• Microbiology and Biotechnology Letters
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• v.49 no.1
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• pp.24-31
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• 2021

This study aimed to investigate the melanogenesis inhibitory activity of epicatechin-3-O-gallate (ECG) isolated from Polygonum amphibium L. ECG was isolated from the ethanol extract of P. amphibium L, and its chemical structure was determined using spectroscopic methods such as LC-ESI-MS, 1D-NMR, and UV spectroscopy. ECG inhibited the melanogenesis of B16F10 cells in a dose-dependent manner. Particularly, it decreased the melanin content by 27.4% at 200 µM concentration, compared with the control, in B16F10 cells, without causing cytotoxicity. It is noteworthy that the expression of three key proteins, including tyrosinase, tyrosinase-related protein-1 (TRP-1), TRP-2, and microphthalmia-associated transcription factor (MITF), involved in melanogenesis, is significantly inhibited by ECG. The ECG isolated in this study caused the inhibition of body pigmentation and tyrosinase activity in vivo in the zebrafish model. These results suggest that the ECG isolated from P. amphibium L. is an effective anti-melanogenesis agent.

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

• Journal of the Society of Cosmetic Scientists of Korea
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• v.48 no.1
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• pp.11-24
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• 2022

It has been reported that the ethanolic extract of the root of Piper methysticum (P. methysticum) inhibits melanogenesis in melanocyte stimulating hormone (MSH)-activated B16 melanoma cells. Flavokawain B (FKB) and Flavokawain C (FKC) isolated from this extract have been found to inhibit melanin production based on anti-melanogenesis activity. This study was designed to find out the inhibition and its process of FKB and FKC on melanin synthesis in melan-a melanocytes. FKB and FKC inhibited melanogenesis at 10 μM, 5 μM respectively in melan-a melanocytes. However, they did not inhibit extracellular tyrosinase activity from melan-a melanocytes. FKB reduced the protein level of tyrosinase (Tyr), tyrosinase-related protein 1 (TRP-1), tyrosinase-related protein 2 (TRP-2), microphthalmia-associated transcription factor (MITF) and the mRNA level of Tyr and TRP-1. FKC reduced the protein level of TRP-2 and MITF and the mRNA level of TRP-1 and Tyr. The reduced expression of Tyr and TRP-1 might be resulted from the decreased MITF which regulates major melanogenic proteins. However, since the mRNA expression of MITF did not change by FKB and FKC treatment, the effects of FKB and FKC on extracellular signal regulating kinase (ERK)/AKT phosphorylation, known to regulate the degradation of MITF, were confirmed. FKB and FKC significantly increased the phosphorylation of ERK1/2, not in AKT. These results suggest that FKB and FKC may be helpful as a potential depigmenting agent for various hyper-pigmentary disorders.

• Journal of the Korean Applied Science and Technology
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• v.38 no.3
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• pp.883-890
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• 2021

In this study, we investigated the melanogenesis inhibitory effects of Rubus crataefifolius Leaf Extract (RCLE) in B16F10 melanoma cells. We examined the effects of RCLE on the melanin contents and tyrosinase activity, as well as the protein expression levels of the melanogenic enzymes TRP-1, TRP-2, and MITF in α-MSH -stimulated B16F10 melanoma cells. RCLE effectively inhibited tyrosinase activity and melanogenesis, suppressed the phosphorylation of PKA and CREB, and expression of MIT involved in the melanogenesis pathway, and down-regulated expression of melanogenesis related proteins. These result suggest that RCLE inhibited α-MSH-stimulated melanin synthesis by suppressing MITF expression. Therefore, our study suggests that RCLE has potential as a safe treatment for excessive pigmentation or as a natural ingredient in cosmetics.

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

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

• Journal of Life Science
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• v.24 no.10
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• pp.1063-1069
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• 2014

Reactive oxygen species (ROS) are known to lead to oxidation of lipids, proteins, and DNA and cause skin damage. Moreover, ROS promote melanogenesis, which causes melasma, age spots, and freckle. The main compounds of the herbal medicines Poria cocas, Glycyrrhiza uralensis, and Ulmus macrocarpa were reported to be parchymic acid, glabridin, and flavonoids, respectively. The aim of this study was to investigate the whitening and antioxidant effects of a mixture of P. cocas, G. uralensis, and U. macrocarpa extracts (PGUE) in B16F1 cells to develop whitening cosmetics. PGUE inhibited DPPH radicals and lipid peroxidation, in addition to high reduction power, compared with Glycyrrhiza uralensis ethylacetate extracts (GUEE). Furthermore, PGUE exhibited a protective effect against DNA oxidation induced by the hydroxyl radicals. In addition to its antioxidant activity, the inhibitory activity of PGUE against tyrosinase, which is associated with melanogenesis, was greater than that of arbutin used as a positive control. Moreover, PGUE exerted an inhibitory effect on melanin synthesis in live melanoma cells and reduced the expression levels of superoxide dismutase-1 (SOD-1) and tyrosinase related protein-1 (TRP-1). These results indicate that PGUE has skin whitening and antioxidant effects, suggesting that this mixture can be used as the main ingredient in the development of effective whitening cosmetics.

• 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.

• Fisheries and Aquatic Sciences
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• v.22 no.5
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• pp.11.1-11.8
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• 2019

Background: In the present study, the skin-whitening effects of a marine-sourced mixture that includes a fucoidanrich extract of Undaria pinnatifida (UPEF), a phlorotannin-rich extract of Ecklonia cava (ECE), and glycosaminoglycans (GAGs) from sea squirt skin were investigated. Methods: The whitening effects of the mixture and its components were evaluated by measuring the inhibition of mushroom tyrosinase and melanin synthesis in alpha-melanocyte-stimulating hormone (${\alpha}$-MSH)-stimulated B16F10 melanoma cells. Results: Each component alone markedly inhibited mushroom tyrosinase in a dose-dependent manner, and in ${\alpha}$-MSH-stimulated B16F10 cells, they inhibited melanin synthesis and were cytotoxic. However, the whitening effects of UPEF, ECE, and GAGs in combination were greater than those of each component alone. A mixture in the ratio of 4:5:1 (UEG-451) showed the strongest activity without cytotoxicity. Further study suggested that UEG-451 inhibits ${\alpha}$-MSH-stimulated melanogenesis in B16F10 cells by downregulating tyrosinase and tyrosinase-related proteins, such as TRP-1 and TRP-2, via the inhibition of MITF expression. Conclusions: These results suggest that mixing the different components at optimum ratios might be an effective way to improve their bioactivities and reduce toxicity and that UEG-451 possesses strong whitening effects that could be used in the cosmetic industry.

• The Korea Journal of Herbology
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• v.38 no.5
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• pp.61-67
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• 2023

Objective : Mori Fructus has been used to relieve thirst, and treat dizziness, tinnitus, and insomnia caused by poor constitution. This study was performed to investigate the protective effect of the ethanol extract of Mori Fructus (MF) in ultraviolet B (UVB)-induced apoptotic cell death in human keratinocyte cells. Methods : MF was prepared by extracting 100 g of Mori Fructus in 1 L of 100% ethanol for 48 h. 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay was used to measure cell viability. Apoptosis was determined by terminal deoxynucleotidyl transferase dUTP nick end labeling (TUNEL) assay, and the expression of apoptosis-related proteins was observed by Western blot. Tyrosinase activity was measured with a colorimetric commercial kit. Results : MF promoted cell vitality and inhibited apoptosis of UVB-induced HaCaT cells. MF pretreatment reduced TUNEL-positive cells and increased the expression of caspase-3 and -9. MF also displayed antioxidant effect with high radical scavenging ability. At 2 ㎎/㎖ concentration, the 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid (ABTS) and 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical inhibition rates were 55.3 ± 4.6% and 48.5 ± 1.3%, respectively. Furthermore, MF showed a concentration-dependent inhibitory effect on tyrosinase. Conclusion : These results suggest that MF functions as a protective regulator in UVB-induced HaCaT cells by regulating apoptosis and partially exerting antioxidant effects. In addition, the tyrosinase inhibitory effect of MF shows the potential for MF to be used for skin pigmentation.