• Title/Summary/Keyword: tyrosinase protein

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Inhibitory effect of melanin synthesis using organic solvent extracts from Scolopendra subspinipes mutilans (왕지네의 유기용매 추출물을 이용한 멜라닌 합성 저해효과)

  • Kim, In-Woo;Lee, Joon Ha;Kwon, Yong-Nam;Kim, Sang-Hee;Yun, Eun-Young;Nam, Sung-Hee;Ahn, Mi-Young;Hwang, Jae-Sam
    • Journal of Sericultural and Entomological Science
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    • v.52 no.1
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    • pp.1-5
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    • 2014
  • This study was performed to determine the whitening effect of organic solvent extracts from the centipede, Scolopendra subspinipes mutilans. We prepared different concentrations (50%, 70% and 100%) of ethanol, methanol, 100% ethyl acetate and water extracts. We tested melanin inhibitory effect and tyrosinase activity using B16/F10 melanoma cell. As a result, treatment of organic solvent extracts is decreased the biosynthesis of melanin and tyrosinase activity to 36 ~ 86%. Especially the 70% ethanol extracts was the most effective in B16/F10 melanoma cells. In the study on melanogenic protein expression, 70% ethanol extracts of Scolopendra subspinipes mutilans blocked glycosylation of tyrosinase. Therefore this result suggests that 70% ethanol extracts could be developed as skin whitening agents.

Anti-Oxidative, Anti-Inflammatory, and Anti-Melanogenic Activities of Endlicheria Anomala Extract (Endlicheria anomala (Nees) Mez 추출물의 항산화, 항염증 및 미백 활성)

  • Jin, Kyong-Suk;Lee, Ji Young;Kwon, Hyun Ju;Kim, Byung Woo
    • Microbiology and Biotechnology Letters
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    • v.41 no.4
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    • pp.433-441
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    • 2013
  • In this study, the anti-oxidative, anti-inflammatory, anti-melanogenic activities of Endlicheria anomala (Nees) Mez methanol extract (EAME) were evaluated by use of in vitro assays and cell culture model systems. The results revealed that EAME scavenges various radicals such as 1,1-diphenyl-2-picryl hydrazyl hydrogen peroxide induced reactive oxygen species, and lipopolysaccharide induced nitric oxide. Furthermore, EAME induced the expression of anti-oxidative enzymes such as heme oxygenase 1, thioredoxin reductase 1, NAD(P)H dehydrogenase 1, and their upstream transcription factor, nuclear factor-E2-related factor 2. Moreover, EAME inhibited in vitro DOPA oxidation and 3-isobutyl-1-methylxanthine induced melanogenesis in B16F10 cells. Its anti-melanogenic activity will have originated from the inhibition of tyrosinase enzyme activity and melanogenesis related protein expression. Taken together, these results provide the important new insight that E. anomala possesses various biological activities such as anti-oxidative, anti-inflammatory, and anti-melanogenic. Therefore, it might be utilized as a promising material in the fields of nutraceuticals and cosmetics.

Anti-inflammatory and whitening effects of ginseng complex as a cosmetic material (화장품소재로서의 인삼복합물의 항염증 및 미백효능 검증)

  • Jang, Young-Ah
    • Journal of the Korean Applied Science and Technology
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    • v.35 no.2
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    • pp.325-335
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    • 2018
  • This study is for checking the possibility of ginseng complex as cosmetic materials. For this we carried out biological active evaluation about anti-inflammatory and whitening effects by using ethanol extract of ginseng complex. Samples were prepared by extracting 70% ethanol from each of Panax ginseng C. A. Meyer (A), Phellinus linteus (B) and Pinus rigida Mill. (C), and mixing them at a ratio of (A) 1 : (B) 1 : (C) 0.5. In order to evaluate the anti-inflammatory effects of the samples in macrophages (RAW 264.7 cells), MTT assay was used to evaluate the toxicity of the samples and the inhibitory activity of nitric oxide production and the expression levels of inflammation-related proteins and genes. To evaluate the whitening effect of the samples in melanoma (B16F10 cell), MTT assay was used to evaluate the toxicity of the sample, cellular tyrosinase inhibition, and melanin contents. The inhibitory activity of nitric oxide in the LPS-induced RAW 264.7 cells was 71.2% at $25{\mu}g/mL$ concentration and western blot analysis showed that the expression of iNOS and COX-2 protein decreased in a concentration-dependent manner. Inhibition of tyrosinase activity showed 36.8% inhibition at $50{\mu}g/mL$ concentration of ginseng complex and inhibition of melanin contents showed 47.8% inhibition at $50{\mu}g/mL$ concentration. From the results of the experiment, it was confirmed that the ginseng complex had excellent anti-inflammatory and whitening effect and could be used as a safe natural cosmetic material in the future.

Whitening and Anti-oxidative Constituents from the Extracts of Hydrangea petiolaris Leaves (등수국 잎 추출물 유래 미백 및 항산화 활성 성분)

  • Jo, Seong Mi;Kim, Jung Eun;Lee, Nam Ho
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.48 no.2
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    • pp.123-134
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    • 2022
  • In this study, the whitening and antioxidant effects of the extracts from Hydrangea petiolaris (H. petiolaris) leaves was confirmed, and the chemical structure was identified by separating the active ingredients. In the whitening tests using α-MSH stimulated B16F10 melanoma cells, the n-hexane (Hex) fraction inhibited the cellular melanogenesis and intracellular tyrosinase activities without causing cell toxicity. In addition, the Hex fraction reduced expression of tyrosinase and TRP-2 protein. Upon the anti-oxidative studies by DPPH and ABTS+ radicals, potent radical scavenging activities were observed in the ethyl acetate (EtOAc) fraction. Also, for the cellular protective effects on HaCat keratinocytes damaged by H2O2, the EtOAc fraction indicated protective effects against oxidative stress. Eight phytochemicals were isolated from the extract of H. petiolaris leaves; ethyl linoleate (1), ethyl linolenate (2), 1-linoleoyl glycerol (3), 1-linolenoyl glycerol (4), epi-catechin (5), afzelin (6), quercitrin (7), hyperin (8). Among the isolates, the compounds 5 - 8 showed DPPH and ABTS+ radical scavenging activities. The contents of quercitirin, a major isolated in this extract, determined by HPLC analysis were confirmed to be about 31.3 mg/g for the 70% ethanol extract and 169.8 mg/g for the EtOAc fraction. Based on these results, it was suggested that the extract from H. petiolaris leaves could be potentially applicable as whitening and anti-oxidative ingredients in cosmetic formulations.

New Whitening Agent : Selina-4(14), 7(11)-dien-8-one (신규 미백제 : Selina-4(14), 7(11)-dien-8-one)

  • Kim, Cheong-Taek;Chang, Yun-Hee;Lee, Sang-Hwa;Kang, Sang-Jin;Cho, Wan-Goo
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.31 no.1 s.49
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    • pp.17-23
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    • 2005
  • We had previously reported that Selina (selina-4(14), 7(11)-dien-8-one) was isolated from methanol extract of Afractylodes rhizome and has strong whitening activity in B16 melanoma cells. In this report, we demonstrated its action mechanism in melan-a cells, non-tumorigenic melanocytes. We also investigated the clinical efficacy of cosmetic preparation containing Selina. Selina reduced the melanin synthesis of Melan-a cells by $50\%$ at a concentration of $10 {\mu}g/mL$ without any apparent cytotoxicity. We also found that the treatment of cells with Selina decreased tyrosinase activity by $60\%$ at a concentration of $10 {\mu}g/mL$ but Selina was not a direct inhibitor of tyrosinase activities. To elucidate the action mechanism of Selina, we investigated the changes in mRNA and protein level of tyrosinase, TRP-1 and TRP-2 using RT-PCR and western blotting, respectively. As a result, the mRNA and protein level of tyrosinase were markedly reduced at $10 {\mu}g/mL$ of Selina without any effect on TRP-1 and TRP-2. These results suggest that Selina exerts its whitening effect mainly through regulating expression of tyrosinase. A 7 week-clinical trial using formulation containing $0.2\%$ selina-4(14), 7(11)-dien-8-one with 20 volunteers resulted in statistically significant whitening effect (p < 0.05), without any adverse effect. Based on these results, Selina (selina-4(14), 7(11)-dien-8-one) can be s useful and safe ingredient for the cleanness and brightness of skin.

Melanogenesis regulatory constituents from Premna serratifolia wood collected in Myanmar

  • WOO, SO-YEUN
    • Proceedings of the Plant Resources Society of Korea Conference
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    • 2019.04a
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    • pp.21-22
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    • 2019
  • Melanin is a mixture of pigmented biopolymers synthesized by epidermal melanocytes that determine the skin, eye, and hair colors. Melanocytes produce two different kinds of melanin, eumelanin (dark brown/black insoluble pigments found in dark skin and dark hair and pheomelanin (lighter red/yellow). The biological role of melanin is to prevent skin damage by ultraviolet (UV) radiation. However, the overproduction or deficiency of melanin synthesis could lead to serious dermatological problems, which include melasma, melanoderma, lentigo, and vitiligo. Therefore, regulating melanin production is important to prevent the pigmentation disorders. Myanmar has a rich in natural resources. However, the chemical constituents of these natural resources in Myanmar have not been fully investigated. In the effort to search for compounds with anti-melanin deposition activity from Myanmar natural resources, five plants were collected in Myanmar. Extracts of these collected five plants were tested for anti-melanin deposition activity against a mouse melanoma cell line (B16-F10) induced with ${\alpha}$-melanocyte-stimulating hormone (${\alpha}$-MSH) and 3-isobutyl-1-methylxanthine (IBMX), and their anti-melanin deposition activities were compared with the positive control, arbutin. Among the tested extracts, the CHCl3 extracts of the Premna serratifolia (syn: P. integrifolia) wood showed anti-melanin deposition activities with IC50 values of $81.3{\mu}g/mL$. Hence, this study aims to identify secondary metabolites with anti-melanin deposition activity from P. serratifolia wood of Myanmar. P. serratifolia belongs to the Verbenaceae family and is widely distributed in near western sea coast from South Asia to South East Asia, which include India, Malaysia, Vietnam, Cambodia, and Sri Lanka. People in Tanintharyi region located in the southern part of Myanmar utilize the P. serratifolia, Sperethusa crenulata, Naringi crenulata, and Limonia acidissima as Thanaka, traditional cosmetics in Myanmar. Thanaka is applied in the form of paste onto skins to make it smooth and clear, as well as to prevent wrinkles, skin aging, excessive facial oil, pimples, blackheads, and whiteheads. However, the chemical constituents responsible for their cosmetic properties are yet to be identified. Moreover, the chemical constituents of P. serratifolia was almost uncharacterized. Investigation of the P. serratifolia chemical constituents is thus an attractive endeavor to discover new anti-melanin deposition active compounds. The investigation of the chemical constituents of the active CHCl3 extract of P. serratifolia led to isolation of four new lignoids, premnan A (1), premnan B (2), taungtangyiol C (3), and 7,9-dihydroxydolichanthin B (4), together with premnan C (5) (assumed to be an artifact), one natural newlignoid,(3R,4S)-4-(1,3-benzodioxol-5-ylcarbonyl)-3-[(R)-1-(1,3-benzo dioxol-5-yl)-1-hydroxy methyl]tetrahydro-2-furanone (6), and five known compounds (7-11)1,2). The structures of all isolated compounds were determined on the basis of their spectroscopic data and by comparison with the reported literatures. The absolute configurations of 1-3 and 5 were also determined by optical rotation and circular dichroism (CD) data analyses1). The anti-melanin deposition activities of all the isolated compounds were evaluated against B16-F10 cell line. 7,9-Dihydroxydolichanthin B (4) and ($2{\alpha},3{\alpha}$)-olean-12-en-28-oic acid (11) showed strong anti-melanin deposition activities with IC50 values of 18.4 and $11.2{\mu}M$, respectively, without cytotoxicity2). On the other hand, compounds 1-3, 5, and 7 showed melanogenesis enhancing activities1). To better understand their anti-melanin deposition mechanism, the effects of 4 and 11 on tyrosinase activities were investigated. The assay indicated that compounds 4 and 11 did not inhibit tyrosinase. Furthermore, we also examined the mRNA expression of microphthalmia-associated transcription factor (MITF), tyrosinase (TYR), tyrosinase-related protein-1 (TRP-1), and tyrosinase-related protein-2 (TRP-2). Compounds 4 and 11 down-regulated the expression of Tyr and Mitf mRNAs, respectively. Although the P. serratifolia wood has been used as traditional cosmetics in Myanmar for centuries, there are no scientific evidences to support its effectiveness as cosmetics. Investigation of the anti-melanin deposition activity of the chemical constituents of P. serratifolia thus provided insight into the effectiveness of the P. serratifolia wood as a cosmetic agent.

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Manufacturing Protein-DNA Chip for Depigmenting Agent Screening (전사인자 저해제 통한 미백제 탐색용 단백질 칩 제작)

  • Han Jung-Sun;Kwak Eun-Young;Lee Hyang-Bok;Shin Jlung-Hyun;Baek Seung-Hak;Chung Bong-Hyun;Kim Eun-Ki
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.30 no.4 s.48
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    • pp.479-483
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    • 2004
  • An attempt was made to develop a proteinchip for screening of MITF (microphthalmia transcription factor) inhibitor. Binding of MITF to E-box causes transcription of several pigmenting genes including tyrosinase gene. We investigated binding of MITF and its DNA binding site (E-box) using a protein-DNA chip with various detection methods including flurorescence (Cyt3). SPR (surface plasmon resonance) and SPRi (surface plasmon resonance imaging). A fusion protein (MITF-Maltose Binding Protein) was attached on the glass plate by chemical modification. An inhibitory synthetic DNA oligomer, artificially designed based on the E-box sequence, inhibited the binding of MITF and E-box. These results showed the potentials of flurorescence-based MITF protein chip as a microarray for high throughput screening (HTS) system of depigmenting agents.

Melanogenesis Promotion by 3-Deazaneplanocin A, a Specific Inhibitor of S-Adenosylhomocysteine Hydrolase, in B16/F10 Melanoma Cells (B16/F10 흑색종 세포에서 S-Adenosylhomocysteine Hydrolase 의 선택적 저해제 3-Deazaneplanocin A 에 의한)

  • Hwang, Yun Jeong;Boo, Yong Chool
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.47 no.2
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    • pp.107-121
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    • 2021
  • Skin hypopigmentation, which is observed in albinism or vitiligo, occurs when melanin synthesis is decreased by genetic, epigenetic, and other factors. To identify drug candidates that can promote melanin synthesis in cells, we screened an epigenetic modulator library consisting of 141 cell-permeable, small molecule drugs. B16/F10 murine melanoma cells were treated with each drug at 0.1 𝜇M and melanin synthesis and cell viability were subsequently monitored. As a result, (-)-neplanocin A, 3-deazaneplanocin A (DZNep), and DZNep hydrochloride were found to increase cellular melanin synthesis without causing cytotoxicity. Because these three structurally related drugs exhibited similar dose-dependent effects on melanin synthesis and cell viability, DZNep was selected as a representative drug for additional experiments. DZNep increased intracellular melanin content and tyrosinase (TYR) activity. DZNep also induced the expression of TYR, tyrosinase-related protein 1 (TYRP1), and dopachrome tautomerase (DCT) at the mRNA and protein levels. DZNep also induced the mRNA and protein expression of microphthalmia-associated transcription factor (MITF), a key regulator of melanin synthesis. DZNep is a specific inhibitor of S-adenosylhomocysteine hydrolase and it caused the accumulation of S-adenosylhomocysteine that inhibits histone methyltransferases in cells. This study suggests that melanogenesis can be modulated by targeting S-adenosylhomocysteine hydrolase in certain cellular contexts.

Nutritional and Physiological Functionalities of Liriope Tuber (Cheongsim and Liriope Tuber No. 1) (맥문동(청심, 맥문동 1호)의 영양특성 및 생리 기능성)

  • Song, Jung-Hwa;Kang, Min-Gu;Kim, Na-Mi;Lee, Jong-Soo
    • Korean Journal of Medicinal Crop Science
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    • v.19 no.6
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    • pp.478-483
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    • 2011
  • The goal of this study was to investigate the nutritional characteristics and physiological functionality of Liriope tuber for development of new bioactive compound from Liriope tuber. Crude protein and carbohydrate contents of Chenogsim were 9.25% and 77.98%, respectively and crude protein, 9.86% and carbohydrate, 79.08% were also contained in Liriope tuber No.1. Both of Liriope tubers were showed very high contents of sucrose (Cheongsim; 4.08%, Liriope tuber No.1; 4.91%), oxalic acid (0.98%, 0.86%) and glutamic acid (3.736 g/100 g, 4,196 g/100 g). Among several physiological functionalities, tyrosinase inhibitory activity were showed very high 86.4% in Cheongsim and 82.02% in Liriope tuber No.1, respectively.

Inhibition of Melanogenesis by Abietatriene from Vitex Trifolia Leaf Oil

  • Lee, Hong Gu;Kim, Tae Yoon;Jeon, Jung Hoon;Lee, Sang Hwa;Hong, Yoon Ki;Jin, Mu Hyun
    • Natural Product Sciences
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    • v.22 no.4
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    • pp.252-258
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    • 2016
  • Vitex trifolia L. has been used traditionally to treat various illnesses, such as inflammation, headache, migraine, and gastrointestinal infections. We analyzed and evaluated the composition of V. trifolia leaf oil. Based on the results, we isolated abietatriene from V. trifolia leaf oil and investigated the effect of V. trifolia leaf oil and its active compound abietatriene on melanogenesis in B16F10 melanoma cells. They significantly decreased melanin contents and melanogenic factors, such as tyrosinase, TRP-1, TRP-2, and MITF dose-dependently in both protein and mRNA levels. Protein and mRNA expressions were determined by Western blot analysis and quantitative real time RT-PCR. Findings indicate that V. trifolia leaf oil and abietatriene reduce melanogenesis by regulating the expression of melanogenic factors. These results suggest that V. trifolia leaf oil and abietatriene could comprise a useful therapeutic agent for treating hyperpigmentation and used as effective skin-whitening agents.