• Journal of the Society of Cosmetic Scientists of Korea
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• v.27 no.1
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• pp.99-109
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• 2001

Novel glucoconjugates phenolic moiety, 3-(methoxycarbonyl)-4-(hydroxyphenyl)-$\beta$-D-glucopyranoside(4), 3-(methoxyacetyl)-4-(hydroxyphenyl)-$\beta$-D-glucopyranoside(7), 4-(hydroxyphenyl)-$\beta$-D-ribofuranoside(11), were synthesized. In order to investigate their depigmentation effect, inhibitory activity against mushroom tyrosinase and inhibitory activity of melanin synthesis in B16 melanoma cell were evaluated in vitro. Compound 11 showed 92.0$\mu\textrm{g}$/㎖ of tyrosinase inhibitory activity whereas compound 4 and 7 showed very low activity not less than 300$\mu\textrm{g}$/㎖. Inhibitory activities of melanin synthesis in B16 melanoma cell of compound 4, 7, and 11 were 8.7, 15.1, and 36.0%, respectively, at the concentration of 100$\mu\textrm{g}$/㎖. Inhibitory activity of compound 11 was much higher than that of arbutin at the same concentration.

• 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.

• Journal of Physiology & Pathology in Korean Medicine
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• v.23 no.3
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• pp.574-580
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• 2009

Melanogenesis is induced mainly by ultraviolet radiation of sunlight and ${\alpha}$-Melanocyte stimulation hormone (${\alpha}$-MSH) which binds to a specific G protein coupled receptor. ${\alpha}$-MSH and cAMP-elevating agents are known to melanin syntheisis and dendrite outgrowth. The purpose of this study was to investigate the mechanism of melanogenesis inhibition in B16/F10 cells by ethanol extract of Artemisiae Capillaris Herba. In the present study, ${\alpha}$-MSH led to a stimulation of melanin synthesis that appeared to result from an increased tyrosinase activity and melanin content. However, the ethanol extract of Artemisiae Capillaris Herba inhibited the ${\alpha}$-MSH-induced tyrosinase activity and melanin content. In control conditions, B16/F10 cells displayed a fibroblastic appearance while ${\alpha}$-MSH treatment promoted the emergence of small and numerous dendrites from the plasma membrane. The ethanol extract of Artemisiae Capillaris Herba abolished the ${\alpha}$-MSH-induced dendricity. Regarding protein levels of the melanogenic enzymes, the amounts of tyrosinase were increased after incubation with ${\alpha}$-MSH. The treatment of Artemisiae Capillaris Herba ethanol extract decreased the ${\alpha}$-MSH expression levels of tyrosinase. Based on these findings, it is likely that the ethanol extract of Artemisiae Capillaris Herba exerts its depigmenting effects in B16/F10 cells through the suppression of tyrosinase expression, which are key enzymes for melanogenesis.

• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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• v.21 no.1
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• pp.104-112
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• 2008

Objective : This experimental study was preformed to investigate the effect of ethanol extract of Belamcandae Rhizoma (EBR) on dermal bioactive properties related to cosmeceuticals such as radical scavenging activity and depigmentation. Methods : The free radical scavenging activity of EBR was assayed in cell free systems using 1,1-diphenyl-2-picrylhydrazyl (DPPH). Antibacterial potency was measured by the size of inhibition zone with change of volume. Cell viability was measured by MTT assay and tyrosinase activity was assessed using L-DOPA. Results : EBR showed slightly radical scavenging activity and protected against UVB-induced cell cytotoxicity. Futhermore, EBR showed antibacterial activities on S. epidermidis and S. aureus. Although the proliferation of B16/F10 cells was decreased by EBR, necrosis was not revealed. EBR augmented tyrosinase activity and dendrite outgrowth in B16/F10 cells. Conclusions : These results suggest that EBR has antioxidative ＆ antibacterial activities, and stimulate melanogenesis.

• Proceedings of the SCSK Conference
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• 2003.09b
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• pp.174-183
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• 2003

To obtain effective and safe topical depigmenting agents, we synthesized hydroxybenzoates, alkoxybenzoates, and 3,4,5-trimethoxycinnamate containing a thymol moiety and screened then for high-level inhibitory activity against melanin synthesis. Among them, 5-methyl-2-(methylethyl)phenyl (2Ε)-3-(3,4,5-trimethoxyphenyl)prop-2-enoate (Melasolv)$^{TM}$ 4h, showed the most potent depigmenting effect ($IC_{50}$/ = 10$\mu$M) with low cytotoxicity ($IC_{50}$/ = 200$\mu$M). To find the inhibition mechanism of our candidate, various in vitro tests were performed such as DPPH assay, tyrosinase activity in mushroom or in culture cell and expression of tyrosinase, TRP-l and TRP-2. The result of this study suggested that 4h inhibited melanin synthesis by reducing the expression of tyrosinase and TRP-l at the transcriptional level in melan-a melanocytes.s.

• Journal of the Korean Society of Food Science and Nutrition
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• v.37 no.12
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• pp.1679-1683
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• 2008

The objectives of this study were to determine inhibitory effect on tyrosinase activity and antioxidant activity of the methanolic extract from grape seeds and to investigate relationships between tyrosinase inhibitory activity and antioxidant activity of the extract. The 80% methanol extracts of grape seeds were fractionated subsequently with hexane, chloroform, ethyl acetate and water. The methanolic extract and fractions from grape seeds inhibited tyrosinase activity in a concentration dependent manner. The methanolic extracts showed the highest inhibitory effects on tyrosinase activity. The inhibitory effects of the ethyl acetate fraction from the methanolic extract on tyrosinase activity was higher than other fractions. The ethyl acetate fraction from methanolic extracts showed higher antioxidant activity and contained higher polyphenolic and flavonoid contents compared to other fractions. The correlation coefficients among the polyphenoilc content of methanolic extracts, ABTS radical cation scavenging activity and inhibitory effect of tyrosinase were relatively high. These results suggest that grape seeds may have potential as a depigmentation agent for cosmetics and functional food products.

• Journal of Physiology & Pathology in Korean Medicine
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• v.21 no.5
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• pp.1243-1249
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• 2007

The aim of this study was to investigate the effect of ethanol extract of Fagopyrum esculentum on the melanogenesis. To determine whether ethanol extract of Fagopyrum esculentum suppress melanin synthesis in cellular level, B16F10 melanoma cells were cultured in the presence of different concentrations of Fagopyrum esculentum ethanol extract. In the present study, we examined the effects of Fagopyrum esculentum ethanol extract on cell proliferation, melanin contents, tyrosinase activity, expression of melanogenic enzyme proteins including tyrosinase, tyrosinase-related protein 1 (TRP-1) and tyrosinase-related protein 2 (TRP-2). Cell proliferation was slightly increased by treatment with ethanol extract of Fagopyrum esculentum $(25-200 {\mu}g/m{\ell}).$ The ethanol extract of Fagopyrum esculentum effectively suppressed melanin contents at a dose of $100 {\mu}g/m{\ell}).$ It was observed that the color of cell pellets was totally whitened compared with the control. The ethanol extract of Fagopyrum esculentum inhibited tyrosinase activity, regulate melanin biosynthesis as the key enzyme in melanogenesis. Using western blot analysis, the ethanol extract of Fagopyrum esculentum dose-dependently decreased tyrosinase and TRP-1 protein levels, and tyrosinase and TRP-1 were detected in similar manner. ${\alpha}-MSH$ leads to a stimulation of melanin synthesis through increase of tyrosinase activity, melanin contents and cytoplasmic dendricity. In this study, ethanol extract of Fagopyrum esculentum down-regulated the ${\alpha}-MSH$-induced tyrosinase activity, melanin contents and cytoplasmic dendricity. Regarding protein levels of the melanogenic enzymes, the amounts of tyrosinase and TRP-1 was increased after incubation with a-MSH. The treatment of ethanol extract of Fagopyrum esculentum decreased the ${\alpha}-MSH$-induced expression levels of tyrosinase and TRP-1. These results suggest that the ethanol extract of Fagopyrum esculentum exerts its depigmenting effects through the suppression of tyrosinase, TRP-1 and cytoplasmic dendricity. And it may be a potent depigmetation agent in hyperpigmentation condition.

• Journal of Physiology & Pathology in Korean Medicine
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• v.22 no.4
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• pp.829-834
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• 2008

This study was to investigate the effect of Ponciri Fructus ethanol extract on the melanogenesis. The Ponciri Fructus markedly decreased melanin contents of B16F10 cells at a dose of $80{\mu}g/m{\ell}$. It was observed that the color of cell pellets was totally whitened compared with the control. The treatment of Ponciri Fructus inhibited tyrosinase activity, regulate melanin biosynthesis as the key enzyme in melanogenesis. Regarding protein levels of the melanogenic enzymes, the Ponciri Fructus dose-dependently decreased tyrosinase and TRP-1 protein levels, and tyrosinase and TRP-1 were detected in similar manner. These results suggest that the Ponciri Fructus ethanol extract exerts its depigmenting effects through the suppression of tyrosinase and TRP-1.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.30 no.1
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• pp.33-38
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• 2004

Melanin pigmentation in human skin is a major defense mechanism against ultraviolet light of the sun, but abnormal pigmentation such as freckles, liver spot could be a serious aesthetic problem. Nearly all studies are mainly concentrated on searching for the materials that have inhibitory activities on tyrosinase. In this work, to isolate phenolic compounds from Gastrodia elata, we purified the extract through solvent fractionation, column chromatography, and recrystallization. They were identified as 4-hydroxybenzyl alcohol 1, bis(4-hydroxyphenyl)methane 2, gastrodin (4-${\beta}$-D-glucopyranosyloxybenzyl alcohol) 3 on the base of spectroscopic evidences. In order to investigate their depigmentation effect, inhibitory activity against mushroom tyrosinase and inhibitory activity of melanin synthesis in B16 melanoma cells were evaluated in vitro. We have found that 4-hydroxybenzyl alcohol 1 and gastrodin (4- ${\beta}$-D-glucopyranosyloxybenzyl alcohol) 3 have no tyrosinase inhibitory activity, but inhibit the melanin synthesis in B16 melanoma cells. Tyrosinase inhibitory activities of bis(4-hydroxyphenyl)methane 2 (IC$\_$50/ = 400 $\mu\textrm{g}$/mL) and butanol fraction (IC$\_$50/ = 46 $\mu\textrm{g}$/mL) were lower/higher than that of arbutin (IC$\_$50/ = 114 $\mu\textrm{g}$/mL), but inhibitory activities of melanin synthesis in B16 melanoma cells were much higher than that of arbutin. Especially, tyrosinase inhibitory activities of isolated phenolic fraction (IC$\_$50/ = 2.37 $\mu\textrm{g}$/mL) from butanol fraction was very higher than that of arbutin (IC$\_$50/ = 114 $\mu\textrm{g}$/mL). Therefore, these results suggest that isolated phenolic compounds from Gastrodia elata have inhibitory activity against mushroom tyrosinase and inhibitory activity of melanin synthesis in 816 melanoma cells in vitro.

• Journal of Physiology & Pathology in Korean Medicine
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• v.24 no.4
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• pp.674-680
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• 2010

The purpose of this study was to investigate the effects of Fructus Ligustri Lucidi (FLL) on the process of melanogenesis. Cell viability of B16F10 cells was measured by MTT assay and melanin content was assessed using the method of Hosoi with some modifications. Methanol extract of Fructus Ligustri Lucidi (MFLL) significantly inhibited melanin synthesis in a concentration-dependent manner, and it reduced the activity of tyrosinase, the rate-limiting melanogenic enzyme. Additionally, $\alpha$-melanocyte stimulation hormone ($\alpha$-MSH)-induced hyperpigmentation was down-regulated by MFLL. MFLL was fractionated by organic solvent. In the present study, Hexane extract of Fructus Ligustri Lucidi (HFLL) inhibited tyrosinase activity and melanin production of B16F10 cells in the absence or presence of $\alpha$-MSH. Ethyl acetate, butanol and water layers did not affect tyrosinase activity and melanin production. Meanwhile ethyl acetate, butanol and water layers showed DPPH free radical scavenging activity. These results suggest that extract of FLL could be used as functional biomaterial in developing a skin whitening agent having the antioxidant activity.