• Journal of Ginseng Research
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• v.42 no.3
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• pp.389-399
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• 2018

Background: The antioxidant effects of Panax ginseng have been reported in several articles; however, little is known about the antimelanogenesis effect, skin-protective effect, and cellular mechanism of Panax ginseng, especially of P. ginseng calyx. To understand how an ethanol extract of P. ginseng berry calyx (Pg-C-EE) exerts skin-protective effects, we studied its activities in activated melanocytes and reactive oxygen species (ROS)-induced keratinocytes. Methods: To confirm the antimelanogenesis effect of Pg-C-EE, we analyzed melanin synthesis and secretion and messenger RNA and protein expression levels of related genes. Ultraviolet B (UVB) and hydrogen peroxide ($H_2O_2$) were used to induce cell damage by ROS generation. To examine whether this damage is inhibited by Pg-C-EE, we performed cell viability assays and gene expression and transcriptional activation analyses. Results: Pg-C-EE inhibited melanin synthesis and secretion by blocking activator protein 1 regulatory enzymes such as p38, extracellular signal-regulated kinases (ERKs), and cyclic adenosine mono-phosphate response element-binding protein. Pg-C-EE also suppressed ROS generation induced by $H_2O_2$ and UVB. Treatment with Pg-C-EE decreased the expression of matrix metalloproteinases, mitogen-activated protein kinases, and hyaluronidases and increased the cell survival rate. Conclusion: These results suggest that Pg-C-EE may have antimelanogenesis properties and skin-protective properties through regulation of activator protein 1 and cyclic adenosine monophosphate response element-binding protein signaling. Pg-C-EE may be used as a skin-improving agent, with moisture retention and whitening effects.

• Journal of Microbiology and Biotechnology
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• v.29 no.8
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• pp.1204-1211
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• 2019

Fungal exopolysaccharides are important natural products having diverse biological functions. In this study, exopolysaccharides from Fomitopsis castanea mycelia (FEPS) were prepared, and the highest mushroom tyrosinase inhibitory activity was found. FEPS were prepared from cultivation broth by ethanol precipitation method. The extraction yield and protein concentration of FEPS were 213.1 mg/l and 0.03%, respectively. FEPS inhibited mushroom tyrosinase with the half maximal inhibitory concentration ($IC_{50}$) of 16.5 mg/ml and dose-dependently inhibited cellular tyrosinase activity (63.9% at $50{\mu}g/ml$, and 83.3% at $100{\mu}g/ml$) in the cell-free extract of SK-MEL-5 human melanoma cell and ${\alpha}$-melanocyte-stimulating hormone (${\alpha}-MSH$)-stimulated melanin formation in intact SK-MEL-5 human melanoma cell. The $IC_{50}$ of FEPS against NO production from RAW264.7 macrophage cells was $42.8{\pm}0.64{\mu}g/ml$. By in vivo study using a zebrafish model, exposure of FEPS at $400{\mu}g/ml$ to dechorionated zebrafish embryos for 18 h decreased the pigment density, compared to that without FEPS-treated control.

• Journal of Physiology & Pathology in Korean Medicine
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• v.23 no.1
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• pp.63-75
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• 2009

The aim of this study was to elucidate the antimelanogenic effect of Dokhwalkisaeng-tang(Duohujisheng-tang) in B16F10 melanoma cells. Dokhwalkisaeng-tang(DKT) was used to develop the effective prescription of inhibition of melanin production. We determined inhibitory effects of DKT on melanin-release, melanin production, and tyrosinase activity in B16F10 melanoma cells. And to explicate the action-mechanism of DKT, melanin-related gene expressions were determined using RT-PCR and real time RT PCR technique in B16F10 melanoma cells. DKT inhibited melanin-release, melanin production in B16F10 melanoma cells considerably. DKT inhibited tyrosinase activity in vitro and in B16F10 melanoma cells. DKT inhibited the expression of tyrosinase, TRP-1, TRP-2 in B16F10 melanoma cells. DKT inhibited the expression of PKA, PKC, MMP-2 and MITF in B16F10 melanoma cells. On the other hand, DKT increased the expression of ERK-1, ERK-2, AKT-1 in B16F10 melanoma cells. From these results, we propose that DKT may have effect on the antimelanogenesis.

• Journal of Pharmaceutical Investigation
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• v.28 no.3
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• pp.177-183
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• 1998

Low toxicity, reverse thermal gelation and high drug loading capabilities suggest that poloxamer 407 gels have great potential as a topical drug delivery system. Kojic acid (KA) is an antimelanogenic agent which has been widely used in cosmetics to whiten the skin color. However, it has the drawbacks of skin irritancy due to its acidic pH. Poloxamer gels of different polymer contents were formulated to overcome the problem and compared to the cream type formulations of either w/o/w multiple emulsion cream or o/w type emulsion cream. Using Franz diffusion cells mounted with a synthetic cellulose membrane (MWCO 12,000), drug release characteristics of the formulations were evaluated by the HPLC assay of KA concentration in the receptor compartment of pH 7.4 phosphate buffered saline solutions. Drug release from w/o/w multiple emulsion cream was controlled by oil membrane, showing the apparent zero order release kinetics. The KA release from the poloxamer gels was also controlled by the gel matrix, showing that drug release increased linearly as KA contents increase, but decreased exponentially as the polymer contents increase. In the skin irritancy test, the primary irritancy index(PII) of poloxamer gel base was lower than those of multiple emulsion cream base and o/w cream. Depending on KA contents or polymer contents in the gel. PH values in poloxamer gels were ranged from 1.3 to 2.0, which are interpreted as low or negligible irritation on skin. There was a good correlation between the log value of flux in drug release and PII value in skin irritation. It was possible to conclude that the poloxamer gels containing KA might be a good candidate for an antimelanogenic topical delivery system by virtue of the controlled release of the drug and the reduced skin irritancy.

• Journal of Pharmaceutical Investigation
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• v.28 no.2
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• pp.87-92
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• 1998

Kojic acid (KA) is an antimelanogenic agent which has been widely used in cosmetics to whiten the skin color. However, it has the drawbacks of the skin irritancy and the instability against the pH, temperature, and light. In order to overcome these problems, various topical gels and multiple emulsion creams which can control the release of active ingredient, KA, were formulated employing cream bases of mineral oil with caprylic capric triglyceride and hydrophilic polymers such as chitosan, carbopol. and pluronics. Using Franz diffusion cells mounted with a synthetic cellulose membrane (MWCO 12,000), drug release characteristics of the formulations were evaluated by the HPLC assay of KA concentration in the receptor compartment of pH 7.4 phosphate buffered saline solution. Drug release from chitosan-based gels (ChitoGel) obeyed to the first order kinetics with a rapid release especially in the initial period. However, pluronic-based gels (PluGel) and carbopol-based gels (CarboGel) revealed controlled release of drug to some extent, followed by the square root-time kinetics. Moreover, the release of KA was further controlled with the W/O/W multiple emulsion creams (MultiCream), showing the apparent zero order release kinetics by virtue of dynamic ratecontrolling membrane of the oil layer. The flux $(J,\;{\mu}g/cm^2/hr)$ of ChitoGel. CarboGel. PluGel. and MultiCream in the initial period of 6hr were 73.30, 28.67. 24.04 and 7.72, respectively. On the other hand, the skin irritancy score of ChitoGel and MultiCream were observed as 2.5 and 2.3 respectively, in the rabbit skin irritation test. Although there were insignificant differences at p<0.05 between those formulations, it was possible to conclude that the W/O/W multiple emulsion creams containing KA might be a good candidate for an antimelanogenic drug delivery system due to the controlled release of acidic drug molecules.

• Journal of Ginseng Research
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• v.41 no.4
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• pp.602-607
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• 2017

Background: Panax ginseng is a traditional herb used for medicinal purposes in eastern Asia. P. ginseng contains various ginsenosides with pharmacological effects. In this study, floralginsenoside A (FGA), ginsenoside Rd (GRD), and ginsenoside Re (GRE) were purified from P. ginseng berry. Methods: Chemical structures of FGA, GRD, and GRE were determined based on spectroscopic methods, including fast atom bombardment mass spectroscopy, ID-nuclear magnetic resonance, and infrared spectroscopy. Inhibitory activities of these compounds on melanogenesis were studied by measuring the expression of protein and melanin content in the melan-a cell line. This inhibitory activity was confirmed by observing pigmentation and tyrosinase activities of zebrafish. Results: GRD, GRE, and FGA were not cytotoxic at concentrations less than $20{\mu}M$, $80{\mu}M$, and $160{\mu}M$ in melan-a cells, respectively. GRD, GRE, and FGA inhibited melanin biosynthesis in melan-a cells by 15.2%, 22.9%, and 23.9% at $20{\mu}M$, $80{\mu}M$, and $160{\mu}M$, respectively. FGA was observed to display the most potent inhibitory effect. In addition, FGA decreased microphthalmia-associated transcription factor protein expression in a dose-dependent manner. Moreover, FGA induced extracellular signal-regulated kinase phosphorylation level in melan-a cells. In addition, melanin pigment content and tyrosinase activity in zebrafish treated with FGA at $160{\mu}M$ were reduced. Conclusion: FGA showed the most potent inhibition of melanogenesis in both in vitro and in vivo studies. This study suggests that FGA purified from P. ginseng may be an effective melanogenesis inhibitor.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.30 no.3 s.47
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• pp.415-418
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• 2004

Arbutin is a glycosylated hydroquinone found at high concentration in certain plants capable of surviving extreme and sustained dehydration. It has been reported to have an inhibitory effect of melanogenesis and to be hydrolyzed easily to yield glucose and hydroquinone by ${\beta}-glucosidase.$ While hydroquinone also has an anti-melanogenic effect, however, is carefully used as a topical whitening agent because of side effects. The present study was undertaken to examine the inhibitory effect of an whitening agent containing arbutin and ${\beta}-glucosidase$ on UV radiation induced pigmentation in human skin. Experimental subjects were UVB-irradiated on the back. UVB-irradiated areas were assigned to three groups: arbutin and ${\beta}-glucosidase$ treated group, vehicle control, and no-application control. Arbutin and ${\beta}-glucosidase$ treatment inhibited pigmentation by 50.17 percent, compared with the controls (N : 10: P<0.05). These results suggest that the whitening agent containing arbutin and ${\beta}-glucosidase$may be used as an agent to inhibit melanin formation induced by UV radiation.

• Journal of the Korean Society of Food Science and Nutrition
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• v.44 no.12
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• pp.1905-1911
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• 2015

Melanin is one of the most important factors affecting skin color. Melanogenesis is the bioprocess of melanin production by melanocytes in the skin and hair follicles and is mediated by several enzymes, such as tyrosinase, tyrosinase related protein (TRP)-1, and TRP-2. Convenient enzymatic transformation of the simple phenol pyrogallol with polyphenol oxidase originating from pear to an oxidative product, purpurogallin, was efficient. The structure of the pyrogallol oxidation product was identified on the basis of spectroscopic methods. The biotransformation product purpurogallin showed significant inhibitory effects against both melanin synthesis and tyrosinase activity in a dose-dependent manner in B16 melanoma cells. In addition, purpurogallin significantly attenuated melanin production by inhibiting TRP-1, and TRP-2 expression through modulation of their corresponding transcription factors, and microphthalamia- associated transcription factor in B16 cells. Consequently, purpurogallin derived from convenient enzymatic transformation of pyrogallol might be a beneficial material for reducing skin hyperpigmentation.

• Korean Journal of Food Science and Technology
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• v.44 no.1
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• pp.94-99
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• 2012

We investigated the in vitro antioxidant and antimelanogenesis effects of ethanol extracts from eggplant (Solanum melongena L.) peels. The total phenolics and chlorogenic acid in ethanol extracts were 2,465 mg/100 g and 2.08 mg/100 g, respectively. ABTS radical scavenging activity, ferric reducing/antioxidant power assay, and malondialdehyde (MDA) inhibitory effect of the extracts increased in a dose-dependent manner. In addition, the extracts generally showed strong UV absorption in the range of UV-B (290-320 nm). The $IC_{50}$ of mushroom tyrosinase inhibitory activity of ethanol extracts from eggplant peels was 870 ${\mu}g/mL$. Importantly, the melanin syntheses of B16/F10 melanoma cells were decreased by extracts in a concentration-dependent manner. Overall, these results suggest that eggplant peels can be potentially applied as a anti-melanogenic agent as well as an antioxidant resource.

• Microbiology and Biotechnology Letters
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• v.47 no.2
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• pp.195-200
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• 2019

The purpose of this study was to investigate the melanogenesis inhibiting activity of the ethanol extract from Polygonum amphibium L. Firstly, the n-hexane (Hx), chloroform ($CHCl_3$), ethyl acetate (EA), n-butanol (BuOH), and water (Water) fractions were isolated from the P. amphibium L. ethanol extract. The efficacy of melanogenesis was found to significantly decrease via the EA and BuOH fractions when compared to the control in B16F10 cells. EA particularly showed the lowest melanin content in B16F10 cells when compared to all the other extracts. Concentration-dependent inhibition of melanin synthesis was also observed in the EA fraction at concentrations below $50{\mu}g/ml$, which did not exhibit cytotoxicity in B16F10 cells. Notably, the expression of three key proteins (tyrosinase, tyrosinase-related protein-1 (TRP-1), and TRP-2), which are involved in melanogenesis, were significantly decreased via the EA fraction. EA also inhibited body pigmentation in vivo in a zebrafish model. Overall, we demonstrated melanogenesis suppression using the EA fraction from P. amphibium L., which could be a potential candidate for an antimelanogenesis agent.