• Bulletin of the Korean Chemical Society
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• v.29 no.1
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• pp.43-46
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• 2008

The aim of present study was to examine the inhibitory effects of hydroxamic acid derivatives on the melanogenesis. We found that hydroxamic acid moiety was important for anti-melanogenic activity. Compounds 1a and 1b strongly inhibited melanin synthesis via deactivation of tyrosinase. Hydroxamic acid has metal ion chelating ability which is similar to that kojic acid, however, anti-tyrosinase mechanism of compounds 1a and 1b was different from that of kojic acid. They showed noncompetitive inhibition kinetics

• The Korea Journal of Herbology
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• v.32 no.3
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• pp.71-78
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• 2017

Objectives : The various grape extracts derived from grape pulp, seed and skin, containing various types of polyphenols and flavonoids, have been known to have anti-inflammatory, antioxidant and improve cardiovascular condition as well as sun's damaging effects. However, there have been rare reports of various beneficial effects of grape fruit stem extract (GFSE), one of the waste products of grapes. We investigated anti-inflammatory and melanogenesis inhibitory effects of GFSE. Methods : One-hundred gram of grape fruit stem was extracted with 80% ethanol at room temperature for 3 days. After filtration, the ethanol was removed using vacuum evaporator, then lyophilized to obtain the dry extract which was stored at $-20^{\circ}C$ until used. NO levels were measured by using Greiss reagent. Prostaglandin $E_2$ ($PGE_2$) production was measured by ELISA assay. The expression levels of iNOS, COX-2, TRP-1 and TRP-2 were evaluated by western blot analysis. Results : GFSE reduced the level of nitric oxide and prostaglandin $E_2$ ($PGE_2$) production in a dose-dependent manner, compared to control. Expressions of cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) protein were also effectively inhibited by the GFSE. In a tyrosinase inhibitory activity, GFSE significantly reduced the tyrosinase activity and melanin content in a dose dependent manner, compared to control. GFSE also decreased the expression of tyrosinase related protein-1 (TRP-1) and tyrosinase related protein-2 (TRP-2), known as a melanocyte-specific gene product involved in melanin synthesis. Conclusions : Therefore, these results indicated that GFSE had powerful anti-inflammatory and anti-melanogenic effects.

• 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.

• Proceedings of the Korean Society of Applied Pharmacology
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• 2005.04a
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• pp.131-148
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• 2005

This study is peformed to investigate the effect of water extract from Vaccinium uliginosum L., on melanin production in B 16 melanoma cells, procollagen production and matrix metalloproteinase-1(MMP-1) inhibition in human fibroblast cells. One hundred grams of the Vaccinium uliginosum L. was extracted with 2000 mL of water($90^{\circ}C$, 16h, 2times). The water extracts were lyophilized and stored at $4^{\circ}C$ until used. Dry weight yields of extracts of Vaccinium uliginosum L. were $3\%$(w/w). Extracts from Vaccinium uliginosum L. showed scavenger activities on DPPH radical, superoxide anion radical, hydroxyl radical, hydrogen peroxide and singlet oxygen radical. And these substances inhibited release of cyiokines from human keratinocyte after UV B exposure. Therefore we confirmed that extracts from Vaccinium uliginosum L. had antioxidative effect. These substances inhibited purified tyrosinase activity and melanogenesis in B 16 melanoma cells treated/untreated IL-$1{\alpha}$. Moreover this extract stimulated procollagen production and inhibited MMP-1 production in human fibroblast cells treated/untreated IL-$1{\beta}$. Therefore we confirmed that extracts from Vaccinium uliginosum L. had whitening effect. And these substances decreased degree of wrinkle in hairless mouse skin that induced by UV B irradiation. Therefore we confirmed that extracts from Vaccinium uliginosum L. had anti-wrinkle effect. From the above results, it is possible that Vaccinium uliginosum L. may be developed to be an anti-melanogenesis agent and anti-wrinkle 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 Marine Bioscience and Biotechnology
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• v.13 no.1
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• pp.1-9
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• 2021

Codium fragile (Suringar) Hariot, a green alga of the Codiales family, has been reported to have several bioactive properties, including antioxidant and anti-inflammatory properties. However, its antiobesity and whitening effects and their underlying mechanisms are unclear. This study aimed to evaluate the antiobesity and melanogenesis inhibitory effects of C. fragile using methanol extracts of C. fragile (MECF). The results of this study revealed that MECF inhibited the accumulation of lipid droplets and triacylglycerol in differentiated 3T3-L1 adipocytes, which was associated with the inhibition of the expression of adipogenesis-related transcription factors, such as peroxisome proliferator-activated receptor γ, CCAAT/enhancer-binding protein-α (C/EBPα), and C/EBPβ, which function as the key regulators of adipogenesis. Also, MECF reduced tyrosinase activity and melanin content in B16F10 cells as well as the expression of tyrosinase, tyrosinase-related protein-1 (TRP-1), TRP-2, and microphthalmia-related transcription factor in the presence of α-melanocyte-stimulating hormone. Taken together, our findings suggest that the extract of C. fragile could be considered a promising functional ingredient for the prevention and treatment of obesity and skin pigmentation in the food and cosmetic industry.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.36 no.2
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• pp.145-150
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• 2010

Anoectochilus formosanus, commonly known as "Jewel Orchids", which has been used in traditional folk medicines for feber, pain, and diseases of the lung and liver in Taiwan. We artificially cultured Anoectochilus formosanus plantlet by using the bioreactor culture system for this study from Anoectochilus formosanus. Previously, several studies have been reported on pharmacological activities of lipid-metabolism, hepatoprotective activity, anti-tumor activity and immuno-stimulating effects but other efficacy were not well known as a cosmetic ingredient for skin care. In this study, we investigated the effect of melanogenesis in B16 mouse melanoma cells and lipid droplet accumulation in 3T3-L1 preadipocytes about Anoectochilus formosanus plantlet extract. We report that Anoectochilus formosanus plantlet extract inhibits the cytoplasmic lipid droplet accumulation through adipogenic differentiation of preadipocytes as well as inhibition of tyorsinase activity and melanogenesis. As a result, our findings indicate that Anoectochilus formosanus plantlet extract may be the potential natural ingredient for whitening and slimming cosmetic products.

• Korean Journal of Plant Resources
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• v.35 no.6
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• pp.704-712
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• 2022

Research on whitening materials using natural alternatives is actively being conducted. The aim of this study was to investigate the in vitro inhibitory effects of Ranunculus chinensis Bunge (RCB) on melanogenesis and associated enzymes, such as tyrosinase, tyrosinase-related protein (TRP)-1, and TRP-2 in B16F10 murine melanoma cells. We found that RCB extract significantly attenuated melanin synthesis and reduced the activity of intracellular tyrosinase, a rate-limiting melanogenic enzyme. Western blot analysis showed that RCB extract decreased the protein expression of tyrosinase and TRP-1. In addition, it significantly decreased the expression of microphthalmia-associated transcription factor (MITF), a key regulator of melanogenesis. Extracellular signal-regulated kinase (ERK) activation has been reported to be involved in the inhibition of melanogenesis. Thus, we investigated whether the hypopigmentary effects of RCB extract were related to the activation of ERK. RCB extract induced ERK phosphorylation in a dose-dependent manner. Furthermore, it markedly inhibited body pigmentation in a zebrafish model. Our results suggest that RCB extract inhibits melanogenesis by activating ERK pathway-mediated suppression of MITF and its downstream target genes, including tyrosinase. Therefore, RCB extract can be used as a whitening agent in the development of functional cosmetics.

• Journal of Ginseng Research
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• v.45 no.5
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• pp.555-564
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• 2021

Background: Ginsenosides of Panax ginseng are used to enhance skin health and beauty. The present study aimed to investigate the potential use of ginsenoside Rf (Rf) from Panax ginseng as a new anti-pigmentation agent. Methods: The anti-melanogenic effects of Rf were explored. The transcriptional activity of the cyclic adenosine monophosphate (cAMP) response element binding protein (CREB) and the expression levels of tyrosinase, microphthalmia-associated transcription factor (MITF), and tyrosinase-related proteins (Tyrps) were evaluated in melanocytes and UV-irradiated ex vivo human skin. Results: Rf significantly inhibited Forskolin (FSK) or UV-stimulated melanogenesis. Consistently, cellular tyrosinase activity and levels of MITF, tyrosinase, and Tyrps were downregulated. Furthermore, Rf suppressed MITF promoter activity, which was stimulated by FSK or CREB-regulated transcription coactivator 3 (CRTC3) overexpression. Increased CREB phosphorylation and protein kinase A (PKA) activity induced by FSK were also mitigated in the presence of Rf. Conclusion: Rf can be used as a reliable anti-pigmentation agent, which has a scientifically confirmed and reproducible action mechanism, via inhibition of CREB/MITF pathway.

• 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.