• 대한화장품학회지
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• 제23권3호
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• pp.115-121
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• 1997

To identify inhibitors of melanogenesis, we compared the effects of 5 compounds on mushroom tyrosinase, human melanocytic tyrosinase activity and melanin content. The cytotoxicyty of the components were also tested on cultured human melanoctes. Kojic acid showed marked inhibitory effect both on mushroom and human tyrosinase activity. This action of kijic acid is stronger than that of ascorbic acid. Arbutin inhibited human tyrosinase activity of cultured melanocytes although it had slightly inhibitory effect on mushroom tyrosinase activity. Azelaic acid had no effect on human tyrosinase activity. Melanin production was inhibited significantly by kojic acid and tranexamic acid. MTT assay showed that all of the compounds were non-cytotoxic to melanocytes at the concentrations tested. These results suggest that the effect of kojic acid on cultured meanocytes involve inhibition of tyrosinase activity and melanogenesis without affection the cell number.

• Bulletin of the Korean Chemical Society
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• 제33권9호
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• pp.3004-3008
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• 2012

Small molecule conjugated peptides were prepared by solid-phase synthesis as potential novel whitening agents, and their melanogenesis inhibitory activities were investigated. The conjugated small molecules were well-known materials as tyrosinase inhibitors, and peptides were selected from the sequences that are known to antagonize melanocortin receptor 1 (MC1R). Most of small molecules-peptide conjugates showed superior melanin inhibition activity to kojic acid and arbutin. Among these, almost all compounds have -AR- sequence. From this study, we concluded that the small molecule conjugated peptides containing -AR- sequence have melanogenesis inhibitory activities and have potential to be used as novel whitening agents.

• Journal of Microbiology and Biotechnology
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• 제30권5호
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• pp.749-752
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• 2020

In the search for novel, natural melanogenesis inhibitors, a new sesquiterpene, inularin, was isolated from the flowers of Inula britannica, and the structure was determined using spectroscopic and chemical methods. The antimelanogenic effects of inularin on B16F10 melanoma cells and zebrafish embryos were evaluated. Inularin dose-dependently reduced melanocyte-stimulating hormone-induced melanin production and L-DOPA oxidation in B16F10 cells. Zebrafish embryos were used to confirm the antimelanogenic activity. Inularin significantly decreased the pigmentation of embryos compared with untreated controls.

• 생약학회지
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• 제33권4호통권131호
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• pp.399-403
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• 2002

국내외의 각종 피부관련 약재를 중심으로 천연물 data-base를 구축하고, 이로부터 피부 미백에 효과가 있다고 언급된 한방 약재를 추출, 용매 분획하여 얻은 분획물들을 B16 melanoma cell assay를 이용하여 미백 효과를 평가하였다. 이들 중 특히 미백효과가 우수한 여로(藜蘆, Veratrum nigrum L.)의 뿌리를 대상으로 성분연구하여 3개의 미백유효성분인 (3S,20S,25S)-22,26-iminocholesta-5,22(N)-dien-3-ol (verazine), (3S,20R,25S)-22,26-iminocholesta-5,22(N)-dien-3-ol (epi-verazine) and (3R,23R)-14,15,16,17-tetradehydroveratraman-3,23,diol (veratramine)을 분리, 구조분석하였다. 여로로부터 분리된 3종의 미백 유효성분은 흑화 작용의 주요 효소인 tyrosinase에 대한 작용은 확인할수 없었으나, B16 F1 mouse melanoma에 대한 멜라닌 합성 억제능은 $IC_{50}<1\;{\mu}g/ml$로 강하게 나타났다. 또한 이와 같은 강한 멜라닌 합성 저해능을 갖는 이들 물질들의 안전성 확인을 통하여 향후 새로운 미백물질로 이용될 수 있을것으로 사료된다.

• The Korean Journal of Physiology and Pharmacology
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• 제21권3호
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• pp.287-292
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• 2017

Vitiligo is an intriguing depigmentary disorder and is notoriously difficult to be treated. The ultimate goal of vitiligo treatment is to replenish the lost melanocytes by immigration from hair follicle and to restore the normal function of melanogenesis by residual melanocytes. There are two types of topical calcineurin inhibitors called tacrolimus and pimecrolimus, and are recommended as the first-line treatments in vitiligo. Although pimecrolimus is efficacious for the repigmentation of vitiligo, its intrinsic mechanisms have never been investigated in vitro. This research aimed to study the ability of pimecrolimus on stimulating melanogenesis, melanocyte migration and MITF (microphthalmia associated transcription factor) protein expression. Results showed that pimecrolimus at the dosages of 1, 10, $10^2$nM were neither mitogenic nor cytotoxic to melanocytes. The addition of pimecrolimus at 10, $10^2$ and $10^3nM$ significantly increased intracellular tyrosinase activity, which was consistent with the elevated content of melanin content at the same concentrations. The peak effect was seen at 72 h in response to $10^2$nM pimecrolimus. Results of the wound scratch assay and Transwell assays indicate that pimecrolimus is effective in facilitating melanocyte migration on a collagen IV-coated surface. In addition, MITF protein yield reached the highest by pimecrolimus at $10^2nM$. In brief, pimecrolimus enhances melanin synthesis as well as promotes migration of melanocytes directly, possibly via their effects on MITF protein expression.

• 대한약학회:학술대회논문집
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• 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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• pp.321.1-321.1
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• 2002

To indentify inhibitors of melanogenesis. we compared the effect of some natural products on mushroom tyrosinase. human melanocytic tyrosinase activity and melanin content. The cytotoxicity of the component were also tested on cultured mouse melanoma cells, Each extract significantly inhibited tyrosinase activity and melanin synthesis in vitro and B 16 melanoma cell lines. In B 16 cell lines, watermelon's inner shell extract inhibited tyrosinase activity as strong as kojic acid at 150${\um}g$/${\mu}\ell$ concentration. And morning glory'seed extract inhibited melanin synthesis more than kojic acid at 150${\um}g$/${\mu}\ell$ concentration. Each extract were strong inhibitors of tyrosinase activity and total melanin synthesis in B 16 mouse melanoma cell lines at less than 100${\um}g$/${\mu}\ell$ concetration. These result show that extract of watermelon's inner shell. lettuce. morning glory's seed and licorice root could be developed as skin whitening component of cosmetics.

• 생약학회지
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• 제31권2호
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• pp.168-173
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• 2000

Two diterpenes and one new sucrose isovaleryl ester having inhibitory effects on melanogenesis in B16 mouse melanoma were isolated from Euphorbiae Lathyridis Semen which has been used in traditional medicine for cancer, tumors and warts. New sucrose isovaleryl ester was identified as ${\alpha}-D-glucopyranoside$, $3,4,6-tris-O-(3-methyl-l-oxobutyl)-{\beta}-D-fructofuranosyl$, 2,6-bis(3-methylbutanoate) and two diterpenes were identified as ingenol-20-palmitate and 5,10-diacetyl-3-benzoyllathyrol$(Euphorbia\;factor\;L_3)$ from their spectral data.

• The Korean Journal of Physiology and Pharmacology
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• 제24권2호
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• pp.149-156
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• 2020

Sodium 2-mercaptoethanesulfonate (mesna) is a protective agent that is widely used in medicine because of its antioxidant effects. Recently, reactive oxygen species (ROS) were shown to increase pigmentation. Thus, ROS scavengers and inhibitors of ROS production may suppress melanogenesis. Forkhead box-O3a (FoxO3a) is an antimelanogenic factor that mediates ROS-induced skin pigmentation. In this study, we aimed to investigate the whitening effect of mesna and the signaling mechanism mediating this effect. Human melanoma (MNT-1) cells were used in this study. mRNA and protein expression were measured by real-time quantitative PCR and Western blotting analysis to track changes in FoxO3a-related signals induced by mesna. An immunofluorescence assay was performed to determine the nuclear translocation of FoxO3a. When MNT-1 melanoma cells were treated with mesna, melanin production and secretion decreased. These effects were accompanied by increases in FoxO3a activation and nuclear translocation, resulting in downregulation of four master genes of melanogenesis: MITF, TYR, TRP1, and TRP2. We found that mesna, an antioxidant and radical scavenger, suppresses melanin production and may therefore be a useful agent for the clinical treatment of hyperpigmentation disorders.

• 치위생과학회지
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• 제4권2호
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• pp.81-84
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• 2004

천연물로부터 치은에 생성되는 멜라닌의 양을 효과적으로 조절하여 치은 미백을 목표로 하는 물질을 분리하고자 문헌에 소개되고 있는 미백 효과를 가진 전통한약을 비롯하여, 민간에서 사용되고 있는 약 100여 종의 고등식물을 대상으로 B-16 mouse melanoma cell lines에서 melanin 생성 억제 효과를 screening하였다. 그 결과 천궁의 methylene chloride 분획에서 활성을 나타내어 실험재료로 선택하여 2개의 화합물을 분리하였으며 각종 spectral data를 검토하여 linoleic acid methyl ester(1), 1,3-dilinoleoyl-2-stearoyl glycerol(2)로 구조를 규명하였다. 이들 화합물은 B-16 mouse melanoma cell lines에서의 melanin 생성억제 활성을 Kojic acid를 비교 물질로하여 측정하였다. 2종의 화합물 중 1,3-dilinoleoyl-2-stearoyl glycerol은 높은 활성을 보이지 않았으나 linoleic acid methyl ester는 Kojic acid에 비하여 강한 활성을 나타내었다.

• 한국균학회지
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• 제38권2호
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• pp.167-171
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• 2010

The present study aims to evaluate Cordyceps militaris water extract (CMWE) with a view to develop melanogenesis inhibitors. Inhibitory activities of CMWE against tyrosinase, L-DOPA(L-3,4-dihydroxyphenylalanine) oxidation, and melanin biosynthesis in B16 mouse melanoma cells were investigated. CMWE, at $5000\;{\mu}g/ml$, inhibited tyrosinase activity of 71% and DOPA oxidation of 40% as reacting with L-DOPA. Furthermore, B16 mouse melanoma cell survived over 50% from low to high dose on MTT assay, and CMWE markedly inhibited (> 50%) melanin synthesis at $5000\;{\mu}g/ml$. The inhibitory effect of CMWE on melanogenesis was attributed to enhancement of tyrosinase degradation. Key enzyme of melanin biosynthesis is tyrosinase which catalyses a beginning step from tyrosine to DOPA quinine and melanin formation step, respectively. These results indicated that CMWE may be a potential source of novel whitening agents for cosmetic or therapeutic application.