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1.
Cell Mol Biol (Noisy-le-grand) ; 64(5): 80-84, 2018 Apr 30.
Artigo em Inglês | MEDLINE | ID: mdl-29729698

RESUMO

In skin, melanocytes determine skin color using melanogenesis, which induces protective mechanism to oxidative stress and UV damage. However, when melanin is excessive produced by the various stimulus, the accumulated melanin induces hyperpigmentation disease such as melasma, freckles, Melanism ware induced. Therefore, it is implicated to finding potential agents for whitening to be used in cosmetic products. In our present study, we show that Poria cocos Wolf extracts decreased melanin synthesis in B16F10. And then this inhibition of melanogenesis was provoked by regulation of tyrosinase activity and tyrosinase and MITF expression. Moreover, Poria cocos Wolf extracts contained cream improved skin tone using increase of bright value. Overall, these results provide evidence to potential agent for whitening to be used in cosmetic products.


Assuntos
Melaninas/antagonistas & inibidores , Melanócitos/efeitos dos fármacos , Monofenol Mono-Oxigenase/antagonistas & inibidores , Preparações Clareadoras de Pele/farmacologia , Pele/efeitos dos fármacos , Wolfiporia/química , Adulto , Agaricales/química , Animais , Linhagem Celular Tumoral , Método Duplo-Cego , Feminino , Proteínas Fúngicas/antagonistas & inibidores , Proteínas Fúngicas/isolamento & purificação , Proteínas Fúngicas/metabolismo , Regulação da Expressão Gênica , Humanos , Melaninas/biossíntese , Melanócitos/enzimologia , Melanócitos/patologia , Melanoma Experimental/enzimologia , Melanoma Experimental/genética , Melanoma Experimental/patologia , Camundongos , Fator de Transcrição Associado à Microftalmia/antagonistas & inibidores , Fator de Transcrição Associado à Microftalmia/genética , Fator de Transcrição Associado à Microftalmia/metabolismo , Monofenol Mono-Oxigenase/genética , Monofenol Mono-Oxigenase/metabolismo , Pigmentação/efeitos dos fármacos , Pigmentação/genética , Extratos Vegetais/química , Pele/enzimologia , Preparações Clareadoras de Pele/isolamento & purificação , Neoplasias Cutâneas/enzimologia , Neoplasias Cutâneas/genética , Neoplasias Cutâneas/patologia
2.
BMC Complement Altern Med ; 17(1): 71, 2017 Jan 23.
Artigo em Inglês | MEDLINE | ID: mdl-28114924

RESUMO

BACKGROUND: The derivative of caffeamide exhibits antioxidant and antityrosinase activity. The activity and mechanism of N-(4-methoxyphenyl) caffeamide (K36E) on melanogenesis was investigated. METHODS: B16F0 cells were treated with various concentrations of K36E; the melanin contents and related signal transduction were studied. Western blotting assay was applied to determine the protein expression, and spectrophotometry was performed to identify the tyrosinase activity and melanin content. RESULTS: Our results indicated that K36E reduced α-melanocyte-stimulating hormone (α-MSH)-induced melanin content and tyrosinase activity in B16F0 cells. In addition, K36E inhibited the expression of phospho-cyclic adenosine monophosphate (cAMP)-response element-binding protein, microphthalmia-associated transcription factor (MITF), tyrosinase, and tyrosinase-related protein-1 (TRP-1). K36E activated the phosphorylation of protein kinase B (AKT) and glycogen synthase kinase 3 beta (GSK3ß), leading to the inhibition of MITF transcription activity. K36E attenuated α-MSH induced cAMP pathways, contributing to hypopigmentation. CONCLUSIONS: K36E regulated melanin synthesis through reducing the expression of downstream proteins including p-CREB, p-AKT, p-GSK3ß, tyrosinase, and TRP-1, and activated the transcription factor, MITF. K36E may have the potential to be developed as a skin whitening agent.


Assuntos
Anilidas/farmacologia , Ácidos Cafeicos/farmacologia , Melaninas/antagonistas & inibidores , Anilidas/síntese química , Animais , Ácidos Cafeicos/síntese química , Linhagem Celular Tumoral , Proteína de Ligação ao Elemento de Resposta ao AMP Cíclico/antagonistas & inibidores , Proteína de Ligação ao Elemento de Resposta ao AMP Cíclico/metabolismo , Glicogênio Sintase Quinase 3 beta/metabolismo , Interferon Tipo I/antagonistas & inibidores , Interferon Tipo I/metabolismo , Melaninas/biossíntese , Camundongos , Fator de Transcrição Associado à Microftalmia/antagonistas & inibidores , Fator de Transcrição Associado à Microftalmia/metabolismo , Monofenol Mono-Oxigenase/antagonistas & inibidores , Monofenol Mono-Oxigenase/metabolismo , Proteínas da Gravidez/antagonistas & inibidores , Proteínas da Gravidez/metabolismo , Proteínas Proto-Oncogênicas c-akt/metabolismo , Transdução de Sinais/efeitos dos fármacos , Preparações Clareadoras de Pele/síntese química
4.
Chem Biodivers ; 10(3): 313-27, 2013 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-23495149

RESUMO

The MeOH extract of moxa, the processed leaves of Artemisia princeps PAMP. (Asteraceae), exhibited potent 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical-scavenging activity and melanogenesis-inhibitory activity in α-melanocyte-stimulating hormone (α-MSH)-stimulated B16 melanoma cells. Eight caffeoylquinic acids, 1 and 6-12, five flavonoids, 13-17, two benzoic acid derivatives, 18 and 19, three coumarin derivatives, 20-22, four steroids, 23-26, and six triterpenoids, 27-32, were isolated from the MeOH extract. Upon evaluation of compounds 1, 6-23, and four semisynthetic caffeoylquinic acid esters, 2-5, for their DPPH radical-scavenging activity, 15 compounds, 1-13, 17, and 19, showed potent activities (IC(50) 3.1-16.8 µM). The 15 compounds exhibited, moreover, potent inhibitory activities (51.1-92.5% inhibition) against peroxidation of linoleic acid emulsion at 10 µg/ml concentration. In addition, when 27 compounds, 1-8, 10, 12, 13, 15-18, 20-25, and 27-32, were evaluated for their inhibitory activity against melanogenesis in α-MSH-stimulated B16 melanoma cells, five caffeoylquinic acids, i.e., chlorogenic acid (1), ethyl chlorogenate (3), propyl chlorogenate (4), isopropyl chlorogenate (5), and butyl chlorogenate (6), along with homoorientin (17) and vanillic acid (18), exhibited inhibitory activities with 33-62% reduction of melanin content at 100 µM concentration with no or almost no toxicity to the cells (89-114% of cell viability at 100 µM). Western blot analysis showed that compound 6 reduced the protein levels of microphtalmia-associated transcription factor (MITF), tyrosinase, tyrosine-related protein 1 (TRP-1), and TRP-2 mostly in a concentration-dependent manner, suggesting that this compound inhibits melanogenesis on α-MSH-stimulated B16 melanoma cells by, at least in part, inhibiting the expression of MITF, followed by decreasing the expression of tyrosinase, TRP-1, and TRP-2. Furthermore, four compounds, 13, 15, 16, and 30, exhibited cytotoxicities against HL60 human leukemia cell line (IC(50) 7.0-11.1 µM), and nine compounds, 14-16, 23, 26-28, 31, and 32, showed inhibitory effects (IC(50) 272-382 mol ratio/32 pmol 12-O-tetradecanoylphohrbol-13-acetate (TPA)) against Epstein-Barr virus early antigen (EBV-EA) activation induced by TPA in Raji cells.


Assuntos
Antioxidantes/química , Artemisia/química , Ácido Quínico/análogos & derivados , Animais , Antioxidantes/isolamento & purificação , Antioxidantes/toxicidade , Diferenciação Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Células HL-60 , Humanos , Melaninas/antagonistas & inibidores , Melaninas/metabolismo , Hormônios Estimuladores de Melanócitos/antagonistas & inibidores , Hormônios Estimuladores de Melanócitos/metabolismo , Melanoma Experimental/metabolismo , Melanoma Experimental/patologia , Camundongos , Fator de Transcrição Associado à Microftalmia/antagonistas & inibidores , Fator de Transcrição Associado à Microftalmia/metabolismo , Monofenol Mono-Oxigenase/antagonistas & inibidores , Monofenol Mono-Oxigenase/metabolismo , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Extratos Vegetais/toxicidade , Folhas de Planta/química , Ácido Quínico/química , Ácido Quínico/isolamento & purificação , Ácido Quínico/toxicidade
5.
Biosci Biotechnol Biochem ; 76(4): 767-71, 2012.
Artigo em Inglês | MEDLINE | ID: mdl-22484949

RESUMO

Xanthium strumarium L. (Asteraceae) is traditionally used in Korea to treat skin diseases. In this study, we investigated the effects of a X. strumarium stem extract on melanin synthesis. It inhibited melanin synthesis in a concentration-dependent manner, but it did not directly inhibit tyrosinase, the rate-limiting melanogenic enzyme, and instead downregulated microphthalmia-associated transcription factor (MITF) and tyrosinase expression. MITF, the master regulator of pigmentation, is a target of the Wnt signaling pathway, which includes glycogen synthase kinase 3ß (GSK3ß) and ß-catenin. Hence, the influence of X. strumarium stem extract on GSK3ß and ß-catenin was further investigated. X. strumarium induced GSK3ß phosphorylation (inactivation), but the level of ß-catenin did not change. Moreover, a specific GSK3ß inhibitor restored X. strumarium-induced melanin reduction. Hence, we suggest that X. strumarium inhibits melanin synthesis through downregulation of tyrosinase via GSK3ß phosphorylation.


Assuntos
Quinase 3 da Glicogênio Sintase/metabolismo , Melanócitos/efeitos dos fármacos , Fator de Transcrição Associado à Microftalmia/antagonistas & inibidores , Monofenol Mono-Oxigenase/antagonistas & inibidores , Extratos Vegetais/farmacologia , Xanthium/química , Animais , Linhagem Celular Transformada , Relação Dose-Resposta a Droga , Regulação para Baixo/efeitos dos fármacos , Quinase 3 da Glicogênio Sintase/genética , Glicogênio Sintase Quinase 3 beta , Melaninas/genética , Melaninas/metabolismo , Melanócitos/citologia , Melanócitos/metabolismo , Camundongos , Fator de Transcrição Associado à Microftalmia/genética , Fator de Transcrição Associado à Microftalmia/metabolismo , Monofenol Mono-Oxigenase/genética , Monofenol Mono-Oxigenase/metabolismo , Fosforilação , Pigmentação/genética , Extratos Vegetais/isolamento & purificação , Caules de Planta/química , Via de Sinalização Wnt/efeitos dos fármacos , Via de Sinalização Wnt/genética , beta Catenina/genética , beta Catenina/metabolismo
6.
Int J Mol Med ; 29(1): 119-24, 2012 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-21972008

RESUMO

Cordycepin has been a traditional medicine in China and Korea for centuries. This study explored the inhibitory effect of cordycepin on melanogenesis and the relative molecular mechanisms. Cordycepin inhibited melanin synthesis-related enzymes, such as tyrosinase, tyrosinase-related protein-1 (TRP1) and tyrosinase-related protein-2 (TRP2). α-MSH and IBMX were reported as melanin synthesis enhancers. Both of them could increase intracellular melanin synthesis by activation of the microphthalmia-associated transcription factor (MITF) signaling pathway. In the MITF pathway, the phosphorylation of cAMP related binding protein (CREB) activated the transcription of MITF, resulting in increasing melanin synthesis. Cordycepin also decreased the phosphorylation of CREB induced by α-MSH and IBMX in B16F10 melanoma cells. Accordingly, cordycepin inhibited melanogenesis signaling pathways by activating ERK and AKT signaling pathways to regulate the suppression of MITF and its downstream pathways including tyrosinase, TRP1 and TRP2. These results indicate the role of cordycepin as a potent depigmenting agent for cosmetics.


Assuntos
Proteína de Ligação ao Elemento de Resposta ao AMP Cíclico/antagonistas & inibidores , Desoxiadenosinas/farmacologia , Melaninas/metabolismo , Fator de Transcrição Associado à Microftalmia/antagonistas & inibidores , alfa-MSH/metabolismo , 1-Metil-3-Isobutilxantina/antagonistas & inibidores , 1-Metil-3-Isobutilxantina/farmacologia , Animais , Linhagem Celular Tumoral , Cromonas/farmacologia , Proteína de Ligação ao Elemento de Resposta ao AMP Cíclico/metabolismo , MAP Quinases Reguladas por Sinal Extracelular/metabolismo , Flavonoides/farmacologia , Camundongos , Fator de Transcrição Associado à Microftalmia/metabolismo , Monofenol Mono-Oxigenase/efeitos dos fármacos , Morfolinas/farmacologia , Fosfatidilinositol 3-Quinases/metabolismo , Fosforilação/efeitos dos fármacos , Proteínas Proto-Oncogênicas c-akt/metabolismo , Transdução de Sinais/efeitos dos fármacos
7.
Food Chem Toxicol ; 49(12): 3038-45, 2011 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-21946069

RESUMO

Mulberroside A was isolated from the ethanol extract of Morus alba roots. The enzymatic hydrolysis of mulberroside A with Pectinex produced oxyresveratrol and oxyresveratrol-3-O-glucoside. We tested oxyresveratrol, oxyresveratrol-3-O-glucoside, and mulberroside A to determine whether they could inhibit ultraviolet B (UVB) irradiation-induced melanogenesis in brown guinea pig skin. Topical application of mulberroside A, oxyresveratrol, and oxyresveratrol-3-O-glucoside reduced the pigmentation in guinea pig skin. These compounds suppressed the expression of melanogenic enzymes tyrosinase, tyrosinase-related protein-1, and microphthalmia transcription factor. The anti-melanogenesis effect was highest with oxyresveratrol, intermediate with oxyresveratrol-3-O-glucoside, and lowest with mulberroside A. Mulberroside A is a glycosylated stilbene of oxyresveratrol; thus, the deglycosylation of mulberroside A resulted in enhanced inhibition of melanogenesis. Histological analysis with Fontana-Masson staining confirmed that these compounds significantly reduced the melanin content in the epidermis of UVB-irradiated guinea pig skin compared to the vehicle control. Thus, these compounds effectively reduced pigmentation and may be suitable cosmetic agents for skin whitening.


Assuntos
Dissacarídeos/farmacologia , Glucosídeos/farmacologia , Melaninas/biossíntese , Extratos Vegetais/farmacologia , Estilbenos/farmacologia , Raios Ultravioleta/efeitos adversos , Animais , Cobaias , Melaninas/antagonistas & inibidores , Fator de Transcrição Associado à Microftalmia/antagonistas & inibidores , Fator de Transcrição Associado à Microftalmia/genética , Fator de Transcrição Associado à Microftalmia/metabolismo , Monofenol Mono-Oxigenase/antagonistas & inibidores , Monofenol Mono-Oxigenase/genética , Monofenol Mono-Oxigenase/metabolismo , Morus/química , Oxirredutases/antagonistas & inibidores , Oxirredutases/genética , Oxirredutases/metabolismo , Raízes de Plantas/química , Pele/efeitos dos fármacos , Pele/metabolismo , Pele/efeitos da radiação
8.
Arch Pharm Res ; 34(8): 1339-45, 2011 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-21910056

RESUMO

Intracellular cAMP stimulates microphthalmia-associated transcription factor (MITF) induction in melanocytes through cAMP-responsive element binding protein (CREB), which plays a pivotal role in the gene expression of tyrosinase for melanin biosynthesis. In the present study, saucerneol D as a lignan constituent of Saururus chinensis (Saururaceae family) efficiently inhibited melanin production with IC(50) values of 188-297 nM in B16 melanoma cells stimulated with α-melanocyte stimulating hormone (α-MSH) or other cAMP elevators. Moreover, saucerneol D down-regulated α-MSH-induced gene expression of tyrosinase at the transcription level in B16 cells, but it did not directly inhibit the catalytic activity of cell-free tyrosinase. As to the molecular basis of hypopigmenting action, saucerneol D inhibited α-MSH-induced phosphorylation of CREB in the cells, and sequentially suppressed MITF induction. Taken together, this study provides saucerneol D down-regulated the gene expression of tyrosinase, resulting in the inhibition of cAMP-induced melanin biosynthesis, and suggests pharmacological potential of the lignan structure in skin hyperpigmentation.


Assuntos
AMP Cíclico/metabolismo , Lignanas/farmacologia , Melaninas/biossíntese , Melanócitos/metabolismo , Sobrevivência Celular , Proteína de Ligação ao Elemento de Resposta ao AMP Cíclico/genética , Proteína de Ligação ao Elemento de Resposta ao AMP Cíclico/metabolismo , Regulação para Baixo , Avaliação Pré-Clínica de Medicamentos , Expressão Gênica , Hormônios/metabolismo , Hormônios/farmacologia , Humanos , Hiperpigmentação/tratamento farmacológico , Hiperpigmentação/genética , Hiperpigmentação/metabolismo , Lignanas/química , Lignanas/isolamento & purificação , Luciferases/metabolismo , Melaninas/genética , Melanoma/tratamento farmacológico , Melanoma Experimental/genética , Melanoma Experimental/metabolismo , Fator de Transcrição Associado à Microftalmia/antagonistas & inibidores , Fator de Transcrição Associado à Microftalmia/genética , Monofenol Mono-Oxigenase/genética , Monofenol Mono-Oxigenase/metabolismo , Fosforilação , Saururaceae , alfa-MSH/metabolismo , alfa-MSH/farmacologia
9.
Biosci Biotechnol Biochem ; 74(9): 1908-12, 2010.
Artigo em Inglês | MEDLINE | ID: mdl-20834163

RESUMO

In this study, the inhibitory effect of Elephantopus mollis H.B. and K. extract on melanogenesis in B16 murine melanoma cells was examined and possible mechanisms were elucidated. The melanin content in B16 cells decreased when they were treated with E. mollis extract. Inhibition was accompanied by reduced expression of tyrosinase (TYR) and tyrosinase-related protein 1 (TRP1). Furthermore, the expression level of microphthalmia-associated transcription factor (MITF), a major transcriptional regulator of genes encoding melanogenic enzymes such as Tyr and Trp1, decreased as assessed by western blotting and quantitative reverse transcriptase polymerase chain reaction (RT-PCR). These results suggest that E. mollis extract reduces melanogenesis by downregulating Mitf expression, leading to reduced expression of Tyr and Trp1. In addition, melanocortin-1 receptor (MC1R) expression was downregulated by E. mollis extract, suggesting desensitization to α-melanocyte-stimulating hormone (α-MSH) of cells treated with the extract.


Assuntos
Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos , Melanoma/tratamento farmacológico , Fator de Transcrição Associado à Microftalmia/genética , Extratos Vegetais/farmacologia , Plantas Medicinais/química , Regulação para Baixo/genética , Humanos , Melaninas/análise , Melanoma/etiologia , Melanoma Experimental/tratamento farmacológico , Melanoma Experimental/patologia , Glicoproteínas de Membrana , Fator de Transcrição Associado à Microftalmia/antagonistas & inibidores , Monofenol Mono-Oxigenase , Oxirredutases , Extratos Vegetais/uso terapêutico , Receptor Tipo 1 de Melanocortina , alfa-MSH
10.
Pigment Cell Res ; 18(6): 439-46, 2005 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-16280009

RESUMO

The development of effective skin-lightening agents is an increasingly important area of research aimed at the treatment of hyperpigmentation induced by UV irradiation or by medical conditions such as melasma, postinflammatory melanoderma and solar lentigo. Although some inhibit tyrosinase, identifying and understanding the mechanisms of action of other agents is an important goal if more effective pigmentation inhibitors are to be developed. We present here that an extract of Lepidium apetalum (ELA) decreased UV-induced skin pigmentation in brown guinea pigs and melanogenesis of HM3KO human melanoma cells. Interestingly, ELA did not reduce melanogenesis in HM3KO cells unless they were co-cultivated in keratinocyte-conditioned medium prepared by culturing keratinocytes with ELA. Under these conditions, ELA decreased tyrosinase mRNA and protein expression as well as melanin content via an ELA-mediated increase in keratinocyte IL-6 production which in turn was shown to decrease in the expression Mitf, a transcription factor implicated in tyrosinase gene expression and melanocyte differentiation. The results reveal that ELA may be an effective inhibitor of hyperpigmentation caused by UV irradiation or by pigmented skin disorders through a mechanism involving IL-6-mediated downregulation of Mitf rather than a direct inhibition of tyrosinase activity.


Assuntos
Interleucina-6/metabolismo , Lepidium/química , Extratos Vegetais/farmacologia , Pigmentação da Pele/efeitos dos fármacos , Animais , Western Blotting , Diferenciação Celular , Proliferação de Células/efeitos dos fármacos , Proliferação de Células/efeitos da radiação , Células Cultivadas , Regulação para Baixo , Ensaio de Imunoadsorção Enzimática , Cobaias , Queratinócitos/citologia , Queratinócitos/efeitos dos fármacos , Queratinócitos/efeitos da radiação , Melaninas/metabolismo , Melanoma/tratamento farmacológico , Melanoma/etiologia , Fator de Transcrição Associado à Microftalmia/antagonistas & inibidores , Fator de Transcrição Associado à Microftalmia/metabolismo , Monofenol Mono-Oxigenase/genética , Monofenol Mono-Oxigenase/metabolismo , RNA Mensageiro/genética , RNA Mensageiro/metabolismo , Reação em Cadeia da Polimerase Via Transcriptase Reversa , Sementes/química , Transdução de Sinais , Pigmentação da Pele/efeitos da radiação , Raios Ultravioleta
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