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

• Journal of the Society of Cosmetic Scientists of Korea
• /
• v.39 no.2
• /
• pp.159-166
• /
• 2013

In order to develop new skin whitening agents, we prepared the EtOAc layer (AJE) after enzyme treatment of 75% EtOH extract of the Alnus Japonica Steud. We measured their tyrosinase inhibitory activity in vitro and melanin synthesis inhibitory activity in B16-F1 melanoma cells. They did not show inhibitory activity against mushroom tyrosinase but showed melanin synthesis inhibitory activity in a dose-dependent manner. In a melanin synthesis inhibition assay, AJE suppressed melanin production up to 52% at a concentration of $40{\mu}g/mL$. To elucidate the mechanism of the inhibitory effects of AJE on melanogenesis, we measured expression of melanogenesis-related proteins by the western blot assay. As a result, AJE suppressed the expression of tyrosinase related protein 1 (TRP-1) and microphthalmia associated transcription factor (MITF). Moreover, AJE increased the expression of phosphorylated extracellular signal-regulated kinase (p-ERK). These results conclude that ERK activation by AJE reduces melanin synthesis via MITF downregulation and is subsequent to the inhibition of TRP-1 expression. Therefore, we suggest that AJE could be used as active ingredients for skin whitening.

• Microbiology and Biotechnology Letters
• /
• v.50 no.1
• /
• pp.31-39
• /
• 2022

The purpose of this study was to investigate the whitening effects of hot water (AMPW) and ethanol (AMPE) extracts of Mangifera indica L. peel. To verify the whitening effects, tyrosinase inhibitory activity was measured. 9.51% inhibitory activity, and 35.98% inhibitory activity at 1,000 ㎍/ml. The effects of AMPW and AMPE on cell viability were measured using a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay in B16-F10 melanoma cells. Greater than 95% cell viability was observed at 100 ㎍/ml. Thus, subsequent experiments were performed at concentrations less than 100 ㎍/ml. The whitening effects were confirmed by measuring the protein and mRNA expression levels of microphthalmia-associated transcription factor, tyrosinase, tyrosinase-related protein 1 (TRP-1), and TRP-2, which are factors involved in melanin synthesis. Western blotting and reverse transcription-polymerase chain reaction results confirmed that 100 ㎍/ml AMPW and AMPE showed superior inhibitory effects than the control treatment (alpha-melanocyte stimulating hormone only). Therefore, Mangifera indica L. peel extract had a whitening effect, and thus, has potential as a natural material for use in cosmetics.

• Journal of Life Science
• /
• v.33 no.2
• /
• pp.169-175
• /
• 2023

As a protective defensive mechanism against ultraviolet (UV) light exposure in skin tissue, melanocytes produce the pigment melanin. Tyrosinase plays a key role in melanin production in melanocytes. However, the overproduction of melanin can lead to lesions, such as freckles and dark spots. Thus, it is clinically important to find a modulating molecule to control melanogenesis by regulating tyrosinase expression and/or activity. It is known that catechin, a plant flavonoid, can reduce melano- genesis through the downregulation of tyrosinase expression. Here, we tested whether catechin derivatives isolated from the stem bark of Ulmus parvifolia have an effect on melanin production by regulating tyrosinase in mouse melanoma cells and in vitro mushroom tyrosinase. The catechin derivatives used in this study included C5A, C7A, C7G, and C7X. Treatments using these catechin derivatives reduced melanin production in mouse melanoma B16F10 cells in which melanogenesis was stimulated by α-MSH. Notably, the anti-melanogenic effects of catechin derivatives were similar to those of kojic acid, a well-known anti-melanogenic molecule. Both C5A and C7A directly inhibited the activity of tyrosinase isolated from mushrooms in vitro. Furthermore, our in silico computational simulation showed that these two compounds were expected to bind to the active site of tyrosinase, which is similar to kojic acid. In addition, all four catechin derivatives reduced tyrosinase protein expression. In summary, our results showed that catechin derivatives can reduce melanogenesis by regulating tyrosinase activity or expression. Thus, this study suggests that catechin derivatives isolated from U. parvifolia can be novel modulators of melanin production.

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

• Journal of the Society of Cosmetic Scientists of Korea
• /
• v.37 no.3
• /
• pp.211-218
• /
• 2011

Effects of Kenpaullone, a specific inhibitor of GSK3${\beta}$, on melanin synthesis in B16 melanoma cells and human melanocytes were investigated. Kenpaullone showed a melanogenesis stimulation activity in a concentrationdependent manner in murine B16 melanoma cells and human melanocytes without any significant effects on cell proliferation. Tyrosinase activity was increased 48 h after treatment of B16 cells with Kenpaullone. The protein expression level of tyrosinase was dose-dependently enhanced after the treatment with Kenpaullone. At the same time, the expression level of tyrosinase mRNA was also increased after addition of Kenpaullone. The stimulatory effect of Kenpaullone mainly resulted from increased expression of tyrosinase. These findings suggest that the application of GSK3${\beta}$ inhibitors may be a potential therapeutic agent for the treatment of hypopigmentation disorder.

• KSBB Journal
• /
• v.25 no.1
• /
• pp.18-24
• /
• 2010

Juglans mandshurica belongs to the family Juglandaceae is known to contain a wide range of pharmacological activities including anti-cancer, anti-inflammation, astringent, and anti-human immunodeficiency virus-type 1 (HIV-1). Melanogenesis refers to the biosynthesis of melanin pigment in melanocytes. In this study, to investigate the whitening activity of the extracts from Juglans mandshurica, we measured effects on a tyrosinase activity, a melanogenesis, and a tyrosinase synthesis in the B16/BL6 melanoma cells and an antioxidant activity. The extracts significantly scavenged a 1,1-diphenyl-2-picrylhydrazyl (DPPH) and a superoxide anion radicals in a dose-dependent manner with a $SC_{50}$ value of $20\;{\mu}g/mL$ and $25\;{\mu}g/mL$, respectively. Also, the tyrosinase activity and melanogenesis were significantly inhibited by the extracts. Furthermore, the synthesis of tyrosinase protein was significantly decreased by the extracts in enzyme-linked immunosorbent assay. Double blind study on the clinical efficacy of a cream containing 2% of the extracts showed that the extracts have a significant skin whitening effect. Therefore, this study demonstrates that the extracts from Juglans mandshurica may be useful as a potential agent for skin whitening.

• Journal of Physiology & Pathology in Korean Medicine
• /
• v.22 no.3
• /
• pp.649-653
• /
• 2008

The aqueous extract from Asiasari radix (AEAR) was used to investigate the effect of ${\alpha}$-melanocyte stimulating hormone induced melanogenesis in B16F10 mouse melnoma cells. The treatment with AEAR at the 1.0 and 2.0 mg/ml level significantly inhibited the biosynthesis of melanin without changes of cell growth and morphology compared with untreated control. The AEAR-treated cells at the 2.0 mg/ml level were more efficient than commercial arbutin at 0.1 mg/ml. The tyrosinase activity also significantly decreased in AEAR-treated cells at the 1.0 and 2.0 mg/ml level. The Western analyses confirmed the slightly decreased expression of tyrosinase by AEAR treatment. These results indicate that AEAR may contribute to the inhibition of melanin biosynthesis through regulating tyrosinase activity and expression and serve as a new candidate in the design of new skin-whitening or therapeutic agents.

• Korean Journal of Food Science and Technology
• /
• v.49 no.5
• /
• pp.519-523
• /
• 2017

We investigated the applications of functional materials through the examination of a variety of physiological activities of Ipomoea aquatica extract. I. aquatica extract showed low cytotoxicity against murine melanoma B16F10 cells. At concentrations that exerted little or no cytotoxicity to the cells, I. aquatica extract showed high DPPH radical scavenging activity ($ID_{50}$, $7.84{\mu}g/mL$), inhibited tyrosinase activity ($ID_{50}$, $106.56{\mu}g/mL$), and decreased melanin content ($ID_{50}$, $41.75{\mu}g/mL$). The treatment of B16F10 cells with I. aquatica extract suppressed the protein expression of tyrosinase in a dose-dependent manner. These findings suggested that I. aquatica extract inhibited melanin synthesis in murine melanoma B16F10 cells through the suppression of intracellular tyrosinase expression, as well as the simultaneous direct inhibition of tyrosinase activity. Additionally, I. aquatica extract promoted the expression of involucrin, which is related to skin barrier protection. These results indicate that I. aquatica extract may be an appropriate material for the improvement of skin barrier function.

• Korean Journal of Food Science and Technology
• /
• v.48 no.1
• /
• pp.72-76
• /
• 2016

We investigated the application of functional materials by examining a variety of physiological activities of Geranium krameri extract obtained from the National Institute of Horticultural and Herbal Science. Geranium krameri extract had a low cytotoxicity against murine melanoma B16F10 cells. At concentrations with little or no cytotoxicity, Geranium krameri extract showed high DPPH radical scavenging activity ($IC_{50}$, $8.72{\mu}g/mL$) and anti-microbial activities against Bacillus subtilis, Escherichia coli, and Candida albicans. Additionally, Geranium krameri extract inhibited tyrosinase activity ($IC_{50}$, $456.86{\mu}g/mL$) and decreased melanin content ($IC_{50}$, $50.35{\mu}g/mL$). The treatment of B16F10 cells with Geranium krameri extract suppressed the protein expression of tyrosinase in a dose-dependent manner. These findings suggest that Geranium krameri extract inhibits melanin synthesis in murine melanoma B16F10 cells by suppressing intracellular tyrosinase expression, as well as directly inhibits tyrosinase activity simultaneously.