• 대한화장품학회지
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• 제36권3호
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• pp.233-240
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• 2010

신규 미백 소재 개발을 위하여 tyrosinase의 활성을 억제하는 천연물과, alpha-melanocyte stimulating hormone ($\alpha$-MSH)을 저해하는 펩타이드를 결합한 소재를 고체상 합성법으로 제조하였다[1,2]. Tyrosinase 활성 억제 효능이 있는 천연유래물질을 기존 연구를 바탕으로 선정하였으며, 이중에서 상업화 된 물질 17종에 대해 Mushroom Tyrosinase 활성 억제 효과를 측정하여, 그 중 caffeic acid, coumaric acid를 선별하였다. 펩타이드는 $\alpha$-MSH 분비를 억제하며, tyrosinase활성을 억제하는 것으로 알려진 melanostatin을 선정하였으며[3-5], PLG-$NH_2$ (Proline-Leucine-Glycine-$NH_2$) 중에서 유도체화 수율의 저하 원인으로 예상되는 Proline (Pro)의 서열을 다른 아미노산으로 변경하면서 선별된 천연물인 coumaric acid와 caffeic acid에 도입하였다. 또한 최종물질의 원가를 고려하여 acid-amide 형태를 acid형태로 전환한 유도체를 합성하였다. 이들 펩타이드 유도체들에 대해서 B16F1 melanoma cell에서의 멜라닌 생성 억제 효능을 평가하여 유도체화된 물질이 기존의 천연유래물질이나 펩타이드에 비하여 높은 저해효과를 가지는 것을 확인하였다.

• KSBB Journal
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• 제32권3호
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• pp.187-192
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• 2017

In this study, we investigated the effect of Rumex axetosella, Sonchus oleraceus and Euphoibia jolkini extracts on tyrosinase activity and melanin production as natural products of whitening functional cosmetics. To measure the melanin production, 50, 100, $200{\mu}g/mL$ of Rumex axetosella, Sonchus oleraceus and Euphoibia jolkini extracts were treated on ${\alpha}-MSH$ treated B16F10 melanoma cells, respectively. Melanin contents in ${\alpha}-MSH$ treated B16F10 melanoma cells were decreased by 41.5, 51.11, and 61% in $200{\mu}g/mL$ treatment compared to none treatment, respectively. In addition, the intracellular tyrosinase activity was decreased after treatments with all extracts. Furthermore, $100{\mu}g/mL$ of Euphoibia jolkini extract was decreased 81.5% of melanin production in B16F10 melanoma cells. When the three extracts were compared, Euphoibia jolkini extract was considered to be the most functional material for whitening effect.

• 동의생리병리학회지
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• 제21권5호
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• pp.1142-1147
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• 2007

In this study, we investigated the effects of the flowers of Lespedeza bicolor on melanogenesis in a mouse melanocyte cell line, B16/F10 cells. Our results show that the flowers of Lespedeza bicolor significantly inhibits melanin synthesis in concentration-dependent manner. In addition, it was also found to inhibit the activity of tyrosinase, the rate-limiting melanogenic enzyme. While the flowers of Lespedeza bicolor have no direct inhibitory effect on tyrosinase activity in cell free assay system using mushroom tyrosinase. Moreover, the flowers of Lespedeza bicolor effectively suppressed the ${\alpha}-MSH-stimulated$ melanin formation, tyrosinase activity and dendrite outgrowth. These results suggest that the flowers of Lespedeza bicolor is a potent depigmetation agent.

• 한국자원식물학회:학술대회논문집
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• 한국자원식물학회 2022년도 추계학술대회
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• pp.118-118
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• 2022

Carex pumila Thunb. is a plant native to East Asia, Australia, and New Zealand. However, its effect on skin melanogenesis has not been investigated. In the present study, we evaluated its anti-melanogenic properties using B16F10 melanoma cells and zebrafish larvae in the presence or absence of α-melanocyte stimulating hormone (α-MSH). In this study we revealed that concentrations below 50 µg/mL did not induce any cytotoxicity in B16F10 melanoma cells and cardiotoxicity in zebrafish larvae. However, 50 µg/mL treatment significantly inhibited α-MSH-induced extracellular (from 181.24% α 0.62% to 105.15% α 0.31%) and intracellular melanin contents (from 119.8% α 1.2% to 53.4% α 1.7%) as well as intracellular tyrosinase activity (from 143.9% α 4.2% to 103.7% α 1.4%) in B16F10 melanoma cells. At 25 µg/mL and 50 µg/mL concentrations, it could significantly inhibit α-MSH induced hyperpigmentation in zebrafish larvae (from 100% α 2.3% to 60.7% α 1.3% and 47.5% α 1.9% respectively). Additionally, the extract suppressed α-MSH-induced cAMP-CREB-MITF signaling pathway and consequently inhibited tyrosinase expression in B16F10 melanoma cells. In conclusion, our results indicate that this plant extract could suppress the cAMP-CREB-MITF axis which consequently inhibits tyrosinase mediated melanogenesis.

• 한방안이비인후피부과학회지
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• 제26권1호
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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.

• 한국식품영양과학회지
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• 제46권1호
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• pp.34-38
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• 2017

본 연구는 바위수염 메탄올 추출물이 천연 미백 소재로의 가능성을 알아보기 위해 멜라닌 함량, 세포 내 tyrosinase 활성 측정 및 단백질 발현 실험이 수행되었다. 바위수염 메탄올 추출물의 농도에 따른 MTT assay를 통해 세포 생존율 및 증식에 큰 영향을 미치지 않는 $500{\mu}g/mL$ 농도까지를 실험 조건으로 설정하였다. B16F10 melanoma cell의 멜라닌 생성에 미치는 영향을 측정한 결과 대조군에 비하여 ${\alpha}-MSH$만 처리한 경우 뚜렷하게 증가하였고, 바위수염 메탄올 추출물을 100, 300, $500{\mu}g/mL$의 농도로 각각 처리한 결과 ${\alpha}-MSH$만을 처리한 것과 비교해 27%, 41%, 59%로 농도 의존적으로 감소하였다. Tyrosinase 활성도 마찬가지로 바위수염 메탄올 추출물을 100, 300, $500{\mu}g/mL$의 농도로 각각 처리한 결과 ${\alpha}-MSH$만을 처리한 것과 비교해 18%, 49%, 61%로 농도 의존적으로 감소하는 것으로 나타났다. 바위수염 메탄올 추출물이 멜라닌 합성 관련 단백질 발현에 대한 영향을 확인하기 위하여 western blot으로 미백관련 전사인자인 MITF, TRP-1, TRP-2, tyrosinase 발현을 조사하였다. ${\alpha}-MSH$를 단독 처리한 경우에 각 단백질의 발현이 현저하게 증가하는 것을 확인할 수 있었으나, 바위수염 메탄올 추출물을 처리한 경우 농도 의존적으로 감소하는 것으로 나타났으며, 특히 $500{\mu}g/mL$의 농도에서 매우 효과적으로 억제되었다. 이상의 결과로부터 바위수염 추출물은 멜라닌 생합성에 있어서 상위신호단계에 있는 전사인자 MITF의 활성을 억제한다고 보고, 향후 미백 기능성 화장품 소재로서 활용할 수 있을 것으로 사료된다.

• 한방안이비인후피부과학회지
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• 제16권1호
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• pp.100-111
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• 2003

Recently many efforts were focused to understand the mechanical insights of melanogenesis to develop the agents for hyper-pigmentation and hypo-pigmentation. In the melanin biosynthetic pathway, tyrosinase is the rate limiting enzyme, and ${\alpha}$-melanocyte stimulating hormone(MSH) or cAMP-elevating agents stimulate melanogenesis and enhance the melanin synthesis and the tyrosinase activity. The author has analyzed the effects of Rhizoma Bletillae on the basal melanogenic activities of B16 mouse melanoma cells. Rhizoma Bletillae alone markedly suppressed melanin content and tyrosinase activity in a dose-dependent manner. Pretreatment of the cells with Rhizoma Bletillae. The decrease in the tyrosinase activity was paralled by a decrease in the abundance of tyrosinase protein and tyrosinase promoter activity. These results suggest that Rhizoma Bletillae inhibits melanogenesis of B16 melanoma cells via suppression of tyrosinase activity.

• 대한화장품학회지
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• 제38권1호
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• pp.67-73
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• 2012

본 연구에서는 B16 악성흑색종 세포에서 디펩타이드(dipeptide)의 멜라닌생성 저해 효과를 연구하였다. 실험결과 WV (트립토판-발린), WM (트립토판-메치오닌), CQ (시스테인-글루타민)는 멜라닌 생성을 농도 의존적으로 감소시켰다. 그러나 디펩타이드는 멜라닌 생합성과정의 속도 조절 단계 효소인 타이로시네이즈(tyrosinase)의 활성을 직접 감소시키지는 않았다. 따라서 타이로시네이즈의 발현양상을 조사하였고, 실험 결과 ${\alpha}$-MSH가 유도한 타이로시네이즈 발현이 WV, WM, 그리고 CQ에 의해 억제되었다. 그러므로 WV, WM, 그리고 CQ가 타이로시네이즈의 억제성 조절(down-regulation)을 통해 멜라닌 생성을 감소시킨다고 제안될 수 있다.

• 생약학회지
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• 제45권3호
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• pp.262-267
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• 2014

Royal jelly composes of many components, especially protein. Protein is a major factor which cause allergy. We focused on water soluble royal jelly (WSRJ) that was removed allergy - inducing protein. 10-hyroxy-2-decenoic acid content of WSRJ is 2.42 g/100 g, which is double compared to that of lypophilized RJ. To further access WSRJ as a cosmetic ingredient and potential external treatment for topical use, we investigated its ability to inhibit tyrosinase activity and melanin biosynthesis on melanogenesis in B16F1 melanoma cells. We found that WSRJ increased the cell viability in B16F1 melanoma cell and WSRJ (1~10 mg/ml) inhibited melanin synthesis in with 10 nM ${\alpha}$-melanocyte-stimulating hormone (${\alpha}$-MSH) for 48 h. WSRJ inhibited direct tyrosinase activity, which decreased melanin synthesis in ${\alpha}$-MSH stimulated B16F1 melanoma cells. Thease findings suggest that WSRJ induces the down regulation of melanogenesis by inhibiting tyrosinase activation.

• 한국자원식물학회:학술대회논문집
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• 한국자원식물학회 2019년도 추계학술대회
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• pp.90-90
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• 2019

Hibiscus syriacus exhibited promising potential as a new source of food and colorants containing various anthocyanins. However, the function of anthocyanins from H. syriacus has not been investigated. In the current study, we evaluated whether anthocyanins from the H. syriacus varieties Pulsae and Paektanshim (PS and PTS) inhibit melanin biogenesis. B16F10 cells and zebrafish larvae were exposed to PS and PTS in the presence or absence of ${\alpha}$-melanocyte-stimulating hormone (${\alpha}$-MSH), and melanin contents accompanied by its regulating genes and proteins were analyzed. PS and PTS moderately downregulated mushroom tyrosinase activity in vitro, but significantly decreased extracellular and intracellular melanin production in B16F10 cells, and inhibited ${\alpha}$-MSH-induced expression of microphthalmia-associated transcription factor (MITF) and tyrosinase. PS and PTS also attenuated pigmentation in ${\alpha}$-MSH-stimulated zebrafish larvae. Furthermore, PS and PTS activated the phosphorylation of extracellular signal-regulated kinase (ERK), whereas PD98059, a specific ERK inhibitor, completely reversed PS- and PTS-mediated anti-melanogenic activity in B16F10 cells and zebrafish larvae, which indicates that PS- and PTS-mediated anti-melanogenic activity is due to ERK activation. Moreover, chromatography data showed that PS and PTS possessed 17 identical anthocyanins as a negative regulator of ERK. These findings suggested that anthocyanins from PS and PTS inhibited melanogenesis in vitro and in vivo by activating the ERK signaling pathway.