• Bulletin of the Korean Chemical Society
• /
• v.30 no.2
• /
• pp.475-478
• /
• 2009

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

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

• Journal of Physiology & Pathology in Korean Medicine
• /
• v.21 no.5
• /
• pp.1243-1249
• /
• 2007

The aim of this study was to investigate the effect of ethanol extract of Fagopyrum esculentum on the melanogenesis. To determine whether ethanol extract of Fagopyrum esculentum suppress melanin synthesis in cellular level, B16F10 melanoma cells were cultured in the presence of different concentrations of Fagopyrum esculentum ethanol extract. In the present study, we examined the effects of Fagopyrum esculentum ethanol extract on cell proliferation, melanin contents, tyrosinase activity, expression of melanogenic enzyme proteins including tyrosinase, tyrosinase-related protein 1 (TRP-1) and tyrosinase-related protein 2 (TRP-2). Cell proliferation was slightly increased by treatment with ethanol extract of Fagopyrum esculentum $(25-200 {\mu}g/m{\ell}).$ The ethanol extract of Fagopyrum esculentum effectively suppressed melanin contents at a dose of $100 {\mu}g/m{\ell}).$ It was observed that the color of cell pellets was totally whitened compared with the control. The ethanol extract of Fagopyrum esculentum inhibited tyrosinase activity, regulate melanin biosynthesis as the key enzyme in melanogenesis. Using western blot analysis, the ethanol extract of Fagopyrum esculentum dose-dependently decreased tyrosinase and TRP-1 protein levels, and tyrosinase and TRP-1 were detected in similar manner. ${\alpha}-MSH$ leads to a stimulation of melanin synthesis through increase of tyrosinase activity, melanin contents and cytoplasmic dendricity. In this study, ethanol extract of Fagopyrum esculentum down-regulated the ${\alpha}-MSH$-induced tyrosinase activity, melanin contents and cytoplasmic dendricity. Regarding protein levels of the melanogenic enzymes, the amounts of tyrosinase and TRP-1 was increased after incubation with a-MSH. The treatment of ethanol extract of Fagopyrum esculentum decreased the ${\alpha}-MSH$-induced expression levels of tyrosinase and TRP-1. These results suggest that the ethanol extract of Fagopyrum esculentum exerts its depigmenting effects through the suppression of tyrosinase, TRP-1 and cytoplasmic dendricity. And it may be a potent depigmetation agent in hyperpigmentation condition.

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

• Journal of the Society of Cosmetic Scientists of Korea
• /
• v.27 no.1
• /
• pp.119-131
• /
• 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 the Society of Cosmetic Scientists of Korea
• /
• v.34 no.4
• /
• pp.287-301
• /
• 2008

In order to develop a new depigmenting agent, extracts were obtained from 60 native plants and their antimelanogenic activities were screened by evaluating the inhibitory effect on tyrosinase which is a major enzyme responsibles for the melanin synthesis. The extracts of Trichosanthes kirilowii fruits, Phyllostachys bambusoides inner films (BIF), Clerodendrum trichotomum leaves, and Acer okamotoanum leaves showed relatively high inhibitory effect on tyrosinase and their $IC_{50}$ values were $50{\sim}100{\mu}g/mL$. The extract of BIF inhibited melanin synthesis of B16F10 melanoma cells by 52%, which was the highest among those of various extracts. Furthermore, the effect of BIF extract is 10% higher than that of arbutin (42%), a popular depigmenting agent in Korea. Ten compounds having antimelanogenic activity were isolated from the BIF extract by solvent extraction and chromatography. These compounds were identified as phenolic derivatives: SM701, SM702, SM703, and BPR211 were hydroquinone derivatives; SM707 a gallic acid derivative; SM704, SM705, SM706, SM708 and SM709 ferulic acid derivatives. The free radical scavenging activities of these compounds were measured and compared to those of hydroquinone and vitamin C. The $SC_{50}$ values scavenging 50% DPPH of SM702 and SM709 were $60{\sim}70{\mu}M$ similar to that of hydroquinone and those of SM701 and SM708 were $30{\sim}40{\mu}M$ slightly lower than that of vitamin C. These results suggest the presence of components having high antioxidant activity in the BIF extract. The SM709, identified as 1,2-O-diferulylglycerol, inhibited the activities of tyrosine hydroxylase and dopa oxidase by 18 and 60%, respectively. The SM709 also inhibited the melanin synthesis of B16F10 melanoma cells by 62% and this was the highest antimelanogenic activity among those obtained from the various purified compounds. Therefore, antimelanogenic activity of the BIF extract was concluded to be due to both inhibition of DOPA oxidase and antioxidant activity.

• Proceedings of the SCSK Conference
• /
• 2003.09b
• /
• pp.241-242
• /
• 2003

The effects of N-acetylphytospingosine(NAPS), one of the phytospingosine derivatives, on melanogenesis of B 16F 1 0 mouse melanoma cell lines were investigated. We assessed the effect of NAPS on the depigmentation of B16F10 cells. The melanin content of cells was significantly reduced by NAPS. We examined the inhibitory effect of NAPS on tyrosinase activity using L-dopa as a substrate and the results showed that tyrosinase activity was inhibited in a does-dependent manner. The mRNA level of tyrosinase as well as that of tyrosinase related protein-l (TRP-l) and tyrosinase related protein-2 (TRP-2) genes were not affected by NAPS based on a reverse transcription-polymerase chain reaction (RT-PCR) assay. We also performed a Western blotting analysis using anti-tyrosinase antibody. It showed that there is no change in tyrosinase protein level after treatment of NAPS. These results suggest that the depigmenting mechanism of NAPS in B16F10 melanoma cells involves inhibition of melanosomal tyrosinase activity, rather than the mRNA expression or protein level of tyrosinase.

• Proceedings of the PSK Conference
• /
• 2002.10a
• /
• pp.248.2-248.2
• /
• 2002

This study reports depigmenting potency of 1,3-selenazol-4-one derivatives. which would be based upon the finding of direct inhibition to mushroom tyrosinase. 1,3-Selenazol-4-one derivatives exhibited inhibitory effect on dopa oxidase activity of mushroom tyrosinase. In this study. inhibitory effects of six kinds of 1,3-selenazol-4-one derivatives (3a, 3c, 3d, 3e, 3g and 3i) on mushroom tyrosinase were investigated. (omitted)

• YAKHAK HOEJI
• /
• v.49 no.5
• /
• pp.375-379
• /
• 2005

The green marine algae, Capsosiphon fulvescens is one of the important economic seaweeds cultured in Korea. In this study, we investigated the effects of Capsosiphon fulvescens on melanogenesis using B16 cells. Our results showed that Capsosiphon fulvescens significantly inhibits melanin synthesis and it reduces the activity of tyrosinase, the rate-limiting melanogenic enzyme. Western Blot analysis using anti-tyrosinase antibody revealed that Capsosiphon fulvescens ($10\~40\;{\mu}g/ml$ decreased tyrosinase protein levels. Cell proliferation was dose-dependently inhibited by 10, 20 and 40 ${\mu}g/ml$ Cap­sosiphon fulvescens, without cytotoxicity and morphological change. These results suggest that the depigmenting effect of Capsosiphon fulvescens is correlated with the suppression of tyrosinase activity and protein level, which are key enzymes for melanogenesis.