• Biomolecules & Therapeutics
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• v.29 no.4
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• pp.445-451
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• 2021

Salicylamide, a non-steroidal anti-inflammatory drug (NSAID), is used as an analgesic and antipyretic agent. We have previously shown that several NSAIDs have anti-melanogenic properties in B16F1 melanoma cells. In contrast, we have found that salicylamide enhances melanin contents in B16F1 melanoma cells; however, the underlying mechanism is not known. Therefore, we investigated the mechanism through which salicylamide stimulates melanogenesis. Interestingly, salicylamide enhanced diphenolase activity in a cell-free assay. Western blotting and real-time RT-PCR revealed that salicylamide increased tyrosinase expression via transcriptional activation of the Mitf gene. Together, our results indicate that salicylamide could be used as an anti-hypopigmentation agent for skin and/or hair.

• 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 Plant Resources Society of Korea Conference
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• 2021.04a
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• pp.53-53
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• 2021

Abeliophyllum distichum Nakai (A. distichum), endemic species of Korea, is classified according to the petals and calyx colors. Recently, A. distichum cv. Okhwang 1, which has the golden flower, designated the first official cultivar improved from A. distichum species. The study on the chloroplast genome of A. distichum cv. Okhwang 1 have been reported, but no studies on bioactivity such as antioxidant, anti-inflammatory, and anti-cancer have been progressed. This study was conducted to evaluate the inhibition on melanogenesis of the flower from A. distichum cv. Okhwang 1 (FAO). Antioxidant activity was measured using DPPH and ABTS radical scavenging assays. Inhibition effects on melanogenesis of FAO were confirmed by expression of tyrosinase-related proteins and mRNAs using immunoblotting and RT-qPCR. Tyrosinase is an enzyme that regulates both stimulation and inhibition of melanogenesis. Stimulated MITF in cellular levels increases the expressions of tyrosinase, TRP-1, and TRP-2 to induce melanogenesis. As a result, FAO inhibited the expression of MITF, followed by down-regulated tyrosinase, TRP-1, and TRP-2, which lead to inhibit melanin overproduction. In conclusion, these results indicated that FAO reduced reactive oxygen species (ROS) and markedly inhibited the expression of melanin-related factors. The present study suggested providing that FAO has the potential for development as a functional cosmetic material derived from natural.

• Journal of Applied Biological Chemistry
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• v.65 no.2
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• pp.93-99
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• 2022

Lysosome organelle extract (LOE) was derived from egg whites. The lysosome is an intracellular organelle that contains several hydrolysis enzymes. Previous studies have reported that LOE performs important functions, such as melanin de-colorization and anti-melanin production in B16F10 melanoma cells. However, its principal molecular and cellular mechanisms have not been elucidated till date. In non-cytotoxic conditions, LOE significantly inhibited α-MSH induced melanin synthesis of murine B16F10 cells. The anti-melanogenic activity of LOE was mediated by suppressing the mRNA expression of tyrosinase enzyme, tyrosinase related protein-1/2 (TRP-1/2), and microphthalmia-associated transcription factor (MITF) genes. By performing western blot analysis, we found that LOE significantly attenuated melanogenesis. In this case, LOE helped in increasing extracellular receptor kinase (ERK) phosphorylation in α-MSH induced B16F10 cells. Furthermore, MITF is found to be a key regulatory transcription factor in melanin synthesis; it was down-regulated by LOE through ERK phosphorylation. In this experiment, PD98059 (MEK inhibitor) was used to check whether LOE directly regulated the activity of ERK. Although LOE exerted inhibitory effect on melanin synthesis, we could not observe this effect in PD98059-treated α-MSH induced B16F10. These results strongly indicate that LOE is related to ERK activation and MITF degradation in anti-skin pigmentation. Hence, LOE should be utilized as a whitening agent of skin in the near future.

• Journal of the Korean Applied Science and Technology
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• v.40 no.6
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• pp.1278-1288
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• 2023

Hesperidin(HD) is a a potent antioxidant flavonoid found in various plants. In this study, the recovery of cell death, anti-inflammatory, and melanogenesis inhibitory activities of Hesperidin glucoside (HDG), a water-soluble HD, were compared with HD in vitro. HDG was prepared by an enzymatic glycosylation reaction from HD, and the water solubility of HDG was increased by more than 20,000 times compared to HD. Cell toxicity was significantly lower for HDG than HD. Both HD and HDG increase cell viability in UV damaged HaCaT cells. HD and HDG also reduced an inflammatory mediator such as nitric oxide (NO), and pro-inflammatory cytokines such as tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6) in the cells irradiated with UV, and the reducing effect of HDG was slightly higher than that of HD. In the melanogenesis inhibition assay using the Melanoma B16F10 cells, HDG showed a superior inhibitory activity compared to HD. In conclusion, HDG, a glucosylated product of HD with high water solubility showed more than equal ability of cell recovery and anti-inflammatory potential, and higher melanogenesis inhibition activity compared to HD in vitro.

• Journal of Life Science
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• v.29 no.11
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• pp.1200-1207
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• 2019

Ultraviolet radiation exposure is a major cause of extrinsic skin aging, which leads to skin hyperpigmentation. Loganin, a major iridoid glycoside obtained from Corni fructus, has anti-inflammatory, anti-diabetic, and neuroprotective effects. In this study, we investigated the mechanisms underlying the anti-melanogenic effects of loganin in B16F10 melanocytes treated with ${\alpha}$-melanocyte stimulating hormone (${\alpha}-MSH$) and 3-isobutyl-1-methylxanthine (IBMX). Anti-melanogenic activity was measured by treating cells with loganin at concentrations between 1 and $20{\mu}m$. Cell viability assays confirmed that doses of loganin up to $20{\mu}m$ were not cytotoxic. Loganin significantly and dose-dependently decreased intracellular melanin production. We also investigated potential molecular signaling pathways for the anti-melanogenesis effects of loganin. Western blotting showed that treatment with ${\alpha}-MSH$ and IBMX increased the phosphorylation of cAMP response element-binding protein (CREB) and the gene expressions of microphthalmia-associated transcription factor (MITF) and tyrosinase. Addition of loganin suppressed these increases, while promoting the phosphorylation of extracellular signal regulated kinase (ERK) and the anti-melanogenesis response. Our data therefore indicated that loganin could attenuate the increased melanin synthesis induced by ${\alpha}-MSH$ and IBMX treatment of B16F10 melanocytes. This attenuation appears to occur by downregulation of CREB phosphorylation and MITF and tyrosinase gene expression and upregulation of ERK phosphorylation. These finding suggests that loganin could be a valuable candidate for treatment of skin diseases related to hyperpigmentation.

• Korean Journal of Medicinal Crop Science
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• v.19 no.5
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• pp.388-394
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• 2011

Mume fructus is the roasted fruits of Prunus mume and has been used as traditional chinese medicine. In this study, mume fructus extracts were prepared by three different methods including hot water extract (sample1), fermentation extract using Lactobacillus (Sample2-LP and sample-LA) and ethanol extract (sample3). Total polyphenol and flavonoid contents were improved by fermentation process, compared to water extract. Sample 3 showed the highest activity in DPPH radical scavenging. The cytotoxicity of the sample 2-LP was in the range of 83.3% cell viability at $300{\mu}g/m{\ell}$ concentration. Mume fructus extracts in a concentration-dependent manner inhibited melanogenesis and NO synthesis was inhibited. Specifically, the extracts fermented by L. plantarum (sample2-LP) showed higher anti-oxidant activity, anti-inflammatory and skin whitening activity than other extracts. It suggests that sample 2-LP could be potentially used as a resource of materials for functional cosmetics.

• Microbiology and Biotechnology Letters
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• v.41 no.4
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• pp.433-441
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• 2013

In this study, the anti-oxidative, anti-inflammatory, anti-melanogenic activities of Endlicheria anomala (Nees) Mez methanol extract (EAME) were evaluated by use of in vitro assays and cell culture model systems. The results revealed that EAME scavenges various radicals such as 1,1-diphenyl-2-picryl hydrazyl hydrogen peroxide induced reactive oxygen species, and lipopolysaccharide induced nitric oxide. Furthermore, EAME induced the expression of anti-oxidative enzymes such as heme oxygenase 1, thioredoxin reductase 1, NAD(P)H dehydrogenase 1, and their upstream transcription factor, nuclear factor-E2-related factor 2. Moreover, EAME inhibited in vitro DOPA oxidation and 3-isobutyl-1-methylxanthine induced melanogenesis in B16F10 cells. Its anti-melanogenic activity will have originated from the inhibition of tyrosinase enzyme activity and melanogenesis related protein expression. Taken together, these results provide the important new insight that E. anomala possesses various biological activities such as anti-oxidative, anti-inflammatory, and anti-melanogenic. Therefore, it might be utilized as a promising material in the fields of nutraceuticals and cosmetics.

• Journal of the Korean Society of Food Science and Nutrition
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• v.44 no.7
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• pp.993-999
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• 2015

For the purpose of investigating the in vitro antidiabetic activity of a medicinal herb and herb mixture extracts prepared through traditional antidiabetic prescription, this study examined ${\alpha}$-glucosidase inhibitory activity. Tyrosinase, a type I membrane glycoprotein, is synthesized and glycosylated in the endoplasmic reticulum (ER) and Golgi. The enzyme is subsequently transported to melanosomes, where it participates in melanogenesis. Previous studies showed that disruption of early ER N-glycan processing by an ${\alpha}$-glucosidase inhibitor suppresses tyrosinase enzymatic activity and melanogenesis. According to the results, most oriental medicinal herbal extracts were stronger than acarbose and N-butyldeoxynojirimycin, known as an ${\alpha}$-glucosidase inhibitor. Interestingly, ethyl acetate layer of enzyme hydrolyzed Cheongsimyeonjaeum had an inhibitory effect on melanin synthesis in B16F1 cells, although it did not inhibit tyrosinase activity directly. Together, ${\alpha}$-glucosidase inhibition activity could be used to evaluate anti-melanogenesis, although cross-checking with melanin inhibitory assay is recommended.

• Proceedings of the Plant Resources Society of Korea Conference
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• 2022.09a
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• pp.104-104
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• 2022

Dendropanax morbiferus H. Lev has been reported to have some pharmacologic activities and also interested in functional cosmetics. We found that the water extract of D. morbiferus leaves significantly inhibited tyrosinase activity and melanin formation in α-melanocyte stimulating hormone (MSH)-induced B16-F10 cells. D. morbiferus reduced melanogenesis-related protein levels, such as microphthalmia? associated transcription factor (MITF), TRP-1, and TRP-2, without any cytotoxicity. Two active ingredients of D. morbiferus, (10E)-9,16-dihydroxyoctadeca-10,17-dien-12,14-diynoate (DMW-1) and (10E)-(?)-10,17-octadecadiene-12,14-diyne-1,9,16-triol (DMW-2) were identified by testing the anti-melanogenic effects and then by liquid chromatography-tandem mass spectrometry (LC/MS/MS) analysis. DMW-1 and DMW-2 significantly inhibited melanogenesis by the suppression of protein kinase A (PKA)/cyclic AMP (cAMP)-responsive binding protein (CREB) and p38 MAPK phosphorylation. DMW-1 showed a better inhibitory effect than DMW-2 in α-MSH-induced B16-F10 cells. D. morbiferus and its active component DMW-1 inhibited melanogenesis through the downregulation of cAMP, p-PKA/CREB, p-p38, MITF, TRP-1, TRP-2, and tyrosinase. These results indicate that D. morbiferus and DMW-1 may be useful ingredients for cosmetics and therapeutic agents for skin hyperpigmentation disorders.