• Journal of the Korean Applied Science and Technology
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• v.36 no.2
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• pp.592-599
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• 2019

This study is to stabilize insoluble and unstable active ingredient which is Idebenone (INCI name: hydroxydecyl ubiquinone) in a multi-lamellar vesicle (MLV) and to stabilize it in the skin care cosmetics. Idebenone is good effective raw material in the treatment of Alzheimer's disease in the medical field and a powerful antioxidant in dermatology. It is well known as a substance that inhibits the formation of melanin and cleans the skin pigment. However, it did not dissolve in any solvent and it was difficult to apply in cosmetic applications. Niosome vesicle was able to develop a nano-particle by making a multi-layer of idebenone encapsulated with a nonionic surfactant, hydrogenated lecithin and glycine soja (soybean) sterols and passing it through a high pressure microfluidizer. Idebenone niosome vesicle (INV) has been developed to have the ability to dissolve transparently in water and to promote transdermal penetration. The appearance of the INV was a yellowish liquid having specific odor, and the particle size distribution of INV was about 10~80 nm. The pH was 5~8 (mean=6.8). This capsulation with idebenone was stored in a $45^{\circ}C$ incubator for 3 months and its stability was observed and quantitatively measured by HPLC. As a result, the stability of the sample encapsulated in the niosome vesicle (97.5%) was about 66.3% higher than that of the non-capsule sample of 32.5%. Idebenone 1% INV was used for the efficacy test and clinical trial evaluation as follows. The anti-oxidative activity of INV was 38.2%, which was superior to that of 12.8% tocopherol (control). The melanin-reducing effect of B16 melanoma cells was better than INV (17.4%) and Albutin (control) (9.6%). Pro-collagen synthesis rate was 128.2% for INV and 89.3% for tocopherol (control). The skin moisturizing effect was 15.5% better than the placebo sample. The elasticity effect was 9.7% better than the placebo sample. As an application field, INV containing 1% of idebenone is expected to be able to develop various functional cosmetic formulations such as skin toner, ampoule essence, cream, eye cream and sunblock cream. In addition, it is expected that this encapsulated material will be widely applicable to emulsifying agents for skin use in the pharmaceutical industry as well as the cosmetics industry.

• Microbiology and Biotechnology Letters
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• v.47 no.2
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• pp.195-200
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• 2019

The purpose of this study was to investigate the melanogenesis inhibiting activity of the ethanol extract from Polygonum amphibium L. Firstly, the n-hexane (Hx), chloroform ($CHCl_3$), ethyl acetate (EA), n-butanol (BuOH), and water (Water) fractions were isolated from the P. amphibium L. ethanol extract. The efficacy of melanogenesis was found to significantly decrease via the EA and BuOH fractions when compared to the control in B16F10 cells. EA particularly showed the lowest melanin content in B16F10 cells when compared to all the other extracts. Concentration-dependent inhibition of melanin synthesis was also observed in the EA fraction at concentrations below $50{\mu}g/ml$, which did not exhibit cytotoxicity in B16F10 cells. Notably, the expression of three key proteins (tyrosinase, tyrosinase-related protein-1 (TRP-1), and TRP-2), which are involved in melanogenesis, were significantly decreased via the EA fraction. EA also inhibited body pigmentation in vivo in a zebrafish model. Overall, we demonstrated melanogenesis suppression using the EA fraction from P. amphibium L., which could be a potential candidate for an antimelanogenesis agent.

• Korean Journal of Food Science and Technology
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• v.54 no.3
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• pp.280-287
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• 2022

The loquat (Eriobotrya japonica) is a fruit tree belonging to the Rosaceae family. Loquat fruit extracts from three cultivars (Tanaka, Mogi, and Jinwang) were prepared using absolute methanol and homogenization and ultrasound sonication procedures. We measured the total phenolic and flavonoid content of the fruit extracts and their antioxidant capacities. In addition, we evaluated tyrosinase activity and anti-melanogenic effects in B16F1 melanoma cells. The fruit extract from cv. Tanaka had the highest total phenolic content and showed the highest antioxidant capacity in the ABTS assay. The loquat fruit extract from cv. Jinwang had the highest total flavonoid content and showed the highest antioxidant capacity in the DPPH assay. Loquat fruit extracts from the Tanaka and Jinwang cultivars effectively inhibited mushroom tyrosinase activity. The loquat fruit extracts reduced intracellular oxidative stress in B16F1 melanoma cells. Treating B16F1 melanoma cells with loquat fruit extract from cv. Tanaka at a concentration of 125 ㎍/mL effectively inhibited melanin synthesis. However, treating the B16F1 melanoma cells with loquat fruit extracts from the Jinwang and Mogi cultivars did not. These results suggest that loquat fruit extracts from the Tanaka cultivar may serve as potential sources of antioxidants and act as a skin-whitening agent.

• 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 Convergence for Information Technology
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• v.12 no.3
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• pp.244-251
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• 2022

This study attempted to investigate the applicability of Geranium maculatum extract as a cosmeceutical ingredient. For this, DPPH, ABTS and FRAP assays were performed to assess radical scavenging activities. To evaluate antioxidant substances, in addition, polyphenol and flavonoid concentrations were measured. Furthermore, cytotoxicity, whitening and anti-inflammatory tests were conducted, using B16F10 and RAW 264.7 cells, and the results found the followings: In the DPPH and ABTS assays, 265.8 mg ascorbic acid/g and 168.5 mg ascorbic acid/g of antioxidant capacities were found respectively. According to the FRAP assay, 1 mg Geranium maculatum extract was same with ascorbic acid 229±9 ㎍ in terms of reducing power. In polyphenol and flavonoid concentrations, 32.989±1.610 mg/g and 11.098±0.261 mg/g were observed each. The above results show that cells survived in the test concentrations more than 80 percent, confirming the low toxicity of Geranium maculatum extract. According to whitening testing, melanin synthesis was reduced depending on concentration, and at the same time, 40.62±2.07% of melanin production inhibition was found at 100 ㎍/mL. In anti-inflammatory testing, inflammation was reduced depending on concentration, and 27.86±2.82% of inhibition of inflammation was detected simultaneously, confirming the applicability of Geranium maculatum extract as a cosmeceutical ingredient.

• Journal of the Korean Society of Food Science and Nutrition
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• v.46 no.1
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• pp.34-38
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• 2017

Myelophycus simplex Papenfuss, a type of brown algae, is known to be majorly distributed in along the southern coast of Korea and Japan. The purpose of this study was to investigate the effects of M. simplex Papenfuss methanol extract (MSPME) on melanogenesis in ${\alpha}$-melanocyte-stimulating hormone-stimulated B16F10 melanoma cells. Melanin contents of B16F10 melanoma cells were decreased by 27, 41, and 59% in a dose-dependent manner, upon MSPME treatment at 100, 300, and $500{\mu}g/mL$, respectively. Tyrosinase activities in B16F10 melanoma cells were decreased by 18, 49, and 61% in a dose-dependent manner, upon MSPME treatment at 100, 300, and $500{\mu}g/mL$, respectively. MSPME suppressed expression of tyrosinase, tyrosinase-related protein-1, tyrosinase-related protein-2, and melanocyte-inducing transcription factor in B16F10 melanoma cells. Concentration of $50{\mu}g/mL$ of MSPME especially induced greater decreases in tyrosinase activity, melanin contents, and melanogenic enzyme protein expressions. This results indicate that MSPME inhibits melanin synthesis and tyrosinase activity, and M. simplex Papenfuss extract may be an ideal candidate as a skin whitening agent.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.35 no.3
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• pp.243-250
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• 2009

To develop a new natural whitening agent for cosmetics, we investigated the inhibitory effects of Poria cocos Bark extracts (PCBE) and its active compound on melanogenesis. PCBE showed ROS scavenging activities in 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical and xanthine/xanthine oxidase system with the $IC_{50}$ values of $19.4{\pm}2.21{\mu}g$/mL and $IC_{50}=103{\pm}3.33{\mu}g$/mL, respectively. PCBE reduced intracellular tyrosinase activity about 34 % at concentration of $50{\mu}g$/mL. And PCBE reduced melanin contents of B16 melanoma cells about 51 % at concentration of $50{\mu}g$/mL without cell cytotoxicity (below $100{\mu}g$/mL). We purified one active compound from PCBE and identified its structure. It was identified as 3-$\beta$-hydroxylanosta-7,9(11),24-trien-4-oic acid, triterpene family, by $^1H$-NMR, $^{13}C$-NMR and Mass analysis. 3-$\beta$-hydroxylanosta-7,9(11),24-trien-4-oic acid showed ROS scavenging activities in DPPH radical and xanthine/xanthine oxidase system with the $IC_{50}$ values of $4.3{\pm}0.15{\mu}g$/mL and $54{\pm}1.67{\mu}g$/mL, respectively. Also, it was shown that 3-$\beta$-hydroxylanosta-7,9(11),24-trien-4-oic acid reduced intracellular tyrosinase activity about 43 % at concentration of $10{\mu}g$/mL. And it inhibited melanin synthesis in a dose dependent manner ($IC_{50}=3.6{\mu}g$/mL) without cell cytotoxicity (below $100{\mu}g$/mL). 3-$\beta$-hydroxylanosta-7,9(11),24-trien-4-oic acid inhibited tyrosinase, TRP-1 and TRP-2 expression at protein level. These results suggest that PCBE and 3-$\beta$-hydroxylanosta-7,9(11),24-trien-4-oic acid reduced melanin formation by the inhibition of tyrosinase activity and expression in B16 melanoma cells. Therefore, we suggest that PCBE could be used as a useful whitening agent.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.35 no.1
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• pp.33-39
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• 2009

To develop a new natural whitening agent for cosmetics, we investigated the inhibitory effects of Pogostemon cablin Bentham extracts (PCE) and its active component on melanogenesis. PCE showed ROS scavenging activities in 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical and xanthine/xanthine oxidase system with the $IC_{50}$ values of $24.2{\pm}2.85{\mu}g/mL$ and $IC_{50}=118{\pm}0.43{\mu}g/mL$, respectively. PCE reduced melanin contents of B16 melanoma cells in a dose-dependant manner and decreased to about 23 % at a concentration of $20{\mu}g/mL$ without cell cytotoxicity (below $100{\mu}g/mL$). And the PCE reduced intracellular tyrosinase activity about 18 % at concentration of $50{\mu}g/mL$. We purified one active compound from PCE and identified its structure. It was identified as patchouli alcohol, sesquiterpene family, by 1H-NMR, $13_C$-NMR, and Mass analysis. Patchouli alcohol also inhibited ROS scavenging activities in DPPH radical and xanthine/xanthine oxidase system with the $IC_{50}$ values of $3.14{\pm}0.12{\mu}g/mL$ and $49{\pm}3.24{\mu}g/mL$, respectively. Patchouli alcohol inhibited melanin synthesis in a dose dependent manner ($IC_{50}=3.9{\mu}g/mL$). And the patchouli alcohol reduced intracellular tyrosinase activity about 40 % at concentration of $10{\mu}g/mL$. Patchouli alcohol inhibited tyrosinase and TRP-2 expression at protein level. These results suggest that PCE and patchouli alcohol reduced melanin formation by the inhibited of tyrosinase activity and expression in B16 melanoma cells. Therefore, we suggest that PCE could be used as a useful whitening agent.

• Journal of Applied Biological Chemistry
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• v.66
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• pp.204-212
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• 2023

Whitening is inhibitory activity of the melanin synthesis of melanocytes. Recently, whitening materials have been developed on natural materials because of its side effects on skin. Figs (Ficus Carica L.) is a fruit belonging to the Moraceae family and whitening activity was reported in focusing on the fig's stem and leaf components, but whitening activity of the figs fruit was not known. Thus, in this study, we tried to observe its anti-melanogenesis as well as antioxidant and anti-inflammation. The radical scavenging activity of figs fruits extract (FFE) was observed as the level of 34.52±1.98%/60.71±1.26% compared to the control in the its maximum concentration in the DPPH/ABTS assay. Cytotoxicity of FFE was observed at 10% concentration by CCK8 assay, so the maximum concentration was set at 5% and applied to all experiments. FFE concentration dependently decreased NO production associated with inducible nitric oxide synthase, cyclooxygenase-2, interleukin-6 and tumor necrosis factor-α gene expression, these strongly suggesting anti-inflammatory activity. In melanin contents assay, FFE significantly down-regulated melanin production in α-MSH-stimulated B16F10 cell as well as tyrosinase inhibition in vitro. In addition, FFE decreased the Microphthalmia-associated transcription factor (MITF) mRNA expression about 94.34% compared to the α-MSH treatment group in RT-PCR. Finally, FFE significantly reduced the MITF, cAMP response element-binding protein and tyrosinase protein expression in the α-MSH stimulated B16F10 cell. Through these results, we found that FFE can not only directly inhibit tyrosinase enzyme activity but also suppress melanogenesis through regulation of MITF gene expression in α-MSH signal transduction.

• Journal of the Korean Applied Science and Technology
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• v.34 no.3
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• pp.623-630
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• 2017

The purpose of this study was to investigate the possibility of applying cosmetic material about extracted from Lycii Fructus seed supercritical fluid. This study was conducted to evaluate the anti-melanogenesis effect and antimicrobial activity about the extracts from Lycii Fructus seed. These researches studied for emulsion physical stability of pH, viscosity, particle size from emulsion containing Lycii Fructus seed extract. As a result, the supercritical fluid extract from Lycii Fructus seed significantly inhibited melanin synthesis by 81.86 % at the concentration $750{\mu}g/mL$. Antimicrobial effects of extract was determined against Staphylococcus aureus, Candida albicans, Escherichia coli. except by Staphylococcus epidermidis. The physical stability of viscosity and pH on the emulsion containing Lycii Fructus seed extract were stable for 28 days. Emulsion containing Lycii Fructus seed extract did not change particles at observation into optical microscope. These results suggest that extracts from Lycii Fructus seed may have value as the potential cosmetic formulation.