• Natural Product Sciences
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• 제17권3호
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• pp.198-201
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• 2011

Tyrosinase is one of the important enzymes in the mammalian melanin synthesis. In the process of melanin synthesis, tyrosine is oxidized to DOPA (3,4-dihydroxyphenylalanine), and DOPA is further oxidized to dopaquinone. Tyrosinase is an enzyme catalyzing this oxidation of tyrosine, so chemicals that inhibit the activity of tyrosinase can be used as skin whitening agents. In this study, we isolated five constituents from the 80% MeOH extract of Morus bombycis cortex by bioactivity-guided fractionation. We performed mushroom tyrosinase inhibition assay. As a result, 7,2',4'-trihydroxyflavanone (1), 2',4',2,4,-tetrahydroxychalcone (2), and oxyresveratrol (3) showed the more potent inhibitory effect compared to kojic acid, a well-known skin whitening agent with antityrosinase effect. Moracinoside M (4) and moracin M-3'-O-${\beta}$-D-glucopyranoside (5) also showed the moderate tyrosinase inhibitory activities.

• 생약학회지
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• 제46권4호
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• pp.315-320
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• 2015

This study was carried out to investigate the effect of ethanolic extract Salicornia herbacea (SHEE) on melanogenesis and mechanism. The SHEE on ${\alpha}$-melanocyte stimulating hormone (${\alpha}$-MSH) induces melanogenesis in B16F10 melanoma cells. The effect of SHEE remarkably decreased protein expression of tyrosinase and tyrosinase relate protein (TRP)-2 increased extracellular signal related kinase (ERK) on ${\alpha}$-MSH 100 nM induced melanogenesis on B16F10 melanoma cells at dose-dependent manner. It has been reported that the activation of ERK reduce melanin synthesis by down-regulating micro-phthalmia-associated transcription fator (MITF). These results sugggest that possibility of extracted korean medicinal herbs as a functional ingredient for whitening cosmetic formula.

• 대한화장품학회지
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• 제24권3호
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• pp.45-50
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• 1998

13 develop an active agent for skin whitening, we examined the inhibitory effects of 285 plant extracts on tyrosinase activity and found some plant extracts have an ability to inhibit tyrosinase activity. Of these plant extracts, ramulus mori extracts showed the highest inhibiting activity on enzyme activity. From these results, we selected ramulus mori as a new active agent for skin whitening. $IC_{50}$/ of this extracts on tyrosinase activity is 12.48$\mu\textrm{g}$/m1. Also, ramulus mori extracts showed inhibitory activity on melanin synthesis in B-16 melanoma cells. We isolated active compound from ramulus mori extracts using various column chromatography and recrystalization and identified its chemical structure using Mass spectroscopy, IR and NMR analysis. So, it is identified as Mulberrin, a maior compound of ramutus mori and turned out that it has potent ability on tyrosinase inhibition. $IC_{50}$/ of this compound for tyrosinase activity is 0.5$\mu\textrm{g}$/ml. Also, this compound showed potent inhibitory activity on melanin synthesis in B-16 melanoma cells. This extracts was turned out to be safe in many safety tests.

• BMB Reports
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• 제46권7호
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• pp.364-369
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• 2013

Endothelin-1 (ET-1) plays an indispensable role in epidermal pigmentation in hyperpigmentary disorders due to a central role in melanogenesis. Nevertheless, precise mechanism involved in ET-1-induced hyperpigmentation is still undefined. Glycoprotein (transmembrane) non-metastatic melanoma protein b (GPNMB) is a key element in melanosome formation. Therefore, we speculated that GPNMB was correlated with ET-1-induced pigmentation. After culturing with ET-1, melanin synthesis was significantly up-regulated, accompanying with increased expression of GPNMB and microphthalmia-associated transcription factor (MITF). Total number of melanosomes and melanin synthesis were sharply reduced via GPNMB-siRNA transfection, indicating ET-1-induced pigmentation by GPNMB-dependent manner. Furthermore, MITF-siRNA transfection strikingly inhibited GPNMB expression and the melanogenesis, and this suppression failed to be alleviated by ET-1 stimulation. All of these results demonstrated that ET-1 can trigger melanogenesis via the MITF-regulated GPNMB pathway. Taken together, these findings will provide a new explanation of how ET-1 induces hyperpigmentation, and possibly supply a new strategy for cosmetic studies.

• 대한화장품학회:학술대회논문집
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• 대한화장품학회 2003년도 IFSCC Conference Proceeding Book II
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• pp.174-183
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• 2003

To obtain effective and safe topical depigmenting agents, we synthesized hydroxybenzoates, alkoxybenzoates, and 3,4,5-trimethoxycinnamate containing a thymol moiety and screened then for high-level inhibitory activity against melanin synthesis. Among them, 5-methyl-2-(methylethyl)phenyl (2Ε)-3-(3,4,5-trimethoxyphenyl)prop-2-enoate (Melasolv)$^{TM}$ 4h, showed the most potent depigmenting effect ($IC_{50}$/ = 10$\mu$M) with low cytotoxicity ($IC_{50}$/ = 200$\mu$M). To find the inhibition mechanism of our candidate, various in vitro tests were performed such as DPPH assay, tyrosinase activity in mushroom or in culture cell and expression of tyrosinase, TRP-l and TRP-2. The result of this study suggested that 4h inhibited melanin synthesis by reducing the expression of tyrosinase and TRP-l at the transcriptional level in melan-a melanocytes.s.

• 약학회지
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• 제57권6호
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• pp.388-393
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• 2013

Previously, we have reported that lovastatin, an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, increased melanin synthesis through intracellular $Ca^{2+}$ release in B16 cells. In this study we investigated the possible involvement of nitric oxide (NO) in the mechanism of lovastatin-induced melanogenesis. Lovastatin elevated NO formation in a dose-dependent manner. Treatment with mevalonate, farnesyl pyrophosphate (FPP) and geranylgeranyl pyrophosphate (GGPP), precursors of cholesterol, did not significantly alter the lovastatin-induced NO production, suggesting that inhibition of cholesterol metabolism may not be involved in the mechanism of this action of lovastatin. Both NO formation and melanogenesis induced by lovastatin was significantly suppressed by treatment with $N^G$-nitro-L-arginine methyl ester (L-NAME) and 2-(4-carboxy-2-phenyl)-4,4,5,5-tetramethylinidazoline-1-oxyl-3-oxide (cPTIO), an inhibitor of NO synthase and a NO scavenger, respectively. The lovastatin-induced NO production was significantly affected not by EGTA, an extracellular $Ca^{2+}$ chelator, but by an intracellular $Ca^{2+}$ chelator (BAPTA/AM) and intracellular $Ca^{2+}$ release blockers (dantrolene and TMB-8). Taken together, these results suggest that lovastatin may induce melanogenesis through NO formation mediated by intracellular $Ca^{2+}$ release in B16 cells. These results further suggest that lovastatin may be a good candidate for the therapeutic application of various hypopigmentation disorders.

• 한국버섯학회지
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• 제19권3호
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• pp.150-159
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• 2021

Anti-melanogenesis and skin anti-wrinkle effects of methanol (ME) and hot water (HE) extracts from the fruiting bodies of Ganoderma applanatum were investigated in this study. The total phenolic contents of the ME and HE of the mushroom were 11.68 and 3.15 ㎍ GAEs/mg, respectively, whereas the total flavonoid contents of the ME and HE were 21.82 and 2.69 ㎍ QEs/mg, respectively. The survival rate of B16-F10 murine melanoma cells treated with 750 ㎍ ME and HE were 83.46% and 85.54%, respectively, thereby suggesting that mushroom extracts were slightly cytotoxic at the tested concentration. The in vitro tyrosinase inhibition by ME (83.15%) and HE (83.44%) was significantly lower than that of kojic acid (99.61%), the positive control, at 2.0 mg/mL. Although the inhibition of cellular melanin synthesis in B16-F10 melanoma cells by 2.0 mg/mL of ME (50.24%) and HE (51.24%) was lower than that of arbutin (64.84%), the inhibition by both ME and HE was higher than 50%. Collagenase inhibition by HE was comparable to 2.0 mg/mL epigallocatechin (EGCG), the positive control; however, elastase inhibition by ME and HE was lower than that of EGCG at the concentration tested. The results showed that the fruiting bodies of G. applanatum had good anti-tyrosinase, good anti-collagenase, and moderate anti-elastase activities, which might be useful for developing novel skin-whitening and anti-wrinkle agents.

• 생명과학회지
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• 제28권8호
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• pp.900-907
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• 2018

본 연구는 화장품 소재로서 미성숙 사과 과피 열수추출물의 가능성을 확인하기 위한 것으로 시료의 항산화, 미백 효과에 대한 생물학적 활성 평가를 수행하였다. 시료의 항산화 평가는 1,1-diphenyl-2-picrylhydrazyl(DPPH) 라디칼 소거능과 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) 양이온 라디칼 소거능으로 확인하였다. 시료의 미백 효과를 평가하기 위해서 멜라노마(B16F10 cell)를 이용해 MTT assay를 통한 샘플의 독성평가, cellular tyrosinase 저해율 측정, 멜라닌 생합성량 측정 및 미백관련 단백질 및 유전자의 발현량을 확인하였다. 그 결과 미숙사과 열수추출물의 $1,000{\mu}g/ml$ 농도에서 DPPH 라디칼 소거능 활성이 77.3%, $ABTS^+$ 라디칼 소거능 활성은 동일농도에서 93.1%로 높은 저해능을 나타내었다. 미백활성 평가결과 미성숙 사과 과피 열수추출물의 농도 $50{\mu}g/ml$에서 tyrosinase 활성 억제 19.8%, 멜라닌 생합성 억제율은 17.3%로 나타냈다. ${\alpha}$-MSH로 유도된 B16F10 세포 내에서 tyrosinase, TRP-1, TRP-2의 단백질 발현은 감소되었고 전사인자 MITF의 활성이 저해되었다. Real- time PCR 실험 결과에서 상위신호단계에 있는 관련 유전자의 발현도 미숙사과 미성숙 사과 과피 열수추출물의 농도가 높아짐에 따라 발현이 낮아지는 것을 확인하였다. 상기 실험 결과로부터 미성숙 사과 과피 열수추출물의 우수한 미백 효능을 확인하였으며 향후 안전한 천연 화장품 원료로 사용될 수 있음을 확인하였다.

• 동의생리병리학회지
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• 제22권6호
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• pp.1444-1448
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• 2008

본 논문은 라벤더 에탄올 추출물이 ${\alpha}$-MSH 유도 멜라닌 생성에 미치는 효과에 관한 것으로 라벤더 추출물이 미백효과에 미치는 연구를 중심으로 한다. 라벤더 에탄올 추출물은 복용 의존적으로 멜라닌 함량과 티로시나아제 활성을 억제했다. 라벤더 에탄올 추출물 처치는 ${\alpha}$-MSH로 촉진된 멜라닌 형성, 티로시나아제 활성, 수상돌기 성장을 효과적으로 억제했고, 라벤더 처치에 의해${\alpha}$-MSH로 유도된 티로시나아제의 mRNA 발현이 유의미하게 감소되었다. 본 연구를 통해 라벤더 추출물이 미백효과가 있음을 알 수 있었으며, 따라서 라벤더가 색소과다침착증에 미백제로 사용될 가능성이 있다는 내용이다.

• 한국식품영양과학회지
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• 제43권5호
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• pp.705-711
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• 2014

피부미백 소재를 개발하기 위해 멜라닌 함량, 세포내 tyrosinase 활성의 측정 및 Western blotting 실험이 수행되었다. 백합(Lilium Oriental Hybrid 'Siberia') 뿌리의 80% 에탄올 추출물로부터 얻은 에틸아세테이트 분획물(R-EA)은 ${\alpha}$-melanocyte stimulating hormone(${\alpha}$-MSH)에 의해 멜라닌 생성이 유도된 B16/F10 흑색종 세포에서 농도 의존적으로 멜라닌 생성을 저해하였다. 정확하게 세포내 tyrosinase 활성과 멜라닌 함량은 에틸아세데이트 분획물 $100{\mu}g/mL$ 처리 시 ${\alpha}$-MSH 단독 처리군에 비해 각각 45%와 74%의 저해율을 보였다. ${\alpha}$-MSH에 의해 멜라닌 생성이 유도된 B16/F10 흑색종 세포에서 단백질 발현양상을 살펴본 결과 TRP-1이 가장 많이 억제된 양상을 확인할 수 있었고 이 결과는 세포내 tyrosinase 활성저해보다 멜라닌 생성저해가 더 많이 일어난 것과 일맥상통하는 것이다. 이를 종합해 볼 때 p-coumaric acid와 resveratrol 함량이 백합뿌리의 에탄올 추출물에 비해 많이 함유된 에틸아세테이트 분획물은 멜라닌 생성 유도물질에 의해 촉진된 ERK의 활성화를 억제하는 피부미백 소재로서 그 가치가 입증된다고 사료된다.