• 동의생리병리학회지
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• 제22권2호
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• pp.371-376
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• 2008

In this study, we have investigated the hypo-pigmentary mechanism of methanol extract of Forsythiae Fructus in human melanocyte cell line, HM3KO. Treatment of HM3KO cells with Forsythiae Fructus extract markedly inhibited melanin biosynthesis in a dose-dependent manner. Decreased melanin contents occurred through the decrease of tyrosinase protein and activity. The mRNA levels of tyrosinase and tyrosinase-related protein 1 (TRP-1) were also reduced by Forsythiae Fructus extract. Moreover, the level of intracellular cyclic AMP (cAMP) was significantly decreased by treatment of Forsythiae Fructus extract. These results suggest that Forsythiae Fructus reduces melanin synthesis by down regulation of tyrosinase mRNA transcription, and this is closely related to the cAMP-dependent pathway.

• 동의생리병리학회지
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• 제30권1호
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• pp.47-53
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• 2016

Kaempferia galanga L. is one of the plants in Zingiberaceae family. It is used by people in many regions of Asia and Africa for relieving toothache, abdominal pain, muscular swelling and rheumatism. Tyrosinase is a key enzyme for melanogenesis, and hyperpigmentation is associated with abnomal accumulation of melanin pigment. This study aimed to investigate the inhibition of melanogenesis by hexane extract of Kaempferia galanga L. (HKG) in B16F10 melanoma cells. Cell-free tyrosinase, melanin contents, intracellular tyrosinase activity and western blot analysis were performed to elucidate the effects on anti-melanogenesis. Cytotoxicity of the extracts was measured using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay and determined the concentration of 12.5, 25 μg/ml. HKG significantly inhibited to activities of intracellular tyrosinase and melanin synthesis in the absence or presence of α-melanocyte stimulating hormone (α-MSH) with dose-dependent manner. And HKG inhibited the expression of tyrosinase, tyrosinase-related protein 1 (TRP-1) and tyrosinase-related protein 2 (TRP-2), regardless of the presence or absence of α-MSH. HKG also down-regulated phosphorylation of p38 and JNK, and up-regulated phosphorylation of Akt. These effects were not related to its cytotoxicity action. These results indicate that HKG has the potential to be a useful therapeutic agent for treating hyperpigmentation disorders and as a beneficial additive in whitening agents in cosmetics industry.

• 한국자원식물학회지
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• 제29권2호
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• pp.155-162
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• 2016

본 연구에서는 Dendrobium speciosum 에탄올추출물의 티로시나아제 억제를 통한 멜라닌형성 저해 효과 및 주름개선효과에 대해 연구하였다. Dendrobium speciosum추출물은 α-MSH만 처리한 군에 비해 티로시나아제 활성을 농도 의존적으로 저해시킴으로서 멜라닌 함량을 감소시켰다. 더 자세한 메카니즘을 알아보기 위하여 멜라닌 합성 관련 유전자인 Tyrosinase-related protein-1, tyrosinase-related protein-2, Microphthalmia-associated transcription factor 발현을 확인하였을 때 Dendrobium speciosum처리군에서 유전자 발현이 농도 의존적으로 감소하였다. 또한 Dendrobium speciosum처리 시 type I procollagen 합성이 증가함으로써 Dendrobium speciosum처리가 collagen 생합성을 증대시킬 것으로 사료된다. 이 결과를 바탕으로 Dendrobium speciosum에탄올 추출물 처리 시 멜라닌합성 관련 유전자의 발현 및 티로시나아제 활성을 저해시켜 멜라닌 합성이 감소됨에 따라 효과적인 미백활성을 가지며 collagen합성을 증대시킴으로서 주름개선에 탁월한 효과를 가지는 것으로 사료되며 이는 기능성 화장품 소재로 사용가능할 것으로 사료된다.

• Natural Product Sciences
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• 제17권1호
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• pp.26-32
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• 2011

Novel tyrosinase inhibitors are important for pigmentation in the skin. Following extraction of tyrosinase inhibitors from edible vegetables or fruits, we found that the Prunus persica flesh extract (PPFE) exhibited potential inhibitory activity for melanogenesis. PPFE showed tyrosinase inhibitory activity in an enzymatic assay and PPFE also significantly inhibited the melanin formation in cultured mouse melan-a cells. Moreover, real-time RT-PCR analysis revealed that the inhibition of melanin production by PPFE was closely related to marked suppression of mRNA expression of tyrosinase and tyrosinase-related protein-1 and -2 (TRP-1 and TRP-2) in melan-a cells. Further investigation found that the modulation of tyrosinase expression by PPFE was associated with the transcriptional regulation of the microphthalmia-associated transcription factor (MITF). PPFE inhibited the promoter activity of MITF and suppressed MITF mRNA expression in melan-a cells. These results indicate that PPFE down-regulates melanogenesis-associated gene expression through MITF-mediated transcriptional regulation and these events might be related to the hypopigmentary effects of PPFE.

• 생명과학회지
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• 제29권11호
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• pp.1192-1199
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• 2019

본 연구는 화장품 소재로서 우절 에탄올추출물의 가능성을 확인하기 위한 것이다. 이를 위해 우리는 연근의 마디부분을 70%에탄올로 추출하여 사용하였으며 미백효능 및 주름개선 효과에 대한 생물학적 활성 평가를 수행하였다. 시료의 미백활성을 알아보기 위해 멜라닌세포(B16F10 cells)의 MTT assay를 이용한 샘플의 독성평가와 멜라닌 생성에 영향을 주는 관련 단백질의 발현량을 확인하였다. 시료의 주름활성억제 평가를 위해 collagenase inhibition assay를 수행하였다. 또한 UVB로 유도된 섬유아세포(CCD-986sk cells)의 MTT assay를 이용한 샘플의 독성평가와 matrix metalloprotease (MMP-1) inhibition 및 procollagen synthesis를 평가하였다. 미백활성 평가를 알아보기 위한 western bolt 결과, 멜라닌 생성과 관련된 두 단백질 Tyrosinase related protein-1 (TRP-1, Tyrosinase related protein-2 TRP-2)의 합성이 농도의존적으로 감소됨을 나타내었다. 게다가 우절 에탄올추출물의 collagenase inhibiion 실험의 결과, $500{\mu}g/ml$의 농도에서 대조군인 EGCG와 효능이 비슷한 80% 이상의 효과를 나타내었다. Procollagen synthesis 결과 UVB 자극군에 의해 콜라겐 합성은 68.8%로 감소되었으며 시료의 $25{\mu}g/ml$의 농도에서 80.2%의 콜라겐 합성에 회복능을 보였다. MMP-1 inhibition 실험결과는 $25{\mu}g/ml$ 농도에서 20.2%의 저해능을 나타내었다. 실험 결과는 NRN의 미백 및 주름 억제 효과를 검증하고, 향후 안전한 천연 화장품 재료로 사용될 수 있음을 확인했다.

• Toxicological Research
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• 제33권1호
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• pp.55-62
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• 2017

We evaluated the antioxidant activity and anti-melanogenic effects of Oenothera laciniata methanol extract (OLME) in vitro by using melan-a cells. The total polyphenol and flavonoid content of OLME was 66.3 and 19.0 mg/g, respectively. The electron-donating ability, 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical-scavenging activity, and superoxide dismutase (SOD)-like activity of OLME ($500{\mu}g/mL$) were 94.5%, 95.6%, and 63.6%, respectively. OLME and arbutin treatment at $50{\mu}g/mL$ significantly decreased melanin content by 35.5% and 14.2%, respectively, compared to control (p < 0.05). OLME and arbutin treatment at $50{\mu}g/mL$ significantly inhibited intra-cellular tyrosinase activity by 22.6% and 12.6%, respectively, compared to control (p < 0.05). OLME ($50{\mu}g/mL$) significantly decreased tyrosinase, tyrosinase-related protein-1 (TRP-1), TRP-2, and microphthalmia-associated transcription factor-M (MITF-M) mRNA expression by 57.1%, 67.3%, 99.0%, and 77.0%, respectively, compared to control (p < 0.05). Arbutin ($50{\mu}g/mL$) significantly decreased tyrosinase, TRP-1, and TRP-2 mRNA expression by 24.2%, 42.9%, and 48.5%, respectively, compared to control (p < 0.05). However, arbutin ($50{\mu}g/mL$) did not affect MITF-M mRNA expression. Taken together, OLME showed a good antioxidant activity and anti-melanogenic effect in melan-a cells that was superior to that of arbutin, a well-known skin-whitening agent. The potential mechanism underlying the anti-melanogenic effect of OLME was inhibition of tyrosinase activity and down-regulation of tyrosinase, TRP-1, TRP-2, and MITF-M mRNA expression.

• Asian-Australasian Journal of Animal Sciences
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• 제26권11호
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• pp.1518-1522
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• 2013

TYR (Tyrosinase) and TYRP1 (Tyrosinase-related protein 1) play crucial roles in determining the coat color of birds. In this paper, we aimed to characterize the relationship of TYR and TYRP1 genes with plumage colors in Korean quails. The SNPs were searched by cDNA sequencing and PCR-SSCP in three plumage color Korean quails (maroon, white and black plumage). Two SNPs ($367T{\rightarrow}C$ and $1153C{\rightarrow}T$) were found in the coding region of TYRP1 gene, but had no significant association with plumage phenotype in Korean quails. The expression of TYR was higher in black plumage quails than that in maroon plumage quails. In contrast, the expression of TYRP1 was lower in black plumage quails than that in maroon plumage quails. This study suggested that the melanic plumage color in Korean quails may be associated with either increased production of TYR or decreased production of TYRP1.

• 생명과학회지
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• 제31권11호
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• pp.1019-1027
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• 2021

천연물에서 피부 미백 효능을 가진 화합물을 개발하기 위한 노력이 많이 이루어지고 있다. 꽃송이 버섯(Sparassis crispa)은 β-glucan의 함량이 건조중량의 40% 이상으로서 항암과 면역증강 효과가 있는 것으로 입증되어 약용으로도 인정받고 있다. 이 연구에서는 S. crispa β-glucan의 멜라닌 생합성 및 tyrosinase 활성억제 효능을 확인함으로써 피부 미백제로서의 활용 가능성을 평가하고자 하였다. 외부 자극제인 α-melanocyte stimulating hormone (α-MSH)와 S. crispa β-glucan (10, 100, 1,000 ㎍/ml)을 B16F1 melanoma 세포에 투여하여 멜라닌 생성량과 tyrosinase 활성도를 측정하였다. Tyrosinase, tyrosinase related protein-1 (TRP-1), TRP-2, microphthalmia-associated transcription factor (MITF)의 발현정도에 대해서는 western blot으로 분석하였다. S. crispa β-glucan을 10, 100, 1,000 ㎍/ml의 농도로 투여하였을 때 α-MSH 만 투여군에 비하여 멜라닌 생성이 각각 13.9%, 18.7%, 39.5% 감소하였다. S. crispa β-glucan을 10, 100, 1,000 ㎍/ml의 농도로 투여하였을 때 β-glucan을 투여하지않은 α-MSH 유도군에 비하여 tyrosinase 활성도는 각각 15.6%, 26.9%, 43.2% 억제되었다. 또한 tyrosinase와 TRP-1, TRP-2, MITF 단백 발현도 효과적으로 감소시켰다. 본 연구 결과에 따르면 S. crispa β-glucan은 MITF 발현을 억제함으로써 tyrosinase 발현을 감소시켜 멜라닌 생성을 억제시킨 것으로 판단된다. 따라서 S. crispa β-glucan은 미백제로서 유용하게 활용할 수 있을 것으로 생각한다.

• 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.

• BMB Reports
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• 제43권7호
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• pp.461-467
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• 2010

Natural products with non-toxic and environmentally friendly properties are good resources for skin-whitening cosmetic agents when compared to artificial synthetic chemicals. Here, we investigated the effect of glyceollin produced to induce disease resistance responses of soybean to specific races of an incompatible pathogen, phytophthora sojae, on melanogenesis and discussed their mechanisms in melanin biosynthesis. We found that glyceollin inhibits melanin synthesis and tyrosinase activity in B16 melanoma cells without cytotoxicity. To elucidate the mechanism of the effect of glyceollin on melanogenesis, we conducted western blot analysis for melanogenic enzymes such as tyrosinase, tyrosinase-related protein-1 (TRP-1), and TRP-2. Glyceollin inhibited tyrosinase and TRP-1 protein expression. Additionally, glyceollin effectively inhibited intracellular cAMP levels in B16 melanoma cells stimulated by $\alpha$-melanocyte stimulating hormone ($\alpha$-MSH). These results suggest that the whitening activity of glyceollin may be due to the inhibition of cAMP involved in the signal pathway of $\alpha$-MSH in B16 melanoma cells.