• 대한화장품학회지
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• 제37권4호
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• pp.319-326
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• 2011

니겔라 사티바(Nigella sativa Linn.) 오일의 미백 효능을 확인하기 위하여 니겔라 사티바 오일 및 오일에서 분리된 유효성분들을 버섯 타이로시네이즈 효소, B16 멜라노마 세포를 이용하여 멜라닌 생성에 관련된 다양한 실험을 실시하였다. B16-F10 멜라노마 세포를 이용한 멜라닌 저해 활성시험 결과에서 니겔라 사티바 오일은 10 mg/mL의 농도에서 약 86 %의 멜라닌 생성을 억제하였으며, RT-PCR과 Western blot을 통한 멜라닌 생성 기작에 대한 영향을 조사한결과, 멜라닌 합성의 주요 단백질인 타이로시네이즈 발현 저해효과가 우수하게 나타났다. 또한, tyrosinase related protein-1 (TRP-1) 및 tyrosinase related protein-2 (TRP-2)의 발현이 억제되는 것을 확인하였다. 따라서, 니겔라 사티바오일은 멜라닌 생합성 저해 효과뿐만 아니라, 멜라닌 합성에 필수적인 효소(타이로시네이즈, TRP-1, TRP-2)의 발현저해를 통해 미백 효과를 나타내는 것으로 확인되었으며, 이에 따라 니겔라 사티바 오일은 멜라닌 생합성을 저해하는미백 소재로 활용할 수 있을 것으로 사료된다.

• The Korean Journal of Physiology and Pharmacology
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• 제18권3호
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• pp.249-254
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• 2014

The purpose of this study is to characterize the effects of KHG26792 (3-(naphthalen-2-yl(propoxy)methyl)azetidine hydrochloride), a potential skin whitening agent, on melanin synthesis and identify the underlying mechanism of action. Our data showed that KHG26792 significantly reduced melanin synthesis in a dose-dependent manner. Additionally, KHG26792 downregulated microphthalmia-associated transcription factor (MITF) and tyrosinase, the rate-limiting enzyme in melanogenesis, although tyrosinase was not inhibited directly. KHG26792 activated extracellular signal-regulated kinase (ERK), whereas an ERK pathway inhibitor, PD98059, rescued KHG26792-induced hypopigmentation. These results suggest that KHG26792 decreases melanin production via ERK activation. Moreover, the hypopigmentary effects of KHG26792 were confirmed in a pigmented skin equivalent model using Cervi cornus Colla (deer antler glue), in which the color of the pigmented artificial skin became lighter after treatment with KHG26792. In summary, our findings suggest that KHG26792 is a novel skin whitening agent.

• KSBB Journal
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• 제28권2호
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• pp.137-145
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• 2013

In order to develop new skin whitening agents, we prepared the $CH_2Cl_2$ layer (NGC) and BuOH layer (NGB) of 75% EtOH extract of the Nelumbinis nucifera Gaertner. We measured their tyrosinase inhibitory activity in vitro and melanin synthesis inhibitory activity in B16-F1 melanoma cells. They did not show inhibitory activity against mushroom tyrosinase but showed melanin synthesis inhibitory activity in a dose-dependent manner. In a melanin synthesis inhibition assay, NGC and NGB suppressed melanin production up to 52% and 46% at a concentration of $100{\mu}g/mL$, respectively. To elucidate the mechanism of the inhibitory effects of NGC and NGB on melanogenesis, we measured the expression of melanogenesis-related proteins by western blot assay. As a result, NGC suppressed the expression of tyrosinase, tyrosinase related protein 1 (TRP-1), tyrosinase related protein 2 (TRP-2), phosphorylated cAMP responsive element binding (p-CREB) protein, and microphthalmia associated transcription factor (MITF). And NGB inhibited the protein expression of tyrosinase and MITF, but had no significant effect on TRP-1, TRP-2, and p-CREB expression. Moreover, NGB increased the expression of phosphorylated extracellular signal-regulated kinase (p-ERK). In addition, we examined the inhibitory effect on the glycosylation of tyrosinase. As a result, NGC and NGB inhibited the activity of ${\alpha}$-glucosidase in vitro and the glycosylation of tyrosinase in B16-F1 melanoma cells. From these results, we concluded that NGC and NGB could be used as active ingredients for skin whitening.

• 한국미생물·생명공학회지
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• 제23권6호
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• pp.641-646
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• 1995

During the screening of inhibitors of melanin biosynthesis from microbial secondary metabolites, a fungal strain MR304 which was capable of producing high level of an inhibitor was selected. Based on taxonomic studies, this fungus could be classified as Trichoderma harzianum. The active compound (MR304-1) was purified from culture broth by Diaion HP-20 column chromatography, ethylacetate extraction, Sephadex LH-20 column chromatographv and HPLC. The inhibitor was identified as 3-(1,5-dihvdroxy-3-isocyanocyclopent-(E)-3-envl)prop-2-enoate by spectroscopic methods of UV, ESIMS, $^{1}$H-NMR, $^{13}$C-NMR, NOE, HMQC and HMBC. MR304-1 showed strong mushroom tyrosinase inhibitory activity with IC$_{50}$ value of 0.25 $\mu $g/ml. It inhibited melanin biosynthesis with 15 mm inhibition zone at 30 $\mu $g/paper disc in Streptomyces bikiniensis, a bacterium used as an indicator organism in this work. It also inhibited melanin biosynthesis in B16 melanoma cells with a niinimum inhibitory concentration of 0.05 $\mu $g/ml.

• 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.

• 대한화장품학회지
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• 제40권1호
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• pp.89-94
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• 2014

물푸레나무 수피 추출물은 주요 생활성 물질로서 esculetin과 esculin을 포함하고 있다. 이 가운데, Esculetin은 B16F10 melanoma cells에서 $IC_{50}$ value $2.8{\mu}M$의 아주 좋은 melanogenesis 억제 활성을 나타내며, 이를 통해 Melan-A cell에서 melanin 합성을 감소시킨다. 더욱이, esculetin은 mushroom tyrosinase에서도 $IC_{50}$ value $40{\mu}M$의 억제 활성을 나타내어 melanin biosynthesis를 저해한다. 위의 결과들로서, 우리는 melanogenic enzyme 활성 조절에 의해 melanin 생성을 저해하는 효과적인 피부미백 물질로서 esculetin을 제안하고자 한다.

• 생약학회지
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• 제39권3호
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• pp.174-178
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• 2008

Melanin is a polymer of phenol which produces hyperpigmentation in the skin. Melanin synthesis is catalyzed by the enzyme tyrosinase. To investigate the whitening activity of the fractions from the ethanol extract of Enteromorpha linza, we studied the inhibitory effect on the tyrosinase activity and melanogenesis in the B16/F1 melanoma cells. The inhibition ratio of tyrosinase activity of ethylacetate fraction from E. linza was as strong as that of kojic acid, a positive control. Also, the melanin production was significantly inhibited by the ethylacetate fraction in a dose dependent manner. The ethylacetate fraction showed the highest activity in the fractions and as strong activity as that of arbutin, a positive control. From these results, we suggest that the E. linza extract might be able to apply to cosmetic and medical fields.

• 약학회지
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• 제58권1호
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• pp.47-52
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• 2014

Clematis mandshurica (Ranunculaceae) has traditionally been used as a remedy for antidiuretic, antifungal, rheumatic conditions and alleviate pain. We carried out to evaluate the anti-oxidative effect, anti-inflammatory effect and anti-melanogenic effect of ethanol extract and solvent fractions of Clematis mandshurica. The ethanol extract and the dichloromethane fraction of Clematis mandshurica showed an anti-oxidative effect in DPPH assay, the inhibitory activity of nitric oxide (NO) production in lipopolysaccharide (LPS) activated RAW 264.7 cell, and melanin synthesis and tyrosinase activity of B16F10 melanoma cells. They reduced NO production and melanin content in a dose-dependent manner at concentrations of $2.5{\sim}10{\mu}g/ml$. They also suppressed iNOS and tyrosinase protein and m-RNA expressions dose dependently, assayed by western blot analysis and RT-PCR experiment.

• 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.

• 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.