• 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.

• 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.

• 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.

• 대한본초학회지
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• 제29권6호
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• pp.157-163
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• 2014

Objectives : Gamisoyo-san complex prescription were made with Angelicae Gigantis Radix, Paeoniae Radix, Atractylodes rhizome white, Hoelen, Bupleuri Radix, Moutan Cortex Radicis, Gardeniae Fructus, Zingiberis Rhizoma Crudus, Menthae Herba. The purpose of this study was to research the whitening effect of the extract from Gamisoyo-san, which is one of the used herbal complex prescription. Methods : This study investigated inhibitory effect of Gamisoyo-san in tyrosinase activity. Cell viability were performed using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay. Then, Gamisoyo-san measured reversed-transcription-PCR for mRNA expression using B16F10 mouse melanoma cells. Results : For whitening effects, the tyrosinase inhibition effect of extract was shown to 52.4% at $5,000{\mu}g/m{\ell}$ concentration. The cell viability on B16F10 melanoma cells of Gamisoyo-san extract showed higher than 75% at $1,000{\mu}g/m{\ell}$ concentration. In this study, an experiment was performed by setting the non-toxic concentration range of 50, 150, $250{\mu}g/m{\ell}$. The Glyceraldehyde-3-phosphate dehydrogenase (GAPDH) was used as a positive control. The microphthalmia-associated transcription factor (MITF), tyrosinase related protein-1 (TRP-1), tyrosinase related protein-2 (TRP-2), tyrosinase mRNA expression inhibitory by reverse transcription-PCR of Gamisoyo-san extract were decreased by 95.3%, 98.8%, 96.3% and 49.5% at $250{\mu}g/m{\ell}$ which the highest concentration. Conclusions : All these findings could verify that whitening effects of Gamisoyo-san extract by tyrosinase inhibitory activity and mRNA expression. The Gamisoyo-san could be used as material for functional cosmetics, such as skin whitening products.

• 대한화장품학회지
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• 제42권1호
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• pp.37-43
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• 2016

바나나잎의 기능성화장품 소재로써 응용 가능성을 규명하고자 바나나잎 추출물이 피부 미백에 미치는 효과를 B16F10 세포주를 활용하여 cell viability, mRNA 발현 및 tyrosinase (Tyr) 활성 저해 실험을 통하여 알아보았다. 10%의 바나나잎 추출물은 tyrosinase 활성을 저해하고, 멜라닌 합성을 65% 감소시키는 것을 확인하였다. 정량적 real-time RT-PCR을 수행한 결과 바나나잎 추출물이 tyrosinase related protein 1 (TRP1) / tyrosinase related protein 2 (TRP2) / tyrosinase mRNA 발현을 각각 20 / 40 / 60% 가량 억제하는 효과를 확인하였다. 또한 바나나잎 추출물이 함유된 크림제형의 임상시험을 수행하여 자외선 조사 직후 바나나잎 추출물이 함유된 크림의 육안평가 결과 유의한 미백효과가 있는 것을 확인하였다. 본 연구 결과는 바나나잎 추출물이 미백 기능성 화장품 소재 뿐 아니라 향후 기전 연구 수행을 통해 다양한 산업화 소재로 개발될 수 있음을 시사한다.

• Applied Microscopy
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• 제41권3호
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• pp.169-177
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• 2011

홍차 열수추출물의 멜라닌 합성 저해능과 작용기전을 알아보기 위해 in vitro 실험으로 항산화능을 확인한 후, melan-a 세포를 사용하여 멜라닌 합성 저해능, tyrosinase 활성 저해능 및 발현저해능 등에 대한 실험을 실시하여 다음과 같은 결과를 얻었다.(1) 항산화능 실험에서 홍차 열수추출물의 총 폴리페놀 및 플라보노이드 함량은 각각 102, 87 mg/g으로 양성대조군인 알부틴(25, 11 mg/g)보다 높았고, 전자공여능 역시 800 ${\mu}g$/mL에서 82%로 알부틴(48%)보다 높았다. (2) Melan-a 세포 실험에서 홍차 열수추출물은 수지상돌기의 발달과 멜라닌 생합성을 효과적으로 저해하였고, 멜라닌 합성 저해능과 tyrosinase 활성 저해능이 알부틴보다 유의하게 (p<0.001) 높았다. (3) Tyrosinase 단백질 발현 저해능 실험에서 알부틴은 발현에 유의한 영향을 미치지 않은 반면, 홍차 열수추출물은 발현을 유의하게 (p<0.001) 저해하였다. (4) 유전자 발현 저해능 실험에서 알부틴과 홍차 열수추출물 모두 tyrosinase, TRP-1과 TRP-2의 mRNA 발현에 영향을 미치지 않았다. 본 연구를 통하여, 홍차 열수추출물은 우수한 항산화능과 함께 멜라닌 합성 저해능을 확인하였으며, 이는 tyrosinase의 생합성을 저해시키기 보다는 tyrosinase 단백질 발현량을 줄이고 tyrosinase 활성을 감소시킴으로써 멜라닌 합성을 저해시키는 것으로 사료된다.

• 생명과학회지
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• 제32권5호
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• pp.355-361
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• 2022

멜라닌 색소는 피부색의 주요 원인이다. 멜라닌 색소는 멜라닌 세포에서 생성된 다음 각질 세포로 전달되어 결국 피부 표면에 다양한 색상을 부여한다. 많은 탈색제 및 피부 미백제가 개발되었지만, 색소 침착을 감소시키기 위한 재료에 대한 수요는 여전히 증가하고 있다. 본 연구에서 천연 화합물을 사용하여 탈색 및 피부 미백에 대한 재료를 찾으려고 시도한 결과 겨우살이(Viscum album var. coloratum) 추출물이 색소 침착을 억제할 수 있음을 발견하였다. 인간 멜라닌 세포에 겨우살이 추출물(mistletoe extracts, ME)을 처리했을 때 색소 침착이 극적으로 감소하였다. 프로모터 리포터 분석은 ME 처리가 HM3KO 흑색종 세포에서 microphthalmia-associated transcription factor (MITF), melanophilin (MLPH), tyrosinase related protein 2 (TRP-2), and tyrosinase (TYR) 유전자의 전사를 억제한다는 것을 보여주었다. 일관되게 ME는 MITF, TRP-1 및 TYR과 같은 색소 침착 관련 분자의 단백질 수준을 감소시켰다. 또한 ME는 cAMP Responsive Element Binding Protein (CREB), AKT 및 ERK의 인산화를 감소시켰다. 이러한 결과는 ME가 색소 침착과 관련된 세포 내 신호 전달의 조절을 통해 멜라닌 생성을 억제한다는 것을 시사한다. 끝으로 ME는 색소 침착에 대한 생체 내 평가 모델인 제브라피쉬 배아의 멜라닌 생성을 현저하게 억제하였다.

• 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.

• 한국약용작물학회지
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• 제22권5호
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• pp.331-338
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• 2014

Dendrobium moniliforme (DM) is a valuable and versatile herbal medicine with the anecdotal claims of antioxidant and anti-inflammation. In the present study, we investigated the whitening and anti-wrinkling effects of DM under various conditions with B16F10 melanoma cells and human dermal fibroblasts. The DM extract inhibited melanin contents and tyrosinase activity in a dose-dependent manner, compared with untreated group. Treatment of the DM extract effectively suppressed the ${\alpha}$-MSH-stimulated melanin formation, tyrosinase activity and dendrite outgrowth. Moreover, the ${\alpha}$-MSH-induced mRNA expressions of tyrosinase-related protein-1 (TRP-1) and tyrosinase-related protein-2 (TRP-2) and protein expression of tyrosinase were significantly attenuated by DM treatment. We also investigated the DM increased the production of type I procollagen and inhibited TNF-${\alpha}$-induced mRNA expressions of MMP-1, -3 in the human dermal fibroblast. These results indicate that DM may be a great cosmeceutical ingredient for its whitening and anti-wrinkle effects.

• 한국약용작물학회지
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• 제23권4호
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• pp.298-304
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• 2015

Dendrobium loddigesii (DL) is a valuable and versatile herbal medicine with the anecdotal claims of anti-oxidant and anti-inflammation. In the present study, we investigated the whitening effects of DL under various conditions with B16F10 melanoma cells. The DL extract inhibited melanin contents and tyrosinase activity in a dose-dependent manner, compared with untreated group. Treatment of the DL extract effectively suppressed the ${\alpha}$-MSH-stimulated melanin formation, tyrosinase activity and dendrite outgrowth. Moreover, the ${\alpha}$-MSH-induced mRNA expressions of tyrosinase-related protein-1 (TRP-1), tyrosinase-related protein-2 (TRP-2), microphthalmia-associated transcription factor (MITF) and protein expression of tyrosinase were significantly attenuated by DL treatment. These results indicate that DL may be a great cosmeceutical ingredient for its whitening effects.