• 한국자원식물학회:학술대회논문집
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• 한국자원식물학회 2019년도 춘계학술대회
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• pp.116-116
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• 2019

Thalictrum rochebrunianum var. grandisepalum (TRG) is a Korean endemic plant, and it is widely used for edible, medicinal, landscape materials. In this study, we examined the protein and mRNA expression levels of MITF, tyrosinase, TRP-1 and TRP-2 by TRG extract (TRGE) in IBMX-treated melanocytes to evaluate the possibility of using TRG as a whitening material. IBMX were reported as melanin synthesis enhancers. It could increase intracellular melanin synthesis by activation of the microphthalmia-associated transcription factor (MITF) signaling pathway. TRGE did not show cytotoxicity at concentrations below $100{\mu}g/ml$ in B16F10 cells. TREG dose-dependently inhibited protein and mRNA levels of MITF, tyrosinase, TRP-1 and TRP-2. Therefore, we suggest that TRGE is an important natural resource for cosmetic raw materials for whitening function.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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• pp.90.1-90.1
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• 2003

This study shows that sphingosine-1-phosphate (S1P) significantly inhibits melanin synthesis in a concentration-dependent manner, and that the activity of tyrosinase was also reduced in S1P-treated cells. In contrast, a specific extracellular signal-regulated protein kinase (ERK) pathway inhibitor, PD98059 increased tyrosinase activity and melanin production, and PD98059 restored the reduced tyrosinase activity and pigmentation induced by SIP. We also found that S1P induces the sustained activation of ERK and the subsequent degradation of microphthalmia-associated transcription factor (MITF), which plays a key role in melanogenesis. (omitted)

• 생명과학회지
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• 제33권5호
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• pp.445-454
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• 2023

백발화는 자외선, melanin 세포 자극 호르몬(α-MSH), 줄기 세포 인자 성장인자(SCF), Wnt 및 endothelin-1 (ET-1)에 의하여 활성화되는 melanogenesis를 조절하는 신호 전달 경로가 제대로 작동하지 못하여 나타난 결과이다. 백발화를 예방하기 위하여, tyrosinase, tyrosine hydroxylase, tyrosinase-related protein (TRP)-1, TRP-2 및 microphthalmia-associated transcription factor (MITF)에 의하여 조절되는 melanogenesis를 자극하는 효과적인 합성 및 천연 화합물이 있다. 이러한 화합물은 백발화 예방을 위한 잠재성을 지니고 있다. 이 기사는 melanogenesis와 백발화와 관련된 신호 전달 경로에서 최근의 진전뿐 만 아니라 백발화의 문제를 해결하기 위한 핵심적인 전략에 대해 기술한다. 특히, 이글에서는 catalase 및 methionine sulfoxide reductase를 조절하는 항산화제, resveratrol, fisetin, quercetin 및 ginsenoside와 같은 sirtuin (SIRT) 1 activator와 같은 melanin 생성을 촉진하는 잠재적으로 효과적인 치료제에 대하여 설명한다. 또한 estrogen, androgen, progesterone 및 dihydrotestosterone를 포함하는 telomerase 발현 및 activator 뿐만 아니라, corticosteroids, calcineurin restrainer 및 palmitic acid methyl ester와 같은 백반증 억제제에 대하여 논의한다. 더불어 latanoprost, erlotinib, imatinib, tamoxifen, 및 levodopa와 같은 백발화를 억제할 수 있는 화합물에 대해서도 탐구한다. 결론적으로 이 기사는 모발 백발화와 관련된 melanin 생성을 촉진시키는 화합물에 대한 최근의 연구동향을 고찰한다.

• 동의생리병리학회지
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• 제34권2호
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• pp.67-74
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• 2020

The objective of this study is to investigate the skin whitening and antioxidant effects of the Anemarrhenae Rhizoma extract (ARE). Following the previously studied method, we examined the inhibitory effects of melanin synthesis and tyrosinase activity by using B16F10 cells. First, we measured the Diphenylpicrylhydrazyl (DPPH) assay, nitrite scavenging activity, and superoxide dismutase-like activity to verifying antioxidant efficacy according to skin whitening. In addition, we confirmed the skin whitening efficacy of ARE by measuring gene expression associated with a skin whitening by the Reverse transcription polymerase chain reaction (RT-PCR) method in B16F10 cells. In this study, we confirmed that ARE has skin whitening and antioxidant effects at high concentrations. In particular, ARE at a concentration of 500 ㎍/ml inhibited the expression of Tyrosinase, TRP-2 (tyrosinase-related protein), and MITF (microphthalmia transcription factor) genes better than Arbutin. In conclusion, our results confirmed that ARE has the potential for development as a skin whitening efficacy substance.

• BMB Reports
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• 제43권12호
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• pp.824-829
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• 2010

Melanin synthesis is regulated by melanocyte specific enzymes and related transcription factors. $\beta$-carboline alkaloids including harmaline and harmalol are widely distributed in the environment including several plant families and alcoholic beverages. Presently, melanin content and tyrosinase activity were increased in melanoma cells by harmaline and harmalol in concentration- and time-dependent manners. Increased protein levels of tyrosinase, tyrosinase-related protein-1 (TRP-1), and TRP-2 were also evident. In addition, immunofluorescence and Western blot analyses revealed harmaline and harmalol increased cAMP response element binding protein phosphorylation and microphthalmia-associated transcription factor expression. In addition to studying the signaling that leads to melanogenesis, roles of the p38 MAPK pathways by the harmaline and harmalol were investigated. Harmaline and harmalol induced time-dependent phosphorylation of p38 MAPK. Harmaline and harmalol stimulated melanin synthesis and tyrosinase activity, as well as expression of tyrosinase and TRP-1 and TRP-2 indicating that these harmaline and harmalol induce melanogenesis through p38 MAPK signaling.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 2007년도 Proceedings of The Convention
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• pp.129-139
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• 2007

Many modalities of treatment for acquired skin hyperpigmentation are available including chemical agents or physical therapies, but none are completely satisfactory. The ideal depigmenting compound should have a potent. rapid and selective bleaching effect on hyperactivated melanocytes, carry no short- or long-term side-effects and lead to a permanent removal of undesired pigment. acting at one or more steps of the pigmentation process. Depigmentation can be achieved by regulating (i) the transcription and activity of tyrosinase, tyrosinase related protein-1 (TRP-1), tyrosinase related protein-2 (TRP-2), and/or peroxidase; (ii) the uptake and distribution of melanosomes in recipient keratinocytes and (iii) melanin and melanosome degradation and turnover of pigmented keratinocytes. One of the interesting point for development of skin whitening agent is Mitf(Microphthalmia-associated transcription factor). Mitf belongs to the basic helix-loop-helix-zip family of trabscription factors and it is crucial as it regulates both melanocyte proliferation as well as melanogenesis and is the major regulator of tyrosinase and the related enzymes (TRPs), as well as many melanosome structural proteins such as pMel17. Recently, we developed MITF-down-regulating agents from natural and synthetic sources, which have anti-melanogenic effect on in vitro and in vivo. We suggested that potent MITF-down regulating agents might be used for skin whitening cosmeceuticals.

• Journal of Ginseng Research
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• 제45권5호
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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.

• Journal of Applied Biological Chemistry
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• 제64권4호
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• pp.323-331
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• 2021

Lincomycin is a lincosamide antibiotic isolated from the actinomycete Streptomyces lincolnensis. Moreover, it has been found to be effective against infections caused by Staphylococcus, Streptococcus, and Bacteroides fragillis. To identify the melanin-inducing properties of lincomycin, we used B16F10 melanoma cells in this study. The melanin content and intracellular tyrosinase activity in the cells were increased by lincomycin, without any cytotoxicity. Western blot analysis indicated that the protein expressions of tyrosinase, tyrosinase related protein 1 (TRP1) and TRP2 increased after lincomycin treatment. In addition, lincomycin enhanced the expression of master transcription regulator of melanogenesis, a microphthalmia-associated transcription factor (MITF). Lincomycin also increased the phosphorylation of p38 mitogen-activated protein kinase (MAPK) and decreased the AKT phosphorylation. Moreover, the activation of tyrosinase activity by lincomycin was inhibited by the treatment with SB203580, which is p38 inhibitor. Furthermore, we also found that lincomycin-induced tyrosinase expression was reduced by H-89, a specific protein kinase A (PKA) inhibitor. These results indicate that lincomycin stimulate melanogenesis via MITF activation via p38 MAPK, AKT, and PKA signal pathways. Thus, lincomycin can potentially be used for treatment of hypopigmentation disorders.

• 대한화장품학회지
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• 제37권4호
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• pp.327-335
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• 2011

5,4'-dihydroxystilbene-3-O-D-glucopyranoside (polydatin)는 호장(Polygonum cuspidatum)에 존재하는 stilbenes류의 하나로 지금까지 피부에서의 효능이 잘 알려지지 않았다. 우리는 호장으로부터 Polydatin을 분리하여 얻었으며, 피부유래의 멜라노사이트와 fibroblast를 이용하여 효능을 검증하였다. 실험결과 멜라노사이트에서 polydatin은 타이로시네이즈 활성과 멜라닌 생성을 억제하였고, 멜라닌 생합성 과정에 관여하는 타이로시네이즈와 전사인자인 microphthalmia-associated transcription factor (MITF)의 발현을 억제하는 것을 확인하였다. 미백효과가 확인된 polydatin에 대하여 human fibroblast를 대상으로 type I procollagen 생합성에 미치는 영향을 분석한 결과 polydatin은 농도 의존적 으로 콜라젠 합성을 촉진함을 알 수 있었다. 또한 polydatin의 피부에서의 효능을 검증하기 위해 인체효력시험을 통해 주름개선과 미백개선 효능을 검증하였으며 이를 통해 주름과 미백기능에 있어 유의한 효과를 확인하였다. 이상의 결과로부터 polydatin은 안전한 피부 미백 개선제 및 주름개선제로 사용될 수 있는 후보물질임을 제안하며, 상업적으로 활용하기 위해 원료화를 성공하였다.

• Journal of Applied Biological Chemistry
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• 제54권4호
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• pp.270-278
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• 2011

구기자, 건조구기엽, 생구기엽 추출물의 미백효과를 검증하였다. Tyrosinase 저해활성 측정결과 건조구기엽 에탄올추출물 $500{\mu}g/mL$에서 44%의 저해활성을 나타내었으며, melanoma cell (B16F10)에서의 melanin 생합성 저해율 측정결과 건조구기 엽 에탄올 추출물 $50{\mu}g/mL$에서 14%의 저해효과를 나타내었다. 구기자, 건조구기엽, 생구기엽 추출물을 처리한 B16F10군에서는 tyrosinase protein의 발현이 처리하지 않은 군보다 감소하였다. 특히, 건조구기엽 추출물의 경우 tyrosinase의 단백질 발현량을 많이 저해하였다. 결과적으로 건조구기엽 추출물의 미백활성이 가장 우수하였으며, 식품 및 화장품의 기능성 소재로 이용이 가능할 것으로 판단된다.