ethanol and the extract was evaporated to dryness. To determine the effects as a whitening agent, various in vitro tests were performed such as free radical scavenging activity, melanin formation assay, tyrosinase activity and expression of tyrosinase, TRP-1 and TRP-2(western blot and RT-PCR) in B16 melanoma cells. S. rhizoma showed scavenging activities of free radicals and reactive oxygen species (ROS) with the $IC_{50}\;of\;638{\mu}g/mL$ against 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical and $21.7{\mu}g/mL$ against superoxide radicals in the xanthine/xanthine oxidase system, respectively. S. rhizoma significantly inhibited melanin production in B16 melanoma cells. S. rhizoma treatment(48 h) suppressed the biosynthesis of melanin up to 27% at 100{\mu}g/mL$ and reduced tyrosinase activity up to 31% at $100{\mu}g/mL$ in B16 melanoma cells. S. rhizoma was also able to significantly inhibit tyrosinase and TRP-1 expression in protein and mRNA level. These results suggest that S. rhizoma inhibited melanin biosynthesis by regulating tyrosinase activity and expression in B16 melanoma cells. Therefore, S. rhizoma may be useful as a new antioxidant and whitening agent to inhibit melanogenesis.

• Journal of Life Science
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• v.21 no.2
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• pp.279-285
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• 2011

The objective of the present study was to evaluate the skin whitening effect of the extracts of 3 herbs, Ligularia fischeri, Solidago virga-aurea and Aruncus dioicus, which were collected from Ullung island. Tyrosinase inhibition activities were 33% in pre-fermented extracts and 45% in post-fermented ones. When tyrosinase activities in B16F10 murine melanoma cells were tested, activities in pre- and post-fermented extracts were 41 and 56.5%, respectively. Thus, the post-fermented extracts might have greater skin whitening effects. The protein expression of MITF, TRP-1, TRP-2, and tyrosinase, which are all skin-whitening related transcription factors, showed that both pre- and post-fermented herbs inhibited protein biosynthesis in B16F10 melanoma cells. Post-fermented herb extracts especially showed a greater decrease of protein expressions. The expression of MITF, a regulatory transcription factor, was also decreased by both extracts but was greater in the post-fermented ones. From the results, it can be concluded that the 3 herb extracts from Ullung island may inhibit melanin biosynthesis by the suppression of MITF activity in a signaling pathway. Results indicate that the post-fermented herbs tested in the present study had skin whitening activities and can be used as functional ingredients for food and cosmetic compositions.

• Proceedings of the Korean Society of Applied Pharmacology
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• 2007.11a
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• pp.79-92
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• 2007

Oxidative stress have known to be a risk factor for the degenerative processes and closely related to a lot of diseases. It is well established that antioxidants are good in protection and therapeutic means against oxidative damage. There is increasing interest in natural antioxidants and many natural antioxidants have been found and utilized as the possible protection for various diseases and skin aging. We have screened natural antioxidant agents for cosmeceuticals, nutraceuticals, and drugs as therapeutic and preventive means against oxidative stress, and have developed a number of novel antioxidants from various natural sources. A novel melanin synthesis inhibitor, Melanocin A, isolated from the metabolite of a fungal strain Eupenicillium shearii F80695 inhibited mushroom tyrosinase and melanin biosynthesis of B16 melanoma cells with $IC_{50}$ value of 9.0 nM and MIC value of $0.9\;{\mu}M$, respectively. Melanocin A also exhibited potent antioxidant activity by scavenging of DPPH and superoxide anion radicals. UV was found to increase the level of hydrogen peroxides and other reactive oxygen species (ROS) in skin tissues. This increase in ROS may not only alter the structure and function of many genes and proteins directly but may also modulate their expressions through signal transduction pathways and, ultimately, lead to skin damage. We investigated the effect of Melanocin A on UV-induced premature skin aging. Firstly, the effect of Melanocin A on UV-induced matrix metalloproteinase (MMP)-9 expression in an immortalized human keratinocyte cell line, HaCaT in vitro was investigated. Acute UV irradiation induced MMP-9 expression at both the mRNA and protein levels and Melanocin A suppressed this expression in a dose-dependent manner. We then investigated UV-induced skin changes in hairless mice in vivo by Melanocin A. Chronic exposure of hairless mouse dorsal skin to UV increased skin thickness and induced wrinkle formation and the gelatinase activities of MMP-2 and MMP-9. Moreover, Melanocin A significantly suppressed UV-induced morphologic skin changes and MMP-2 and MMP-9 expression. These results show that Melanocin A can prevent the harmful effects of UV that lead to skin aging. Therefore, we suggest that Melanocin A should be viewed as a potential therapeutic agent for preventing and/or treating premature skin aging. Terrein is a bioactive fungal metabolite isolated from Penicillium species. Terrein has a relatively simple structure and can be easily synthesized. However, the biologic effects of terrein are comparatively unknown. We found for the first time that terrein potently inhibit melanin production in melanocytes and has a strong hypopigmentary effect in a spontaneously immortalized mouse melanocyte cell line, Mel-Ab. Treatment of Mel-Ab cells with terrein (10-100 mM) for 4 days significantly reduced melanin levels in a dose-dependent manner. In addition, terrein at the same concentration also reduced tyrosinase activity. We then investigated whether terrein influences the extracellular signal-regulated protein kinase (ERK) pathway and the expression of microphthalmia-associated transcription factor (MITF), which is required for tyrosinase expression. Terrein was found to induce sustained ERK activation and MITF down-regulation, and luciferase assays showed that terrein inhibits MITF promoter activity in a dose-dependent manner. To elucidate the correlation between ERK pathway activation and a decreased MITF transcriptional level, PD98059, a specific inhibitor of the ERK pathway, was applied before terrain treatment and found to abrogate the terrein-induced MITF attenuation. Terrein also reduced the tyrosinase protein level for at least 72 h. These results suggest that terrain reduces melanin synthesis by reducing tyrosinase production via ERK activation, and that this is followed by MITF down-regulation.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.34 no.2
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• pp.149-156
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• 2008

To develop a new natural whitening agent for cosmetics, we investigated effects of Acanthopanax sessiliflorum Seeman on melanogenesis. We prepared phenolic acid-rich extract including two phenolic acids, chlorogenic acid and caffeic acid, as predominant constituents from Acanthopanax sessiliflorum Seeman. Phenolic acid-rich extract showed ROS scavenging activities in 1,1-diphenyl-2-picrylhydrazyl(DPPH) radical and xanthine/xanthine oxidase system with the $IC_{50}$ values of $3.43{\pm}0.35{\mu}g/mL$ and $158.91{\pm}1.57{\mu}g/mL$, respectively. Phenolic acid-rich fraction reduced melanin contents of B16 melanoma cells dose-dependantly and the decrease was $27.27{\pm}2.66%$ at a concentration of $100{\mu}g/mL$. And the phenolic acid-rich fraction reduced intracellular tyrosinase activity about $53.67{\pm}8.55%$ at a concentration of $100{\mu}g/mL$. Phenolic acid-rich extract inhibited tyrosinase and TRP-2 expression at protein level. These results suggest that phenolic acid-rich fraction reduced melanin formation by the inhibitions of tyrosinase activity and expression in B16 melanoma cells. Therefore, we suggest that phenolic acid-rich extract could be used as a whitening ingredient in cosmetics.

• Nutrition Research and Practice
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• v.12 no.1
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• pp.3-12
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• 2018

BACKGROUND/OBJECTIVES: Sageretia thea is traditionally used as a medicinal herb to treat various diseases, including skin disorders, in China and Korea. This study evaluated the inhibitory effect of Sageretia thea fruit on melanogenesis and its underlying mechanisms in B16F10 mouse melanoma cells. The active chemical compounds in anti-melanogenesis were determined in Sageretia thea. MATERIALS/METHODS: Solvent fractions from the crude extract were investigated for anti-melanogenic activities. These activities and the mechanism of anti-melanogenesis in B16F10 cells were examined by determining melanin content and tyrosinase activity, and by performing western blotting. RESULTS: The n-hexane fraction of Sageretia thea fruit (HFSF) exhibited significant anti-melanogenic activity among the various solvent fractions without reducing viability of B16F10 cells. The HFSF suppressed the expression of tyrosinase and tyrosinase-related protein 1 (TRP1). The reduction of microphthalmia-associated transcription factor (MITF) expression by the HFSF was mediated by the Akt/glycogen synthase kinase 3 beta ($GSK3{\beta}$) signaling pathway, which promotes the reduction of ${\beta}-catenin$. Treatment with the $GSK3{\beta}$ inhibitor 6-bromoindirubin-3'-oxime (BIO) restored HFSF-induced inhibition of MITF expression. The HFSF bioactive constituents responsible for anti-melanogenic activity were identified by bioassay-guided fractionation and gas chromatography-mass spectrometry analysis as methyl linoleate and methyl linolenate. CONCLUSIONS: These results indicate that HFSF and its constituents, methyl linoleate and methyl linolenate, could be used as whitening agents in cosmetics and have potential for treating hyperpigmentation disorders in the clinic.