• Journal of Microbiology and Biotechnology
• /
• v.32 no.8
• /
• pp.982-988
• /
• 2022

Licorice (Glycyrrhiza) has been used as preventive and therapeutic material for hyperpigmentation disorders. Previously, we isolated noble compounds including dehydroglyasperin C (DGC), dehydroglyasperin D (DGD) and isoangustone A (IAA) from licorice hexane/ethanol extracts. However, their anti-melanogenic effects and underlying molecular mechanisms are unknown. The present study compared effects of DGC, DGD and IAA on pigmentation in melan-a melanocytes and human epidermal melanocytes (HEMn). DGD exerted the most excellent anti-melanogenic effect, followed by DGC and IAA at non-cytotoxic concentrations. In addition, DGD significantly inhibited tyrosinase activity in vitro cell-free system and cell system. Western blot result showed that DGD decreased expression of microphthalmia-associated transcription factor (MITF), tyrosinase and tyrosinase-related protein-1 (TRP-1) in melan-a cells and HEMn cells. DGD induced phosphorylation of MITF, ERK and Akt signal pathway promoting MITF degradation system. However, DGD did not influence p38 and cAMP-dependent protein kinase (PKA)/CREB signal pathway in melan-a cells. These result indicated that DGD inhibited melanogenesis not only direct regulation of tyrosinase but also modulating intracellular signaling related with MITF level. Collectively, these results suggested a protective role for DGD against melanogenesis.

• Journal of Life Science
• /
• v.28 no.8
• /
• pp.908-916
• /
• 2018

Hair loses melanin with aging, which leads to hair graying. The change in hair color is caused by a reduction in tyrosinase activity and an accumulation of hydrogen peroxide ($H_2O_2$) in hair follicles. The purpose of this study was to investigate the effect of ethanolic extract of Oryza sativa (OREE) on melanin production and antioxidative activity in B16F1 cells. In this study, OREE showed low DPPH radical scavenging activity and reducing power. However, it displayed a strong antioxidative effect against intracellular $H_2O_2$ in live cells. OREE did not inhibit DOPA oxidation activity in vitro, but it increased tyrosinase activity at a concentration of $64{\mu}g/ml$. OREE at a concentration higher than $32{\mu}g/ml$ showed cell toxicity in B16F1 cells. However, OREE at a concentration higher than $8{\mu}g/ml$ not only increased melanin synthesis in a dose-dependent manner in B16F1 cells but also increased melanin synthesis in cells treated with $H_2O_2$ inhibiting melanin synthesis. To confirm the effect of OREE on melanin production, Western blot analysis was performed. The results revealed that OREE increased the expression levels of tyrosine hydroxylase and tyrosinase-related protein-2 (TRP-2) involved in melanin production in the $H_2O_2$-treated cells in which melanin production was inhibited. The findings suggest that OREE could improve melanin synthesis and be available for development of hair cosmetics aimed at improving melanin production.

• BMB Reports
• /
• v.45 no.12
• /
• pp.724-729
• /
• 2012

In this study, we evaluated the anti-melanogenesis effects of Caffeoylserotonin (CaS) in B16 melanoma cells. Treatment with CaS reduced the melanin content and tyrosinase (TYR) activity in B16 melanoma cells in a dose-dependent manner. CaS inhibited the expression of melanogenesis-related proteins, including microphthalmia-associated transcription factor (MITF), TYR, and tyrosinase-related protein-1 (TRP-1), but not TRP-2. ${\alpha}$-MSH is known to interact with melanocortin 1 receptor (MC1R) thus activating adenylyl cyclase and increasing intracellular cyclic AMP (cAMP) levels. Furthermore, cAMP activates extracellular signal-regulated kinase 2 (ERK2) via phosphorylation, which phosphorylates MITF, thereby targeting the transcription factor to proteasomes for degradation. The CaS reduced intracellular cAMP levels to unstimulated levels and activated ERK phosphorylation within 30 min. The ERK inhibitor PD98059 abrogated the suppressive effect of CaS on ${\alpha}$-MSH-induced melanogenesis. Based on this study, the inhibitory effects of CaS on melanogenesis are derived from the downregulation of MITF signaling via the inhibition of intracellular cAMP levels, as well as acceleration of ERK activation.

• ALGAE
• /
• v.30 no.2
• /
• pp.163-170
• /
• 2015

Tyrosinase inhibitors are an important component of cosmetic products. Our previous studies have proposed that eckol isolated from the brown alga Ecklonia cava, can be explored as a tyrosinase inhibitor. However, cellular activities and mechanism of action of eckol remain unknown. Therefore, the current study analyzed the eckol binding modes using the crystal structure of Bacillus megaterium tyrosinase. The effects of eckol on melanin synthesis induced by ${\alpha}$-melanocyte stimulating hormone in B16F10 melanoma cells were also investigated. We predicted the 3D structure of tyrosinase and used a docking algorithm to simulate binding between tyrosinase and eckol. These molecular modeling studies were successful (calculated binding energy value, $-115.84kcal\;mol^{-1}$) and indicated that eckol interacts with Asn205, His208, and Arg209. Furthermore, eckol markedly inhibited tyrosinase activity and melanin synthesis in B16F10 melanoma cells. We also found that eckol decreased the expression of tyrosinase, tyrosinase-related protein (TRP) 1, and TRP2. These results indicate that eckol is a potent inhibitor of melanogenesis, and this finding may be useful for the development of novel pharmaceutical and cosmetic agents.

• Microbiology and Biotechnology Letters
• /
• v.48 no.4
• /
• pp.556-563
• /
• 2020

The purpose of this study was to verify the antioxidant and whitening effects of fermented Ambrosia trifida L. extract (ATFE) and to verify its usefulness as a cosmetic material. The antioxidant effects were measured by assessing the electron-donating capacity and 2,2-azino-bis(3-ethyl-benthiazoline-6-sulfonic acid) (ABTS) radical scavenging ability of these extracts. ATFE was shown to have an electron-donation capacity of 68.4% at a concentration of 1000 ㎍/ml. While its ABTS+ radical scavenging ability was shown to be 58.7% at the same concentration. The ATFE tyrosinase inhibitory effect, which is related to skin-whitening, was shown to be 32.35% at a concentration of 1000 ㎍/ml and a cell viability assay using melanoma cells showed a 14.8% reduction in cell viability at a concentration of 100 ㎍/ml. Surviving cells were then used in western blot analyses to evaluate the protein inhibitory effects of ATFE at 25, 50, 100 ㎍/ml where β-actin was used as a positive control. The whitening effects of these extracts were also evaluated by western blot and show that the expression of microphthalmia-associated transcription factors, Tyrosinase-related proteins (TRP)-1, TRP-2 and Tyrosinase were all inhibited, 51.14%, 55.4%, 38.6%, 83.77% respectively, at 100 ㎍/ml ATFE. The efficacy of the whitening effects was verified and the suitability of ATFE as a cosmetic material was assured.

• Proceedings of the Korean Society of Applied Pharmacology
• /
• 2007.11a
• /
• pp.93-114
• /
• 2007

Vaccinium uliginosum L. (VU) is a flowering plant in the genus Vaccinium has berry fruit. This study was performed to investigate the effect of water extract of Vaccinium uliginosum L. and fractions on inhibition of melanogenesis and wrinkle formation. One hundred grams of the Vaccinium uliginosum L. was extracted with 2,000 mL of water ($90^{\circ}C$, 16h, 2 times). The water extracts were lyophilized and stored at $4^{\circ}C$ until used. Vaccinium uliginosum L. extracts showed scavenger activities on DPPH radical, superoxide anion radical, hydroxyl radical, hydrogen peroxide and singlet oxygen radical, dose dependently. And VU extract and fractions reduced melanin contents on B16F10 melanoma and inhibited the expression of melanogenesis-related proteins, tyrosinase, tyrosinase-related protein (TRP-1) and dapachrometa utomerase (Dct, TRP-2). Moreover VU extract and fractions stimulated procollagen production and inhibited MMP-1 production in human fibroblast. And it decreased degree of wrinkle formation in hairless mouse skin that induced by DVB irradiation for 9 weeks. From the above results, it is possible that Vaccinium uliginosum L. may be developed to be the health functional food and functional cosmetics that have anti-melanogenesis and anti-wrinkle effect.

• Korean Journal of Pharmacognosy
• /
• v.47 no.4
• /
• pp.343-351
• /
• 2016

The purpose of this study was to evaluate the whitening effect of aerial part of Pueraria lobata and mechanisms. Aerial part of Pueraria lobata, dose-dependently reduced the melanin content. Aerial part of Pueraria lobata, significantly decreased cellular tyrosinase activity, while there was not any effect on tyrosinase in cell-free conditions. To elucidate the mechanisms behind the aerial part of Pueraria lobata, treated melanogenesis regulation, the expressions of melanogensis related genes, proteins, and the activity of ${\alpha}-glucosidase$ were determined. Aerial part of Pueraria lobata, significantly inhibited gene and protein levels of MITF, tyrosinase and TRP-1. It suppressed the ${\alpha}-glucosidase$, leading to inhibition on the maturation of tyrosinase. Also aerial part of Pueraria lobata, was observed to have the high antioxidant activity. These results suggested that whitening effect of aerial part of Pueraria lobata, should be due to the down-regulation of MITF, tyrosinase and TRP-1 expression and the intercepting maturation of tyrosinase through suppressing ${\alpha}-glucosidase$. Another should be the high anti-oxidant activity. The findings show the possibility that aerial part of Pueraria lobata, can be used as a potential skin-whitening agent.

• Journal of Life Science
• /
• v.27 no.12
• /
• pp.1452-1461
• /
• 2017

Melanin production by melanocytes in human hair follicles decreases with time and leads to the graying process, which is a phenotype of human aging and an index of aging. The reduction in melanin production is the result of decreased tyrosinase activity in hair follicles and an accumulation of active oxygen species, such as hydrogen peroxide. This study investigated antioxidant effects and melanin-promoting effects in B16F1 cells treated with black sesame ethanolic nonpolar-soluble extract (SBEEO) and black sesame ethanolic polar-soluble extract (SBEEP). In antioxidation experiments, both SBEEP and SBEEO did not eliminate 2, 2-diphenyl-1-picrylhydrazyl (DPPH) radical, but SBEEO at $64{\mu}g/ml$ showed low reducing power. SBEEP exerted cytotoxic effects at concentrations greater than $8{\mu}g/ml$, whereas SBEEO showed cytotoxic effects at concentrations greater than $4{\mu}g/ml$. SBEEP and SBEEO induced melanin synthesis, tyrosinase activity, and DOPA oxidase activity in vitro. In live cells, melanin synthesis was greater in the SBEEP treatment group as compared with that in the SBEEO treatment group. SBEEP stimulated melanin synthesis by modulating the expression of tyrosinase-related protein-2 (TRP-2), which is an important enzyme in melanin synthesis. These results imply that SBEEP obtained from black sesame ethanolic extract may have the potential to improve melanin synthesis.

• Journal of the Society of Cosmetic Scientists of Korea
• /
• v.41 no.1
• /
• pp.21-26
• /
• 2015

The purpose of this study is to identify the whitening effect of Androsace umbellata extract. To discover the anti-pigmentation effective, we investigated Androsace umbellata extract on tyrosinase and melanogenesis inhibition. As results, it reduced tyrosinase activity and melanin contents in B16F1 melanoma cells in a dose-dependent manner with decreased to about 32% at a concentration of $25{\mu}g/mL$. To reveal how it works in inner-cellular level, we performed Western blot method. We found out that it also inhibited the protein expression in tyrosinase, tyrosinase related protein 1 (TRP-1), and microphthalmia associated transcription factor (MITF) in melanocytes. Therefore, we successfully identified the whitening effect of Androsace umbellata extract, and this finding suggested that Androsace umbellata extract is a considerable potent cosmetics ingredient for whitening. Based on this, we anticipated further researches about Androsace umbellata extract for gene levels and additional mechanisms to develop not only for functional cosmetics but for medicines or healthcare food.

• The Korean Journal of Physiology and Pharmacology
• /
• v.22 no.1
• /
• pp.53-61
• /
• 2018

Ethyl linoleate is an unsaturated fatty acid used in many cosmetics for its various attributes, such as antibacterial and anti-inflammatory properties and clinically proven to be an effective anti-acne agent. In this study, we investigated the effect of ethyl linoleate on the melanogenesis and the mechanism underlying its action on melanogenesis in B16F10 murine melanoma cells. Our results revealed that ethyl linoleate significantly inhibited melanin content and intracellular tyrosinase activity in ${\alpha}$-MSH-induced B16F10 cells, but it did not directly inhibit activity of mushroom tyrosinase. Ethyl linoleate inhibited the expression of microphthalmia-associated transcription factor (MITF), tyrosinase, and tyrosinase related protein 1 (TRP1) in governing melanin pigment synthesis. We observed that ethyl linoleate inhibited phosphorylation of Akt and glycogen synthase kinase $3{\beta}$ ($GSK3{\beta}$) and reduced the level of ${\beta}-catenin$, suggesting that ethyl linoleate inhibits melanogenesis through $Akt/GSK3{\beta}/{\beta}-catenin$ signal pathway. Therefore, we propose that ethyl linoleate may be useful as a safe whitening agent in cosmetic and a potential therapeutic agent for reducing skin hyperpigmentation in clinics.