• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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• v.17 no.1
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• pp.94-103
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• 2004

Objective: This study was performed to detennine the depigmenting effects of Kamibongpungtongsung-San. Methods: To determine the depigmenting effects of Kamibangpungtongsung-San. we measured the degree of tyrosinase inhibition, melanin production & cell viability in cultured B16 melanoma cells, UV screen and cytoprotective effects on PC12 cells injured by hydrogen peroxide. Results: Komibangpungtongsung-San did not show inhibitory effects on melanin production in melanoma cells, UV screen and cytoprotective effects on PC12 cells injured by hydrogen peroxide. However it showed mild inhibitory effects on tyrosinase activity. Conclusion : This study shows that Kamibangpungtongsung-San, a generally used prescription for dermatologic diseases, do not have depigmenting effects via tyrosinase inhibition. Therefore, the depigmenting effect and mechanism of depigmentation by Kamibangpungtongsung-San need to be evaluated and investigated in other directions.

• Korean Journal of Medicinal Crop Science
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• v.16 no.3
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• pp.192-194
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• 2008

In our previous study, ethylacetate fraction of white ginseng (root of Panax ginseng C.A. Meyer) extract inhibited mushroom tyrosinase activity and melanin production in melanocytes. This study examined its effects on the expression of melanin biosynthesis-related enzymes to explore the depigmenting pathway. Moreover, depigmenting effect on animal skin was examined using UV-B induced hyperpigmented skin of brown guinea pigs. The ethylacetate fraction of the white ginseng extract exhibited depigmenting activity in the skin of brown guinea pig without visible edema. In addition, this fraction reduced tyrosinase expression in melanocytes. The results suggested that ethylacetate fraction of white ginseng extract might be used as skin depigmenting material by inhibition of tyrosinase activity and expression.

• Proceedings of the SCSK Conference
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• 2003.09b
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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.

• 한국생물공학회:학술대회논문집
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• 2003.10a
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• pp.319-319
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• 2003

• Korean Journal of Food Science and Technology
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• v.44 no.1
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• pp.76-81
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• 2012

The objective of the present study was to evaluate the skin depigmentation effect of the extracts of three herbs, Carthamus tinctorius seed, Cyperus rotundus and Schizonepeta tenuifolia. Their effects on tyrosinase and melanin synthesis inhibitory action were assessed. We found that the C. tinctorius seed ethanol extracts reduced the tyrosinase activity and melanin formation of B16F10 melanoma cells. The C. tinctorius seed suppressed the expression in microphthalmia associated transcription factor (MITF), tyrosinase, tyrosinase related protein 1 (TRP-1), and tyrosinase related protein 2 (TRP-2) in B16F10 melanoma cells. These results show that C. tinctorius seed inhibited melanogenesis on the B16F10 melanoma cell. The underlying mechanism of C. tinctorius seed whitening activity may be the inhibition of tyrisinase, MITF, tyrosinase, TRP-1, and TRP-2 expression. The results suggested that C. tinctorius seed has considerable potential as a natural functional ingredient with a depigmentation effect.

• Biomolecules & Therapeutics
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• v.22 no.5
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• pp.431-437
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• 2014

Synthetic compounds that are used in the clinic to regulate skin hyperpigmentation, such as arbutin, hydroquinone, and kojic acid, are only moderately effective. But, their use is limited by side effects. As part of an effort to overcome the limitations, we developed resveratrol-enriched rice (RR) using genetic engineering technique. Each of resveratrol and rice has been reported to produce anti-melanogenic effects. Therefore, we hypothesized that RR would show more anti-melanogenic effects than those of resveratrol or rice alone. Anti-melanogenic effect of RR was done by using melan-a mouse melanocytes. The depigmenting efficacy was then observed following topical application of the RR to UVB-stimulated hyperpigmented dorsal skin of guinea pigs. Treatment with RR extract resulted a $21.4{\pm}0.7%$ decrease in tyrosinase expression at melan-a cells. Colorimetric analysis showed a significantly lower depigmenting value by day 9 following treatment with RR in UVB-irradiated guinea pigs the dorsal skin (p<0.01), indicating that RR produced a depigmentation effect. By staining with Fontana-Masson stain, we found that the RR-treated group had more effect histopathologically in epidermal melanin production than resveratrol or rice alone-treated group. RR was associated with reduction in the levels of microphthalmia-associated transcription factor (MITF), and downregulation of tyrosinase and tyrosinase-related protein (TRP-2) expression, leading to inhibit epidermal melanin production by western blot analysis. This study suggests that the resveratrol-enriched rice may be a promising candidate in regulating skin pigmentation with UVB exposure.

• Journal of Physiology & Pathology in Korean Medicine
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• v.19 no.3
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• pp.662-670
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• 2005

Recently many efforts were focused to understand the mechanical insights of melanogenesis to develop the agents for hyper-pigmentation and hypo-pigmentation. In the melanin bio-synthetic pathway, tyrosinase is the rate limiting enzyme, and ${\alpha}$-melanocyte stimulating hormone(MSH) stimulates melanogenesis and enhances the melanin synthesis and the tyrosinase activity. The author has analyzed the effects of Biota Orientalis Folium on the basal melanogenic activities of B16 mouse melanoma cells, and on the ${\alpha}$-MSH or tyrosinase-induced melanogenesis. Biota Orientalis Folium alone markedly suppressed melanin content and tyrosinase activity in a dose-dependent manner. The decrease of cell propagation was observed in B16 cells treated with 200${\mu}$g/ml dose of Biota Orientalis Folium, indicating that Biota Orientalis Folium-induced depigmenting effect was caused by inhibition of melanin synthesis, not due to destruction of B16 cells. Pretreatment of the cells with Biota Orientalis Folium also suppressed the increase of ${\alpha}$-MSH (10 nM) induced melanin content and tyrosinase activity. Biota Orientalis Folium inhibited the revelation of ${\alpha}$-MSH induced tyrosinase protein and tyrosinase related protein and mRNA of tyrosinase in B16 melanoma cell. These results suggest that Biota Orientalis Folium inhibits melanogenesis and abrogates ${\alpha}$-MSH and tyrosinase-induced melanogenesis in B16 melanoma cells.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.27 no.1
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• pp.119-131
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• 2001

Exposure of the human skin to UV-light can cause sun-tanning, photoaging and even photo-carcinogenesis. Melanin is important in protecting the skin against UV damage, but excessive or uneven melanin production can lead to the formation of freckles and aged spot. Control of hyperpigmentation is becoming even more important as aged population continues to grow. These needs led us to develop effective and safe depigmenting-agent, kojyl 3-aminopropyl phosphate (kojyl-APPA), called Whitegen. The development of whitegen was based on the fact that phosphate group of 3-aminopropyl phosphate can make kojic acid more compatible to the skin membrane and more stable. Instability of kojic acid has been a problem in cosmetic use. The insertion of phosphoester group has been recognized as a powerful tool to improve such physical properties as solubility and stability, because the phosphodiester residue is well characterized as a non-toxic moiety, having a high affinity for cell membranes. Kojyl-APPA showed no tyrosinase inhibition effect compared to kojic acid in vitro, but showed tyrosinase inhibition effect in situ. It means that kojyl-APPA is converted to kojic acid enzymatically in cells. Kojyl-APPA showed the inhibitory activity on melanin synthesis in mouse melanoma and normal humal melnaocytes and also showed long-lasting stability in comparison with its original form (kojic acid). Kojyl-APPA showed depigmenting effects when applied to UVB-induced hyperpigmentated region of guinea pig skin. Based on these results, kojyl 3-aminopropyl phosphate can be used as a safe and effective ingredient for the brightness and cleanness of skin.

• Journal of Life Science
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• v.32 no.5
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• pp.355-361
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• 2022

Melanin pigments are the main cause of skin color. They are produced in melanocytes and then transferred to keratinocytes, which eventually gives the skin surface a variety of colors. Although many skin-lightening or depigmenting agents have been developed, the demand for materials to reduce pig- mentation is still increasing. Here, we tried to find materials for skin-lightening or depigmentation using natural compounds and found that mistletoe (Viscum album var. coloratum) extracts (ME) had an inhibitory effect on tyrosinase activity. As a result, ME significantly reduced pigmentation in human primary melanocytes. In addition, a promoter reporter assay revealed that ME inhibited the transcription of microphthalmia-associated transcription factor (MITF), melanophilin (MLPH), tyrosinase-related protein-2 (TRP-2), and tyrosinase (TYR) genes in HM3KO melanoma cells. In addition, ME decreased the protein level for pigmentation-related molecules, such as TYR and TRP-1. Furthermore, it markedly inhibited the melanogenesis of zebrafish embryos, an in vivo evaluation model for pigmentation. To elucidate the action mechanism of ME, we investigated its effects on intracellular signaling. Eventually, the ME dramatically decreased the phosphorylation of the cAMP responsive element binding protein (CREB), AKT, and ERK. The data suggest that ME may inhibit the melanogenesis pathway by regulating the signaling pathway related to pigmentation. Taken together, these data propose that ME can be developed as a depigmenting or skin-lightening agent.

• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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• v.16 no.2
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• pp.96-118
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• 2003

The effect of Glycyrrhizae Radix water extract, known as depigmenting agent, on melanin biosynthesis was investigated in cellular level by using B16 mouse melanoma cells. The inhibitory effect of Glycyrrhizae Radix water extract on melanogenesis was determined by mushroom tyrosinase assay traditionally using in vitro screening test. To determine whether Glycyrrhizae Radix water extract suppress melanin synthesis in cellular level, B16 mouse melanoma cells were cultured in the presence of different concentrations of Glycyrrhizae Radix water extract. Effects on cell proliferation, melanin biosynthesis, tyrosinase activity, DOPAchrome tautomerase activity, and expression level of mRNA for tyrosinase were examined. The maximum concentration of Glycyrrhizae Radix water extract that was not inhibitory to growth of the cells was 2 mgml. At that concentration, melanin synthesis was significantly inhibited without cytotoxicity after 5 days, compared with untreated cells. The treatment with Glycyrrhizae Radix water extract reduced tyrosinase and DOPAchrome tautomerase activity in a dose-dependent manner. However, the treatment with Glycyrrhizae Radix water extract did not affect significantly mRNA levels for tyrosinase. These results suggest that the inhibitory effect of Glycyrrhizae Radix water extract on melanogenesis is correlated with the suppression of tyrosinase and DOPAchrome tautomerase activity more than altering mRNA levels of tyrosinase.