• Korean Journal of Food Science and Technology
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• v.48 no.1
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• pp.72-76
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• 2016

We investigated the application of functional materials by examining a variety of physiological activities of Geranium krameri extract obtained from the National Institute of Horticultural and Herbal Science. Geranium krameri extract had a low cytotoxicity against murine melanoma B16F10 cells. At concentrations with little or no cytotoxicity, Geranium krameri extract showed high DPPH radical scavenging activity ($IC_{50}$, $8.72{\mu}g/mL$) and anti-microbial activities against Bacillus subtilis, Escherichia coli, and Candida albicans. Additionally, Geranium krameri extract inhibited tyrosinase activity ($IC_{50}$, $456.86{\mu}g/mL$) and decreased melanin content ($IC_{50}$, $50.35{\mu}g/mL$). The treatment of B16F10 cells with Geranium krameri extract suppressed the protein expression of tyrosinase in a dose-dependent manner. These findings suggest that Geranium krameri extract inhibits melanin synthesis in murine melanoma B16F10 cells by suppressing intracellular tyrosinase expression, as well as directly inhibits tyrosinase activity simultaneously.

• Journal of Life Science
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• v.33 no.2
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• pp.169-175
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• 2023

As a protective defensive mechanism against ultraviolet (UV) light exposure in skin tissue, melanocytes produce the pigment melanin. Tyrosinase plays a key role in melanin production in melanocytes. However, the overproduction of melanin can lead to lesions, such as freckles and dark spots. Thus, it is clinically important to find a modulating molecule to control melanogenesis by regulating tyrosinase expression and/or activity. It is known that catechin, a plant flavonoid, can reduce melano- genesis through the downregulation of tyrosinase expression. Here, we tested whether catechin derivatives isolated from the stem bark of Ulmus parvifolia have an effect on melanin production by regulating tyrosinase in mouse melanoma cells and in vitro mushroom tyrosinase. The catechin derivatives used in this study included C5A, C7A, C7G, and C7X. Treatments using these catechin derivatives reduced melanin production in mouse melanoma B16F10 cells in which melanogenesis was stimulated by α-MSH. Notably, the anti-melanogenic effects of catechin derivatives were similar to those of kojic acid, a well-known anti-melanogenic molecule. Both C5A and C7A directly inhibited the activity of tyrosinase isolated from mushrooms in vitro. Furthermore, our in silico computational simulation showed that these two compounds were expected to bind to the active site of tyrosinase, which is similar to kojic acid. In addition, all four catechin derivatives reduced tyrosinase protein expression. In summary, our results showed that catechin derivatives can reduce melanogenesis by regulating tyrosinase activity or expression. Thus, this study suggests that catechin derivatives isolated from U. parvifolia can be novel modulators of melanin production.

• Molecules and Cells
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• v.38 no.2
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• pp.163-170
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• 2015

Lipoteichoic acid (LTA) is a major component of the cell wall of Gram-positive bacteria. Its effects on living organisms are different from those of lipopolysaccharide (LPS) found in Gram-negative bacteria. LTA contributes to immune regulatory effects including anti-aging. In this study, we showed that LTA isolated from Lactobacillus plantarum (pLTA) inhibited melanogenesis in B16F10 mouse melanoma cells. pLTA reduced the cellular activity of tyrosinase and the expression of tyrosinase family members in a dose-dependent manner. The expression of microphthalmia- associated transcription factor (MITF), a key factor in the synthesis of melanin, was also decreased by pLTA. Further, we showed that pLTA activated melanogenesis signaling, such as extracellular signal-regulated kinase (ERK) and phosphatidylinositol 3-kinse (PI3K)/AKT. In addition, the expression of heterogeneous nuclear ribonucleoprotein A1 (hnRNP A1) and HuR, which are important RNA-binding proteins (RBPs), was reduced. pLTA likely degrades MITF via regulation of melanogenic signaling and RNA stability of melanogenic proteins, resulting in the reduction of melanin. Thus, our data suggest that pLTA has therapeutic potential for treating hyperpigmentation disorders and can also be used as a cosmetic whitening agent.

• YAKHAK HOEJI
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• v.49 no.5
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• pp.375-379
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• 2005

The green marine algae, Capsosiphon fulvescens is one of the important economic seaweeds cultured in Korea. In this study, we investigated the effects of Capsosiphon fulvescens on melanogenesis using B16 cells. Our results showed that Capsosiphon fulvescens significantly inhibits melanin synthesis and it reduces the activity of tyrosinase, the rate-limiting melanogenic enzyme. Western Blot analysis using anti-tyrosinase antibody revealed that Capsosiphon fulvescens ($10\~40\;{\mu}g/ml$ decreased tyrosinase protein levels. Cell proliferation was dose-dependently inhibited by 10, 20 and 40 ${\mu}g/ml$ Cap­sosiphon fulvescens, without cytotoxicity and morphological change. These results suggest that the depigmenting effect of Capsosiphon fulvescens is correlated with the suppression of tyrosinase activity and protein level, which are key enzymes for melanogenesis.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.39 no.1
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• pp.19-24
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• 2013

To investigate the efficacy of enzymatic extract of Ecklonia cava and its polyphenol extract (AG-DK) as cosmetic ingredients, the anti-oxidative effect, anti-glycation effect, anti-melanogenic effect, and anti-inflammatory effect of the extracts were evaluated in vitro. The enzymatic extract of E. cava ($SC_{50}$ 42.9 ppm) and AG-DK ($SC_{50}$ 6.4 ppm) showed a strong DPPH free radical scavenging activity. The anti-glycation ability of the enzymatic extract of E. cava and AG-DK was tested using bovine serum albumin (BSA), which inhibited the formation of advanced glycation end-products (AGEs) in the BSA/glucose system. The enzymatic extract of E. cava ($IC_{50}$ 97.2 ppm) and AG-DK ($IC_{50}$ 7 ppm) had inhibitory effects on tyrosinase activity. Moreover, the enzymatic extract of E. cava and AG-DK had an anti-inflammatory effect through the inhibition of nitricoxide (NO) and prostaglandin E2 ($PGE_2$). These findings suggest that the enzymatic extract of E. cava and AG-DK can be applied to skin-care products as cosmetic ingredients.

• Preventive Nutrition and Food Science
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• v.2 no.4
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• pp.285-290
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• 1997

Previously, a 50% aqueous methanol extract of Galla rhois was shown to be the most potent tyrosinase inhibition activity with an {TEX}$IC_{50}${/TEX}(the concentration causing 50% inhibition of tyrosinase activity) of 0.2mg/ml of 205 crude drug extracts. To isolate tyrosinase inhibitors, the methanol extract was evaporated to a small volume in vacuo, and then partitioned stepwise with benzene and ethyl acetate(EtOAc). the EtOAc fraction was solubilized in 10% MeOH solution, and then fractionated successively by Diaion HP-20 and Sephadex LH-20 column chromatography, and preparative HPLC. Three phenolic compounds were isolated, and characterized as gallic acid(GA), methyl gallate(MG) and 1,2,3,4,6-penta-O-galloyl-$\beta$-D-glucose(PGG) by UV, IR, {TEX}${1}^H${/TEX}-&{TEX}${13}^C${/TEX}-NMR, and FAB-MS spectroscopy, PGG({TEX}$IC_{50}${/TEX}=50$\mu\textrm{g}$/ml) showed a considerable inhibitory effect against mushroom tyrosinase, while GA({TEX}$IC_{50}${/TEX}=1.6mg/ml) and MG({TEX}$IC_{50}${/TEX}=234$\mu\textrm{g}$/ml) did not show an appreciable effect. Meanwhile, MG inhibited greatly melanogenesis in a murine melanocyte cell line, Mel-Ab. MG and PGG showed typical noncompetitive inhibition patterns against mushroom tyrosinase. These results suggest that PGG and MG may be potentially useful as either anti-browning or anti-melanogenic agents in foods and cosmetics.

• Korean Journal of Medicinal Crop Science
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• v.19 no.3
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• pp.177-184
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• 2011

This study was performed to assess the antioxidant activities and whitening effects of Agrimonia pilosa Ledeb on melanin synthesis. The whitening effects of Agrimonia pilosa Ledeb water extracts were examined by in vitro mushroom tyrosinase assay and B16BL6 melanoma cells. We assessed inhibitory effect of Agrimonia pilosa Ledeb water extract on expression of melanogenic enzyme proteins including tyrosinase, tyrosinase-related protein 1 (TRP-1) and tyrosinase-related protein 2 (TRP-2) in B16BL6 cells. Inhibitory effect of Agrimonia pilosa Ledeb onto free radical generation was determined by measuring DPPH and hydroxyl radical scavenging activitie. Our results indicated that Agrimonia pilosa Ledeb water extract effectively inhibited free radical generation. In DPPH and hydroxy radical scavenging activity, Agrimonia pilosa Ledeb water extract had a potent anti-oxidant activity in a dose-dependent manner. They significantly inhibited tyrosinase activity in vitro and in B16BL6 melanoma cells. Also, Agrimonia pilosa Ledeb suppressed the expression of tyrosinase in B16BL6 melanoma cells. These results show that Agrimonia pilosa Ledeb inhibited melanin production on the melanogenesis. The underlying mechanism of Agrimonia pilosa Ledeb on whitening activity may be due to the inhibition of tyrosinase activity. We suggest that Agrimonia pilosa Ledeb may be useful as new natural active ingredients for antioxidant and whitening cosmetics.

• Journal of Nutrition and Health
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• v.53 no.2
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• pp.121-128
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• 2020

Purpose: The Rubus coreanus fruit (RF) is an important traditional medicinal herb having antioxidant, anti-inflammatory, and immunoregulatory properties. These activities are known to change dramatically, depending on maturity of the RF. It is presumed that change of functional components, such as flavonoids, tannins, phenolic acids, triterpenoids and organic acids in RF, affect the various bioactivities. This study aimed to confirm changes in the anti-melanogenic effects of RF based on maturity, and to identify the bioactive compounds responsible. Methods: The cell viability of mature RF (MRF) and immature RF (IRF) extracts was investigated using B16F10 cells. To compare the anti-melanogenic effect of MRF and IRF extracts, we first assessed the melanin content. High-performance liquid chromatography analysis was performed to evaluate changes in the level of ellagic acid according to maturity of the RF. In addition, tyrosinase inhibitory activity of both extracts was examined. Results: MRF and IRF extracts (50-200 ㎍/mL) do not affect the cell viability of B16F10 melanoma cells. IRF extract more effectively inhibited melanin synthesis than MRF extract. The content of ellagic acid in IRF extract was higher than that obtained in MRF extract. Furthermore, greater inhibition of tyrosinase activity was observed after exposure to IRF extract than MRF extract. A positive correlation was determined between ellagic acid content and tyrosinase inhibitory activity, and a negative correlation was obtained between ellagic acid content and melanin content. Taken together, our results indicate that ellagic acid is one of the major bioactive compounds of RF that imparts a whitening effect. Conclusion: Our results indicate that ellagic acid in MRF and IRF extracts affect the anti-melanogenesis effect through inhibition of tyrosinase activity. Therefore, the ellagic acid rich IRF has greater potential for application as a natural and functional cosmetic material.

• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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• v.26 no.1
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• pp.1-18
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• 2013

Objective: Recently the demands for the effective and safe depigmentative and anti-aging agents of the skin have increased due to the medical, pharmaceutical and cosmetic reasons. The purpose of this study is to investigate the MKG(Methanol Extract of Kaempferia galanga) and their dermal bioactivity properties related to cosmeceuticals such as depigmentation. Methods: We assessed inhibitory effects of MKG on melanin production in B16/F10 melanoma cells, on mushroom tyrosinase activity, effects of MKG on the expression tyrosinase, TRP-1, TRP-2, GSK-$3{\beta}$, CREB, MITF in B16/F10 melanoma cells without cytotoxicity range. Cell viability was measured by MTT assay and tyrosinase activity was assessed using by DOPA staining, western-blot analysis. We measured inhibition of melanin synthesis and tyrosinase activity by down-regulation of melanogenic enzyme expressions in ${\alpha}$-MSH induced melanogenesis B16/F10 melanoma cells. Results: MKG inhibited tyrosinase-activity, total melanin contents and dendrite out-growth. MKG inhibited melanogenesis by down-regulation of tyorsinase, TRP-1, TRP-2, CREB, and MITF in B16/F10 cells. The treatment with MKG at the 12.5, $25{\mu}g/ml$ level significantly inhibited the melanin synthesis induced ${\alpha}$-MSH in B16/F10 melanoma cells compared with untreated control. Conclusion: These results suggest that MKG inhibit melanin biosynthesis which is involved in hyper-pigmentation. So MKG is considered to be used as a whitening components reducing cytotoxicity.

• 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.