• Bulletin of the Korean Chemical Society
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• v.29 no.1
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• pp.43-46
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• 2008

The aim of present study was to examine the inhibitory effects of hydroxamic acid derivatives on the melanogenesis. We found that hydroxamic acid moiety was important for anti-melanogenic activity. Compounds 1a and 1b strongly inhibited melanin synthesis via deactivation of tyrosinase. Hydroxamic acid has metal ion chelating ability which is similar to that kojic acid, however, anti-tyrosinase mechanism of compounds 1a and 1b was different from that of kojic acid. They showed noncompetitive inhibition kinetics

• The Journal of Korean Medicine
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• v.38 no.4
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• pp.62-81
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• 2017

Objectives: As interests in the beauty of skin is growing continuously, more people are focusing on white and clean skin. Melanin is the major factor that determines skin color. The abnormal concentration of melanin causes various skin diseases such as vitiligo, freckles, and melasma. This study investigated the inhibitory effect of Eriobotryae Folium extracts (EF) with phreatic water (PW) on the melanin synthesis. Methods: The effect of EF on melanin synthesis was evaluated by using mouse melanoma cells (B16F10). To define the mechanisms, real-time PCR and western blot were used. We also evaluated the inhibitory effects of EF and PW on melanin synthesis by using HRM-2 melanin-possessing hairless mice. After UVB irradiation, melanin differences between the skin parts that were treated and untreated with EF and PW. Levels of mRNA were measured by real-time quantitative PCR and histological analysis of the dorsal skin was conducted by hematoxylin and eosin staining. Results: EF inhibited various mechanisms of melanogenesis, and the effect was increased when combined with PW. In vitro experiments have shown that EF inhibited the expressions of tyrosinase related protein-1 (TRP-1) mRNA, tyrosinase mRNA, microphthalmia-associated transcription factor (MITF) mRNA and the tyrosinase inhibitory activation, but it stimulated the extracellular regulated kinase (ERK) mRNA expression. In vivo experiments have shown that EF prevented melanogenesis in the mice dorsal skin and inhibited TRP-1 mRNA expression. Also these effects were increased when combined with PW. Conclusions: EF and PW might be a new and effective treatment for whitening and treating pigmentation of skin.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.20 no.1
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• pp.1-13
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• 1994

An antioxidative compound was isolated from pine needles. This compound was identified as 4-hydroxy-5-methyl-3[2H]-furanone on the basis of spectroscopic evidences. It scavenged 1,1-diphenyl-2-picrylhydrazyl free radicals more efficiently than maltol and tocopherol did. It exhibited an inhibitory effect on the lipid peroxidation of rat liver microsome induced by Fe(ll)/ascorbate, and the protective effect against UV cytotoxicity in cultured human fibroblasts. In addition, HMF appeared to prevent the cellular melanogenesis in the cultured murine melanoma cells, more effectively than kojic acid, a well known inhibitor of melanogenesis, while the former was not so effective as the latter for the inhibilion of the tyrosinase. Considering that cellular melanogenesis is a metabolic process triggered by oxidative stress, it was tentatively deduced that the antioxidative property of HMF may afford the effect against cellular pigmentation by alleviating the causative stress. This study provided a novel inhibitor of melanogenesis, that might be useful for the cosmetic applications.

• Proceedings of the SCSK Conference
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• 2003.09b
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• pp.544-544
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• 2003

We investigated the inhibitory effect of whitening materials with growth factor or alone on melanomas derived from Human (B-16) and mouse (SK-MEL-31) using melanin content. Melanin content was determined by the absorbance value at 470nm per cells. we used the growth factors known as activators of Adenylate cyclase, Protein kinase C and tyrosine kinase pathway separately. In addition, we compared the action of UV-induced with non-biological growth factor with whitening materials in melanomas derived from Human and mouse. The results showed that the aspect of inhibitory effect of whitening materials on B16 and SK-MEL-31 was not different. And, the action of each growth factor involved in the differentiation and proliferation of melanoma on the inhibition of melanogenesis in B-16 and SK-MEL-31 using whitening agents showed no difference. Also, The action of UV -induced and non-biological growth factors didn't exhibit different pattern on the effect of whitening agent in B-16 and SK-MEL-31.

• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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• v.15 no.2
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• pp.20-32
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• 2002

The aim of this study was to investigate the effect of Codonopsis lanceolatae on the melanogenesis of HM3KO human melanoma cells biologically. The cells were treated for 3 days and 5 days with Codonopsis lanceolatae at several concentrations. The effects on tyrosinase activity and melanin contents were examined. And DOPAchrome tautomerase(TRP-2) activity was also examined to search a pathway influencing this inhibitory effect. 1. It was examined mushroom tyrosinase activity was significantly inhibited by Codonopsis lanceolatae. 2. Treatment with Codonopsis lanceolatae did not affect cell viability at the highest concentration, 1 ㎎／ml, and suppressed melanin contents as a time and dose dependent manner. 3. It was investigated treatment with Codonopsis lanceolatae inhibited tyrosinase, a key enzyme forming melanin, activity in a dose-dependent manner. 4. Treatment with Codonopsis lanceolatae did not affect DOPAchrome tautomerase(TRP-2) activity. 5. There was not a morphological change by Codonopsis lanceolatae microscopically. These results suggest that Codonopsis lanceolatae is a candidate for an efficient whitening agent which supresses melanogenesis by a Raper-Mason pathway.

• Journal of Applied Biological Chemistry
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• v.65 no.2
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• pp.93-99
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• 2022

Lysosome organelle extract (LOE) was derived from egg whites. The lysosome is an intracellular organelle that contains several hydrolysis enzymes. Previous studies have reported that LOE performs important functions, such as melanin de-colorization and anti-melanin production in B16F10 melanoma cells. However, its principal molecular and cellular mechanisms have not been elucidated till date. In non-cytotoxic conditions, LOE significantly inhibited α-MSH induced melanin synthesis of murine B16F10 cells. The anti-melanogenic activity of LOE was mediated by suppressing the mRNA expression of tyrosinase enzyme, tyrosinase related protein-1/2 (TRP-1/2), and microphthalmia-associated transcription factor (MITF) genes. By performing western blot analysis, we found that LOE significantly attenuated melanogenesis. In this case, LOE helped in increasing extracellular receptor kinase (ERK) phosphorylation in α-MSH induced B16F10 cells. Furthermore, MITF is found to be a key regulatory transcription factor in melanin synthesis; it was down-regulated by LOE through ERK phosphorylation. In this experiment, PD98059 (MEK inhibitor) was used to check whether LOE directly regulated the activity of ERK. Although LOE exerted inhibitory effect on melanin synthesis, we could not observe this effect in PD98059-treated α-MSH induced B16F10. These results strongly indicate that LOE is related to ERK activation and MITF degradation in anti-skin pigmentation. Hence, LOE should be utilized as a whitening agent of skin in the near future.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.32 no.4 s.59
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• pp.219-225
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• 2006

In this study, we evaluated anti-oxidation, whitening and anti-inflammatory effects of Elsholtzia ciliata extract for use as the cosmeceuticals. Elsholtzia ciliata extracts (30, 70 and 100% methanol extract) exhibited a significant tree radical scavenging effect (up to 80% over 0.025% concentration of 30 and 70% methanol extract, over 0.01% concentration of 100% methanol extract) against DPPH radical generation and showed a significant inhibitory effect (up to 80% over 0.1% concentration) on melanin synthesis in B-16 Melanoma cells. We separated 4 fractions from Elsholtzia ciliata extract (70% methanol extract) by MPLC. The 1st, 2nd, and 3rd fractions showed anti-oxidation (DPPH radical scavenging activity and suppressive effect on Mn-SOD), whitening(inhibitory effect on melanin synthesis) and anti-inflammatory (suppressive effects on $IL-1{\alpha}$, IL-6, COX-2, and total NO synthesis) effects.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.23 no.2
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• pp.63-70
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• 1997

It has been observed that local increase in melanin synthesis or uneven distribution can cause local hyperpigmintation or spot. Pigmentary disorders are caused by various factors, including inflammation, imbalance of hormones, and genetic disorder. Recently the harmfulness of Ultraviolet radiation is increasing due to destruction of ozone layer. Excessive exposure to UV radiation caused post-inflammatory pigmentation. Most women want to avoid uneven skin pigmentation. To satisfy this desire many cosmetic companies have been developing melanogenesis inhibitors and finding promising active agents for use in cosmetic preparations for skin whitening. In cosmetic preparations, many inhibitors such as kojic acid, arbutin, ascorbic acid, and licorice extracts6 have been used as whitening purpose. Plant extracts having an inhibitory effect on melanin formation may be a good choice for cosmetic purpose because of their relatively lower side effects. Therefore, we screened 285 plant extracts for their inhibitory activity in tyrosinase. Of the plant extracts, ramulus mori extracts showed potent tyrosinase inhibition activity. We also identified the active compound in the extract.

• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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• v.24 no.1
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• pp.25-35
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• 2011

Objective : The present study was designed to assess the potential inhibitory activity of an ethanol extract of Belamcandae Rhizoma (EBR) on the alpha-melanocyte stimulating hormone (${\alpha}$-MSH)-induced melanogenesis signal pathway in B16F10 melanoma cells. Methods : Several experiments were performed in B16F10 melanoma cells. We studied tyrosinase activity, melanin content, cell-free tyrosinase activity and DOPA stain, and performed Western blots and RT-PCR for proteins and mRNA involved in melanogenesis. Results : ${\alpha}$-MSH-induced tyrosinase activity and melanin content were inhibited significantly by EBR. EBR markedly suppressed the protein expression level of tyrosinase in B16F10 melanoma cells. On the other hand, the expression of tyrosinase-related protein-1 (TRP-1) and -2 (TRP-2; DCT) were not affected by EBR. To elucidate the mechanism of the depigmenting property of EBR, we examined the involvement EBR in cAMP response element binding (CREB) protein phosphorylation and microphthalmia-associated transcription factor (MITF) signalling induced by ${\alpha}$-MSH. EBR did not regulate CREB phosphorylation and MITF expression by ${\alpha}$-MSH. Nevertheless, the mRNA expression of tyrosinase was significantly attenuated by EBR treatment without changes in the expression of TRP-1 and -2 mRNA. Conclusion : Our study suggested that EBR inhibits ${\alpha}$-MSH-induced melanogenesis by suppressing tyrosinase mRNA.

• Journal of Life Science
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• v.20 no.11
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• pp.1617-1624
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• 2010

Recently, it has been found that Asiasari radix showed a hypopigmenting effect on melanogenesis through activation of mitogen-activated protein kinase (MEK)/extracellular signal-activated kinase (ERK) in B16F10 melanoma cells. However, the hypopigmenting effect of A. radix on the $\alpha$-melanocyte stimulating hormone ($\alpha$-MSH)-stimulated melanogenesis has remained unknown. The purpose of this study was to investigate the inhibitory mechanism of the partially purified A. radix (PPAR)-induced hypopigmentating effects on $\alpha$-MSH-stimulated melanogenesis in B16F10 mouse melanoma cells. PPAR strongly inhibited tyrosinase activity and leads to decreased melanin synthesis in $\alpha$-MSH-stimulated B16F10 melanoma cells. PPAR also decreased the $\alpha$-MSH-induced over-expression of the melanogenic enzymes, tyrosinase, tyrosinase-related protein (TRP)-1, dopachrome tautomerase (Dct) and microphthalmia-associated transcription factor (MITF). We further showed that PPAR inhibits $\alpha$-MSH-induced melanogenesis via phosphorylation of MEK/ERK and PI3K/Akt, and that their activation was blocked by MEK inhibitors, PD98059 and PI3K inhibitors, LY294002 in $\alpha$-MSH-stimulated B16F10 melanoma cells. These results suggest that PPAR inhibits $\alpha$-MSH-induced melanogenesis by activation of MEK/ERK and PI3K/Akt through MITF degradation, which may lead to down-regulation of tyrosinase.