• Journal of Ginseng Research
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• 제42권3호
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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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• 제29권8호
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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.

• 동의생리병리학회지
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• 제23권1호
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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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• 제28권3호
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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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• 제28권2호
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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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• 제41권4호
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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.

• 대한화장품학회지
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• 제30권3호
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• pp.415-418
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• 2004

알부틴은 glycosylated hydroquinone으로 여러 식물들에서, 고농도로 발견되며 비교적 안정한 물질이다. 이는 멜라닌화를 억제하는 작용이 있는 것으로 보고되어 있고, 베타-글루코시다제에 의해 포도당과 hydroquinone으로 쉽게 가수분해된다. Hydroquinone 역시 우수한 항멜라닌화 작용을 가지나, 여러 가지 부작용들로 인해 그 사용이 제한적이거나 주의를 요한다. 이 연구는 알부틴과 베타-글루코시다제를 포함하는 미백 화장품이 자외선 조사로 유도된 색소 침착을 억제하는 효과를 알아보고자 하였다. 대상은 10명의 건강한 성인으로 등 부위에 자외선 B를 조사하여 색소 침착 병변을 만들었고 이 병변들은 세 그룹: 알부틴과 베타-글루코시다제를 함유하는 미백 화장품 도포군, vehicle 대조군, no-application 대조군으로 나누었다. 알부틴과 베타-글주코시다제를 함유하는 미백 화장품 도포군은 no-application 대조군에 비교하여 색소 침착을 $50.17\%$ 억제하였다(N = 10:P<0.05). 따라서 알부틴과 베타-글루코시다제를 함유하는 미백 화장품이 기미 등 자외선 조사로 유도되거나 악화되는 과색소성 질환에 효과적으로 사용될 수 있겠다.

• 한국식품영양과학회지
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• 제44권12호
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• pp.1905-1911
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• 2015

천연 미백소재 개발과 관련하여 많은 연구들이 멜라닌 합성저해 및 활성 메커니즘을 규명하는 데 초점이 맞춰졌으며, 이러한 이유로 tyrosinase 저해제 개발이 다양하게 이루어져 왔다. 본 연구는 배 유래의 polyphenol oxidase를 이용하여 천연에 존재하는 단순 폴리페놀인 pyrogallol의 산화 축합반응을 유도하여 purpurogallin을 효율적으로 생합성하였으며, 본 화합물에 대해서 미백 활성을 평가하였다. 먼저 MTT assay를 통해 세포독성이 없는 농도구간을 설정하였으며, purpurogallin은 $25{\mu}M$ 농도의 melanoma 세포 내에서 tyrosinase 활성을 20% 이상 저해하는 것을 확인하였다. 또한 $25{\mu}M$의 시험 농도에서 purpurogallin은 약 20% 이상의 melanin 생합성 저해 활성을 나타내었다. 미백 관련 전사인자인 MITF, TRP-1, TRP-2, tyrosinase의 단백질 발현을 측정한 결과, 본 화합물은 B16F10 melanoma 세포에서 tyrosinase, TRP-1과 TRP-2의 단백질 생합성을 두 추출물 모두 억제하는 것을 확인하였다. Tyrosinase, TRP-1과 TRP-2의 발현을 조절하는 전사인자로는 MITF가 관여하는 것으로 알려져 있으며, 실제로 MITF는 melanin 생성과 관련된 여러 유전자의 발현을 조절하는 데 중요한 작용을 하고 있다. 따라서 purpurogallin은 melanin 생성과 관련된 중요한 세 가지 단백질의 생합성을 전사단계에서 조절 전사인자인 MITF의 단백질 발현을 억제하는 효과가 있음을 확인하였다. 이상의 결과로부터 멜라닌 생합성에 있어서 상위 신호단계에 있는 전사인자 MITF의 활성을 억제함으로써 하위 신호전달 과정을 억제하는 것임을 시사하며, 향후 추가적인 검증작업을 통해 화장품 소재화가 가능할 것으로 판단된다.

• 한국식품과학회지
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• 제44권1호
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• pp.94-99
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• 2012

본 연구에서는 총 페놀성 화합물 함량(2,465 mg/100 g)을 나타낸 가지 외피 에탄올 추출물의 in vitro 항산화 및 미백 효과를 알아보기 위해 다양한 연구를 진행하였다. 가지 외피 에탄올 추출물의 ABTS radical 소거활성과 FRAP assay결과 농도 의존적인 항산화 활성이 나타났으며 더불어 높은 세포 지질 과산화 억제활성을 보여주었다. 또한 가지 외피 에탄올 추출물의 자외선 흡수도를 측정한 결과 UV-A(320-400 nm)와 UV-B(290-320 nm)영역을 일정 수준 이상의 흡수 경향을 나타냈으며, 특히 UV-B(290-320 nm)영역에서 높은 흡수도를 보여주었다. 최종적으로, 미백효능을 알아보기 위해 mushroom tyrosinase 및 세포 내 멜라닌 함량 저해효과를 측정한 결과 모두 농도 의존적인 저해 효과를 보여주었다. 결국 본 연구결과를 종합해 볼 때 chlorogenic acid를 포함하여 다양한 페놀성 화합물을 함유한 가지 외피 에탄올 추출물은 in vitro 항산화 및 미백 효과를 가지는 기능성화장품 소재로서의 활용 가능성이 있을 것으로 판단된다.

• 한국미생물·생명공학회지
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• 제47권2호
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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.