• Journal of Life Science
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• v.29 no.3
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• pp.279-286
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• 2019

This study evaluated the anti-oxidant and whitening effects of a 70% ethanol extract of the Sambucus sieboldiana var. pendula (Nakai) (SS). At $1,000{\mu}g/ml$ concentration, the electron donating ability of this SS extract was found to be 86.21% and the ABTS+ radical scavenging ability was 97.9%. In terms of whitening activity, the tyrosinase inhibitory effect of the extract was 37%, also at $1,000{\mu}g/ml$ concentration. To explore the extractefftoxicity to B16F10 melanoma cells, a 3-[4,5-dimethyl-thiazol-2-yl]-2,5-diphenyl-tetrazoliumbromide assay was performed. Results showed 90% or more cells remained viable at $100{\mu}g/ml$ concentration. A Western blot of the SS extract was used to measure microphthalmia-associated transcription factor (MITF), tyrosinase-related protein-1 (TRP-1), tyrosinase relate protein-2 (TRP-2), and the tyrosinase protein expression inhibitory effect at 25, 50, $100{\mu}g/ml$ concentrations; ${\beta}-actin$ was used as a positive control. Consequently, the MITF, TRP-1, TRP-2, and the tyrosinase protein expression inhibitory effect were seen to decrease by 34.5%, 45.6%, 58.4%, and 79.6%, respectively, at $100{\mu}g/ml$ concentration. These were also then measured by reverse transcription-polymerase chain reaction at 25, 50, $100{\mu}g/ml$ concentrations with GAPDH as a positive control. As a result, the SS extract was seen to decrease MITF, TRP-1, TRP-2, and the tyrosinase protein expression inhibitory effect by 85.4%, 67.5%, 85.2%, 67.1%, respectively at the $100{\mu}g/ml$ concentration. We therefore confirmed the possibility of Sambucus sieboldiana var. pendula (Nakai) extract as a whitening material.

• Journal of Life Science
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• v.33 no.5
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• pp.445-454
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• 2023

Hair graying is the result of a malfunction in the signaling pathways that control melanogenesis, and it is activated by UV light, melanocyte-stimulating hormone (MSH), stem cell factor (SCF), Wnt, and endothelin-1 (ET-1). To prevent hair graying, synthetic and natural compounds can be used to stimulate melanogenesis effectively under the control of tyrosinase, tyrosine hydroxylase, tyrosinase-related protein-1 (TRP-1), TRP-2, and microphthalmia-associated transcription factor (MITF). This article describes a crucial strategy to resolve the problem of hair graying, as well as recent advances in the signaling pathway related to melanogenesis and hair graying. In particular, the article reviews potentially effective therapeutic agents that promote melanogenesis, such as antioxidants that modulate catalase, methionine sulfoxide reductase, and sirtuin 1 (SIRT1) activators including resveratrol, fisetin, quercetin, and ginsenoside. It also discusses vitiligo inhibitors, such as corticosteroids, calcineurin inhibitors, and palmitic acid methyl ester, as well as activators of telomerase expression and activity, including estrogen, androgen, progesterone, and dihydrotestosterone. Furthermore, it explores compounds that can inhibit hair graying, such as latanoprost, erlotinib, imatinib, tamoxifen, and levodopa. In conclusion, this article focuses on recent research trends on compounds that promote melanin production related to hair graying.

• Proceedings of the Plant Resources Society of Korea Conference
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• 2023.04a
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• pp.56-56
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• 2023

The cone of Pinus rigida × Pinus taeda (PRT), a plant in the Pinaceae family, has long been used in traditional medicine to treat hemostasis, bruises, and burns. Previous research has shown that regulating oxidation-reduction reactions in reactive oxygen species can help inhibit melanogenesis, the process of melanin synthesis, which is a common target for addressing hyperpigmentation. Inhibiting tyrosinase is also known to be effective in this regard. Based on these findings, we conducted an investigation into the inhibitory effect of the ethyl acetate fraction of PRT (ERT) on melanogenesis in B16 F10 cells. We know that the expression levels of melanin biosynthesis-related proteins, including tyrosinase, TRP-1, and TRP-2, are regulated by MITF (microphthalmia-associated transcription factor) and cAMP, with cAMP affecting the activity of protein kinase A (PKA). PKA can reduce melanogenesis, and CREB reduces the phosphorylation of melanin-producing enzymes. In addition, the MAPK signaling pathway, composed of ERK, JNK, p38, and other factors, is also known to play a role in the inhibition of melanogenesis in melanocytes. Our immunoblotting results showed that ERT inhibited the expression of melanin production-related proteins (tyrosinase, TRP-1, TRP-2, and MITF) that were significantly increased by a-MSH treatment to promote melanin production. Furthermore, the phosphorylation levels of factors related to cAMP/PKA/CREB and MAPK signaling pathways were significantly reduced without affecting the total form. In conclusion, we believe that treatment with ERT can inhibit melanin synthesis by modulating the phosphorylation of cAMP/PKA/CREB and MAPK signaling pathways at the cellular level. These findings suggest the potential of ERT as a raw material for functional cosmetics and pharmaceuticals, thanks to its antioxidant activity and ability to inhibit melanogenesis. We thought that these findings of ERT as a natural plant resource will inspire further research and development in this area.

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

• Journal of Life Science
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• v.28 no.6
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• pp.745-752
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• 2018

Melanogenesis is involved in the pigmentation of the hair, eyes, and skin in living organisms. Various signaling pathways stimulated by ${\alpha}-MSH$, SCF/c-Kit, $Wnt/{\beta}-catenin$, nitric oxide and ultraviolet activate melanocyte, leading to melanin production by tyrosinase, tyrosinase-related protein (TRP)-1, and TRP-2 expressed via the microphthalmia-associated transcription factor (MITF). However, the abnormal regulation of melanogenesis causes dermatological issues such as graying hair and vitiligo. Therefore, the activators that promote melanogenesis are crucial for the prevention of graying hair and the treatment of hypopigmentary disorders. Many melanogenesis stimulators have been studied for the development of novel drugs derived from synthesized compounds and natural products. Here, in addition to providing a description of a common signaling pathway in the melanogenesis of graying hair and the vitiligo process for the development of novel anti-hair graying agents, this article reviews natural herbs and the active ingredients that promote melanin synthesis as a pharmaceutical agent for the treatment of vitiligo. In particular, compounds such as Imatinib and Sugen with a stimulating effect on melanogenesis as a side effect of the drugs, are also introduced. Recent advances in research on natural plant extracts such as Polygonum multiflorum, Rhynchosia Nulubilis, Black oryzasativa, and Orysa sartiva, widely known as traditional and medicinal extracts, are also reviewed.

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

• Journal of Physiology & Pathology in Korean Medicine
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• v.34 no.2
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• pp.67-74
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• 2020

The objective of this study is to investigate the skin whitening and antioxidant effects of the Anemarrhenae Rhizoma extract (ARE). Following the previously studied method, we examined the inhibitory effects of melanin synthesis and tyrosinase activity by using B16F10 cells. First, we measured the Diphenylpicrylhydrazyl (DPPH) assay, nitrite scavenging activity, and superoxide dismutase-like activity to verifying antioxidant efficacy according to skin whitening. In addition, we confirmed the skin whitening efficacy of ARE by measuring gene expression associated with a skin whitening by the Reverse transcription polymerase chain reaction (RT-PCR) method in B16F10 cells. In this study, we confirmed that ARE has skin whitening and antioxidant effects at high concentrations. In particular, ARE at a concentration of 500 ㎍/ml inhibited the expression of Tyrosinase, TRP-2 (tyrosinase-related protein), and MITF (microphthalmia transcription factor) genes better than Arbutin. In conclusion, our results confirmed that ARE has the potential for development as a skin whitening efficacy substance.

• Korean Journal of Pharmacognosy
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• v.47 no.4
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• pp.343-351
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• 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 Microbiology and Biotechnology
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• v.30 no.8
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• pp.1184-1194
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• 2020

Melanin is a major factor that darkens skin color as one of the defense systems to prevent the harmful effects of UV light. However, darkened skin from the localized or systemic accumulation of melanin is viewed in many cultures as an esthetic problem. Consequentially, searching for anti-melanogenic agents from natural sources is very popular worldwide. Previous screening of fermented rice products, obtained from various rice cultivars fermented with different sources of loog-pang (Thai traditional fermentation starter), revealed that the highest ability to reduce the melanin content in B16F10 melanoma cells was from unpolished black rice fermented with a defined starter mixture of microbes isolated from loog-pang E11. The aim of this study was to investigate the mechanism of the fermented unpolished black rice (FUBR) on the inhibition of melanogenesis in B16F10 melanoma cells. The strongest reduction of cellular melanin content was found in the FUBR sap (FUBRS). The melanin reduction activity was consistent with the significant decrease in the intracellular tyrosinase activity. The FUBRS showed no cytotoxic effect to B16F10 melanoma or Hs68 human fibroblast cell lines. It also significantly reduced the transcript and protein expression levels of tyrosinase, tyrosinase-related protein 1 (TYRP-1), TYRP-2, and microphthalmia-associated transcription factor. Furthermore, it induced a significantly increased level of phosphorylated ERK, p38 and Akt signaling pathways, which likely contributed to the negative regulation of melanogenesis. From these results, a model for the mechanism of FUBRS on melanogenesis inhibition was proposed. Moreover, these results strongly suggested that FUBRS possesses anti-melanogenesis activity with high potential for cosmeceutical application as a skin depigmenting agent.

• Microbiology and Biotechnology Letters
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• v.47 no.1
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• pp.148-157
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• 2019

A 70% ethanol extract of Erigeron annuus (L.) Pers. was investigated for its whitening activity for application as a functional ingredient in cosmetic products. At the E. annuus extract concentration of $100{\mu}g/ml$, the electron-donating ability was found to be 67.83%, the tyrosinase inhibitory effect (related to skin-whitening) was 69%, the elastase inhibitory effect (related to skin-wrinkling) was 69%, and the astringent effect was 80%. The $ABTS^+$ radical-scavenging ability was 87% at the $500{\mu}g/ml$ concentration. In the cell viability test measured on melanoma cells, 96% of the cells treated with $100{\mu}g/ml$ of the extract were viable. According to the western blot results, the protein expression of the microphthalmia-associated transcription factor (MITF), tyrosinase, tyrosinase-related protein (TRP)-1, and TRP-2 was decreased by 60.22%, 47.83%, 54.79%, and 67.88%, respectively, at the extract concentration of $100{\mu}g/ml$. The protein expression of phosphorylated extracellular signal regulated kinase (p-ERK) and phosphorylated cAMP response element-binding protein (p-CREB) was decreased with increasing concentrations of the extract. Reverse transcription-polymerase chain reaction of the extract showed that the mRNA expression of MITF, tyrosinase, TRP-1, and TRP-2 was decreased by 86.51%, 85.22%, 74.26%, and 66.66%, respectively, at $100{\mu}g/ml$ extract concentration. The findings suggest that the 70% ethanol extract from E. annuus (L.) Pers. has potential as a cosmeceutical ingredient with whitening effect.