• Proceedings of the Plant Resources Society of Korea Conference
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• 2022.09a
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• pp.118-118
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• 2022

Carex pumila Thunb. is a plant native to East Asia, Australia, and New Zealand. However, its effect on skin melanogenesis has not been investigated. In the present study, we evaluated its anti-melanogenic properties using B16F10 melanoma cells and zebrafish larvae in the presence or absence of α-melanocyte stimulating hormone (α-MSH). In this study we revealed that concentrations below 50 µg/mL did not induce any cytotoxicity in B16F10 melanoma cells and cardiotoxicity in zebrafish larvae. However, 50 µg/mL treatment significantly inhibited α-MSH-induced extracellular (from 181.24% α 0.62% to 105.15% α 0.31%) and intracellular melanin contents (from 119.8% α 1.2% to 53.4% α 1.7%) as well as intracellular tyrosinase activity (from 143.9% α 4.2% to 103.7% α 1.4%) in B16F10 melanoma cells. At 25 µg/mL and 50 µg/mL concentrations, it could significantly inhibit α-MSH induced hyperpigmentation in zebrafish larvae (from 100% α 2.3% to 60.7% α 1.3% and 47.5% α 1.9% respectively). Additionally, the extract suppressed α-MSH-induced cAMP-CREB-MITF signaling pathway and consequently inhibited tyrosinase expression in B16F10 melanoma cells. In conclusion, our results indicate that this plant extract could suppress the cAMP-CREB-MITF axis which consequently inhibits tyrosinase mediated melanogenesis.

• Journal of Applied Biological Chemistry
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• v.65 no.4
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• pp.299-306
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• 2022

In this study, derivatives of trimethoxybenzene were investigated as inhibitors of melanogenesis. We examined the effects of methyl 3,4,5-trimethoxybenzoate (MTB), ethyl 3,4,5-trimethoxybenzoate (ETB), methyl 3,4,5-trimethoxycinnamate (MTC), and ethyl 3,4,5-trimethoxycinnamate (ETC). First, the inhibitory effects of these agents on melanin production were evaluated using α-melanocyte-stimulating hormone (α-MSH)-stimulated B16F10 melanoma cells. We found that all derivatives decreased α-MSH-induced melanin production in B16F10 melanoma cells; ETC showed a strong inhibitory effect at half of the concentration of the other derivatives. As tyrosinase is considered a key enzyme of melanogenesis, we also examined whether the derivatives inhibited tyrosinase activity. MTC and ETC reduced mushroom tyrosinase activity and expression levels of α-MSH-induced B16F10 cellular tyrosinase protein. Inhibitory effects of all derivatives on α-MSH-induced B16F10 cellular tyrosinase activity were shown in a dose-dependent manner. Additionally, the derivatives were exposed to diphenylpicrylhydrazyl free radical to examine their antioxidant characteristics. All derivatives showed considerable antioxidant activity, which was 2-fold higher than that of arbutin. In conclusion, the trimethoxybenzene derivatives, including MTB, ETB, MTC, and ETC exerted anti-melanogenic and antioxidant effects on α-MSH-stimulated melanogenesis, demonstrating their potential for use as novel hypopigmenting agents and antioxidants.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.49 no.4
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• pp.307-312
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• 2023

Water chestnut is fruits of Trapa natans var. bispinosa grown wild in Korea. In this study, water chestnut was investigated for anti-pigmentation. Treatment with ethanolic extracts of water chestnut significantly reduced production of melanin in α-MSH simulated B16F10 cells. At 200 ㎍/mL ethanolic extracts of water chestnut, melanin contents were repressed by 43.26% compared to the control group. Additionally, ethanolic extracts of water chestnut reduced expression and activity of tyrosinase, key enzyme in melanogenesis, in α-MSH simulated B16F10 cells. Ethanolic extracts of water chestnut downregulated tyrosinase activity and expression to 23.65% and 62.35%, respectively. These results suggest that ethanolic extracts of water chestnut might be used as a promising whitening ingredients for inhibition of α-MSH-induced melanin synthesis and pigmentation.

• Journal of Life Science
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• v.31 no.11
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• pp.1019-1027
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• 2021

There are a lot of efforts to develop new compounds having skin whitening effect from natural products. Sparassis crispa is a medicinal mushroom containing more than 40% β-glucan, which exhibits anticancer and immunostimulating effects. The aim of this study was to assess the availability of β-glucan extracted from cauliflower mushroom S. crispa as a skin whitener through the evaluation of inhibitory effects of melanin synthesis and tyrosinase activity and their mechanisms. B16F1 cells were treated with S. crispa β-glucan (10, 100, and 1,000 ㎍/ml, respectively) and α-melanocyte stimulating hormone (α-MSH), simultaneously. Content of melanin synthesis and tyrosinase activity were determined. The expressions levels of tyrosinase, tyrosinase related protein-1 (TRP-1), TRP-2 and microphthalmia-associated transcription factor (MITF) were also measured by western blotting. Treatment with 10, 100 and 1,000 ㎍/ml S. crispa β-glucan and 200 nM α-MSH significantly decreased melanin synthesis by 13.9%, 18.7% and 39.5%, respectively, and tyrosinase activity by 15.6%, 26.9% and 43.2%, respectively, compared to the α-MSH alone group. In addition, S. crispa β-glucan inhibited expressions of tyrosinase, TRP-1, TRP-2 and MITF induced by α-MSH. These results indicated that S. crispa β-glucan inhibited MITF expression, thereby reducing tyrosinase expression and inhibiting melanin production in B16F1 melanoma cells. Therefore, S. crispa β-glucan might be available as a skin whitener.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.48 no.1
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• pp.65-70
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• 2022

In this study, the anti-pigmentation efficacy of Panax vietnamensis (P. vietnamensis), a ginseng native to Vietnam, was confirmed. Melanin synthesis was repressed by ethanolic extracts of P. vietnamensis in B16F10 cells, melanocytes originated from mouse. At 250 ㎍/mL ethanolic extracts of P. vietnamensis, melanin contents were repressed by 64.04% compared to the control group. In addition, ethanolic extracts of P. vietnamensis downregulated tyrosinase activity and expression to 53.34% and 59.39%, respectively. As shown our result, ethanolic extracts of P. vietnamensis blocks α-MSH-mediated melanogenesis and is valuable whitening ingredients in cosmetics.

• Journal of the Korean Applied Science and Technology
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• v.38 no.3
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• pp.883-890
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• 2021

In this study, we investigated the melanogenesis inhibitory effects of Rubus crataefifolius Leaf Extract (RCLE) in B16F10 melanoma cells. We examined the effects of RCLE on the melanin contents and tyrosinase activity, as well as the protein expression levels of the melanogenic enzymes TRP-1, TRP-2, and MITF in α-MSH -stimulated B16F10 melanoma cells. RCLE effectively inhibited tyrosinase activity and melanogenesis, suppressed the phosphorylation of PKA and CREB, and expression of MIT involved in the melanogenesis pathway, and down-regulated expression of melanogenesis related proteins. These result suggest that RCLE inhibited α-MSH-stimulated melanin synthesis by suppressing MITF expression. Therefore, our study suggests that RCLE has potential as a safe treatment for excessive pigmentation or as a natural ingredient in cosmetics.

• Journal of Applied Biological Chemistry
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• v.66
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• pp.204-212
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• 2023

Whitening is inhibitory activity of the melanin synthesis of melanocytes. Recently, whitening materials have been developed on natural materials because of its side effects on skin. Figs (Ficus Carica L.) is a fruit belonging to the Moraceae family and whitening activity was reported in focusing on the fig's stem and leaf components, but whitening activity of the figs fruit was not known. Thus, in this study, we tried to observe its anti-melanogenesis as well as antioxidant and anti-inflammation. The radical scavenging activity of figs fruits extract (FFE) was observed as the level of 34.52±1.98%/60.71±1.26% compared to the control in the its maximum concentration in the DPPH/ABTS assay. Cytotoxicity of FFE was observed at 10% concentration by CCK8 assay, so the maximum concentration was set at 5% and applied to all experiments. FFE concentration dependently decreased NO production associated with inducible nitric oxide synthase, cyclooxygenase-2, interleukin-6 and tumor necrosis factor-α gene expression, these strongly suggesting anti-inflammatory activity. In melanin contents assay, FFE significantly down-regulated melanin production in α-MSH-stimulated B16F10 cell as well as tyrosinase inhibition in vitro. In addition, FFE decreased the Microphthalmia-associated transcription factor (MITF) mRNA expression about 94.34% compared to the α-MSH treatment group in RT-PCR. Finally, FFE significantly reduced the MITF, cAMP response element-binding protein and tyrosinase protein expression in the α-MSH stimulated B16F10 cell. Through these results, we found that FFE can not only directly inhibit tyrosinase enzyme activity but also suppress melanogenesis through regulation of MITF gene expression in α-MSH signal transduction.

• Journal of Life Science
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• v.20 no.11
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• pp.1617-1624
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• 2010

Recently, it has been found that Asiasari radix showed a hypopigmenting effect on melanogenesis through activation of mitogen-activated protein kinase (MEK)/extracellular signal-activated kinase (ERK) in B16F10 melanoma cells. However, the hypopigmenting effect of A. radix on the $\alpha$-melanocyte stimulating hormone ($\alpha$-MSH)-stimulated melanogenesis has remained unknown. The purpose of this study was to investigate the inhibitory mechanism of the partially purified A. radix (PPAR)-induced hypopigmentating effects on $\alpha$-MSH-stimulated melanogenesis in B16F10 mouse melanoma cells. PPAR strongly inhibited tyrosinase activity and leads to decreased melanin synthesis in $\alpha$-MSH-stimulated B16F10 melanoma cells. PPAR also decreased the $\alpha$-MSH-induced over-expression of the melanogenic enzymes, tyrosinase, tyrosinase-related protein (TRP)-1, dopachrome tautomerase (Dct) and microphthalmia-associated transcription factor (MITF). We further showed that PPAR inhibits $\alpha$-MSH-induced melanogenesis via phosphorylation of MEK/ERK and PI3K/Akt, and that their activation was blocked by MEK inhibitors, PD98059 and PI3K inhibitors, LY294002 in $\alpha$-MSH-stimulated B16F10 melanoma cells. These results suggest that PPAR inhibits $\alpha$-MSH-induced melanogenesis by activation of MEK/ERK and PI3K/Akt through MITF degradation, which may lead to down-regulation of tyrosinase.

• Journal of Applied Biological Chemistry
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• v.65 no.2
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• pp.93-99
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• 2022

Lysosome organelle extract (LOE) was derived from egg whites. The lysosome is an intracellular organelle that contains several hydrolysis enzymes. Previous studies have reported that LOE performs important functions, such as melanin de-colorization and anti-melanin production in B16F10 melanoma cells. However, its principal molecular and cellular mechanisms have not been elucidated till date. In non-cytotoxic conditions, LOE significantly inhibited α-MSH induced melanin synthesis of murine B16F10 cells. The anti-melanogenic activity of LOE was mediated by suppressing the mRNA expression of tyrosinase enzyme, tyrosinase related protein-1/2 (TRP-1/2), and microphthalmia-associated transcription factor (MITF) genes. By performing western blot analysis, we found that LOE significantly attenuated melanogenesis. In this case, LOE helped in increasing extracellular receptor kinase (ERK) phosphorylation in α-MSH induced B16F10 cells. Furthermore, MITF is found to be a key regulatory transcription factor in melanin synthesis; it was down-regulated by LOE through ERK phosphorylation. In this experiment, PD98059 (MEK inhibitor) was used to check whether LOE directly regulated the activity of ERK. Although LOE exerted inhibitory effect on melanin synthesis, we could not observe this effect in PD98059-treated α-MSH induced B16F10. These results strongly indicate that LOE is related to ERK activation and MITF degradation in anti-skin pigmentation. Hence, LOE should be utilized as a whitening agent of skin in the near future.

• Journal of Physiology & Pathology in Korean Medicine
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• v.30 no.1
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• pp.47-53
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• 2016

Kaempferia galanga L. is one of the plants in Zingiberaceae family. It is used by people in many regions of Asia and Africa for relieving toothache, abdominal pain, muscular swelling and rheumatism. Tyrosinase is a key enzyme for melanogenesis, and hyperpigmentation is associated with abnomal accumulation of melanin pigment. This study aimed to investigate the inhibition of melanogenesis by hexane extract of Kaempferia galanga L. (HKG) in B16F10 melanoma cells. Cell-free tyrosinase, melanin contents, intracellular tyrosinase activity and western blot analysis were performed to elucidate the effects on anti-melanogenesis. Cytotoxicity of the extracts was measured using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay and determined the concentration of 12.5, 25 μg/ml. HKG significantly inhibited to activities of intracellular tyrosinase and melanin synthesis in the absence or presence of α-melanocyte stimulating hormone (α-MSH) with dose-dependent manner. And HKG inhibited the expression of tyrosinase, tyrosinase-related protein 1 (TRP-1) and tyrosinase-related protein 2 (TRP-2), regardless of the presence or absence of α-MSH. HKG also down-regulated phosphorylation of p38 and JNK, and up-regulated phosphorylation of Akt. These effects were not related to its cytotoxicity action. These results indicate that HKG has the potential to be a useful therapeutic agent for treating hyperpigmentation disorders and as a beneficial additive in whitening agents in cosmetics industry.