• Natural Product Sciences
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• v.22 no.3
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• pp.193-200
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• 2016

This study describes the anti-inflammatory, anti-oxidant, and melanogenesis inhibition activities of methanol extract and various organic solvent fractions of Arecae Pericarpium. We examined the inhibition of lipopolysaccharide (LPS)-induced nitric oxide (NO) production in RAW 264.7 cells, 1,1-diphenyl-2-picrylhydrazine (DPPH) scavenging activity, mushroom tyrosinase inhibition activity and melanin contents. The study showed that, among all tested fractions, methylene chloride fraction showed the strongest inhibition of LPS-induced NO production in RAW 264.7 cells ($IC_{50}$ value $8.89{\mu}g/mL$) and DPPH radical scavenging activity ($EC_{50}$ value $21.39{\mu}g/mL$). Methylene chloride and ethyl acetate fractions similarly inhibited mushroom tyrosinase activity. Methanol extract exhibited strongest reduction of melanin content in B16F10 melanoma cells. Based on the bioactivity assay results, methylene chloride and ethyl acetate fractions were further separated. Eight phenolic compounds were isolated, which are dimeric syringol (1), catechol (2), 4-hydroxybenzaldehyde (3), vanillin (4), 4-hydroxyacetophenone (5), apocynin (6), protocatechuic acid (7) and 4-hydroxybenzoic acid (8). Among the isolated compounds tested, catechol showed the strongest inhibition of LPS-induced NO production in RAW 264.7 cells. Catechol also showed the concentration-dependent NF-${\kappa}B$ inhibition activity. Arecae Pericarpium might have potentials to be developed as anti-inflammatory agent or dermatological product for skin-whitening agent.

• YAKHAK HOEJI
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• v.58 no.1
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• pp.21-27
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• 2014

We have developed 8 peptide derivatives as potential MC1R antagonists and their inhibitory effects on ${\alpha}$-MSH induced cell growth in cultured normal human melanocytes (NHM) were investigated. From these experiments, the two most potent peptide derivatives, 5-phenylvaleric acid-(D)His-Arg-Trp-$(Lys)_6NH_2$ (P 6) and 5-phenylvaleric acid-(D)His-Arg-Trp-$(Lys)_9NH_2$ (P 7) were selected for further studies. In ${\alpha}$-MSH depleted NHM cells, we have found that the treatment with 1 ${\mu}M$ of these two peptide derivatives, P 6 and P 7, inhibited the cell proliferation induced by the addition of 1 nM ${\alpha}$- MSH by 70% and 72%, respectively. In NHM cells without previous ${\alpha}$-MSH depletion, 1 ${\mu}M$ treatment in the presence of 10 nM ${\alpha}$-MSH resulted in 70% (P 6) and 80% (P 7) decrease in cell growth and 64% (P 6) and 71% (P 7) reduction in melanin synthesis, respectively. The peptide derivatives P 6 and P 7 were proved to have no apparent cytotoxicity and inhibited the elevation of intracellular cAMP concentration triggered by ${\alpha}$-MSH. In conclusion, our data suggest that the peptide derivatives reported in this study, 5-phenylvaleric acid-(D)His-Arg-Trp-$(Lys)_6NH_2$ (P 6) and 5-phenylvaleric acid-(D)His- Arg-Trp-$(Lys)_9NH_2$ (P 7) strongly antagonize ${\alpha}$-MSH, inhibit cell proliferation and melanin synthesis, and lower the intracellular cAMP concentration, hence have a promising potential as a novel skin lightening agent.

• Molecules and Cells
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• v.38 no.2
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• pp.163-170
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• 2015

Lipoteichoic acid (LTA) is a major component of the cell wall of Gram-positive bacteria. Its effects on living organisms are different from those of lipopolysaccharide (LPS) found in Gram-negative bacteria. LTA contributes to immune regulatory effects including anti-aging. In this study, we showed that LTA isolated from Lactobacillus plantarum (pLTA) inhibited melanogenesis in B16F10 mouse melanoma cells. pLTA reduced the cellular activity of tyrosinase and the expression of tyrosinase family members in a dose-dependent manner. The expression of microphthalmia- associated transcription factor (MITF), a key factor in the synthesis of melanin, was also decreased by pLTA. Further, we showed that pLTA activated melanogenesis signaling, such as extracellular signal-regulated kinase (ERK) and phosphatidylinositol 3-kinse (PI3K)/AKT. In addition, the expression of heterogeneous nuclear ribonucleoprotein A1 (hnRNP A1) and HuR, which are important RNA-binding proteins (RBPs), was reduced. pLTA likely degrades MITF via regulation of melanogenic signaling and RNA stability of melanogenic proteins, resulting in the reduction of melanin. Thus, our data suggest that pLTA has therapeutic potential for treating hyperpigmentation disorders and can also be used as a cosmetic whitening agent.

• The Korean Journal of Physiology and Pharmacology
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• v.25 no.1
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• pp.15-26
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• 2021

Peptides are short chain of amino acids linked by peptide bonds. They are widely used as effective and biocompatible active ingredients in cosmetic industry. In this study, we developed novel peptide mixture and identified its anti-pigmentation effect on melanocytes and keratinocytes. Our results revealed that peptide mixture inhibited melanosome biogenesis through the regulation of microphthalmia-associated transcription factor, a key factor of melanogenesis in melanocytes. And we observed that peptide mixture inhibited melanosome uptake through the reduction of protease-activated receptor 2, a phagocytosis-related receptor in keratinocytes. Furthermore, peptide mixture activated autophagy system resulting in degradation of transferred melanosomes in keratinocytes. The anti-pigmentation effect of multi-targeting peptide mixture was assessed in a human skin equivalent model (MelanoDerm). Melanin contents in epidermal layer were significantly decreased by topical treatment of peptide mixture, suggesting that it can be applied as a novel cosmetics material having a whitening function.

• Journal of the Korean Applied Science and Technology
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• v.34 no.2
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• pp.382-393
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• 2017

In this study, it studies about Phytosphingosine (PhS) and Phytosphingosine-1-phosphate(PhS1P), and it tries to confirm the effect through anti-inflammatory, anti-melanin, MMP-1 revelation inhibition, and Western blot analysis experiment after grasping toxicity about 3 cells by using B16F10 melanin cell, RAW264.7 macrophage, and HDF fibroblast in order to find out whether it is possible to use as cosmetic material or not by studying biological activity in terns of skin care. As a result of this experiment, it confirmed that toxicity about B16F10, RAW264.7, HDF cell is low, and PhS1P appeared stronger inhibition activity than PhS in anti-inflammatory NO inhibitory activity experiment. MMP-1 revelation was greater in PhS1P, and it confirmed that the mechanism is due to reduction in ERK activity. On the other hands, melanin generation inhibitory activity is better than arbutin, and it confirmed that the mechanism is due to inhibition of revelation of MTF and Tyrosinase. In a nutshell, PhS and PhS1P that are bioactive substance may confirm the possibility to be used as functional cosmetic for wrinkle and skin improvement of whitening cosmetic.

• 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 the Society of Cosmetic Scientists of Korea
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• v.36 no.2
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• pp.137-143
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• 2010

Yuza (Citrus junos Sieb ex TANAKA) is a citrus fruit that is cultivated in northeast Asia. Citron is known for containing abundant antioxidants such as vitamin C, flavonoids, for example hesperidin and hesperetin, and terpenoids such as limononin. When mature citron is processed for tea or other beverage food products in Korea, massive amounts of seeds and pericarp are remained as waste. This study aimed to exploit the processed remnant of Citron for developing functional cosmetic applications. Ethanol extracts of Yuza seed and pericarp did not show significant radical scavenging activities measured by DPPH (2,2-diphenyl-1-picrylhydrazyl) method. But they contained significantly high phenolic compounds. Cultured human dermal fibroblasts and HaCaT keratinocytes were irradiated with 25 mJ UVB and the citron extracts were added to the medium of each culture. Cellular damages caused by UVB irradiation were prevented by the addition of the Yuza extract. In addition, the reduction of the enhanced MMP-1 expression after irradiation of UVB in human dermal fibroblasts was observed. Also the increased level of pro-inflammtory TNF-$\alpha$ in the UVB irradiated HaCaT cells was decreased. The collagen expression was enhanced by the extract. Yuza extract markedly inhibited melanin production from $\alpha$-MSH treated B16F1 melanoma cells. Melanin assay, tyrosinase zymography results indicated that Yuza extract had strong depigmenting activity. In conclusion, Yuza ethanol extracts have good anti-photoaging and strong anti-melanogenic efficacies.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.41 no.1
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• pp.85-96
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• 2015

Forsythia fructus has been shown to have antioxidative, anti-inflammatory, antibacterial, anti-aging and whitening effects. This work was carried out to investigate the anti-aging effects of Forsythia viridissima-prescription extracts (Yeongyoseungma-tang, Gamiyeongyoseungma-tang, Hoechunyangkyeok-san) on skin. Skin anti-aging effect of Forsythia viridissima-prescription extracts (Yeongyoseungma-tang, Gamiyeongyoseungma-tang, Hoechunyangkyeok-san) was evaluated by using antioxidant assay, anti-glycation activity, inhibitory effect of tyrosinase activity, expression of type I procollagen and UVA-induced matrix metalloproteinase-1 on HS68 cells, and reduction of ${\alpha}$-MSH-induced melanin on B16F1 cells. Forsythia viridissima-prescription extracts showed anti-oxidative and anti-glycation activity. The pectinex hydrolysed extract from Yeongyoseungma-tang 75% EtOH extract and Gamiyeongyoseungma-tang 75% EtOH extract increased the type I procollagen synthesis, and decreased the UVA-induced MMP-1 expression on HS68 cells. The pectinex hydrolysed extracts of Hoechunyangkyeok-san 75% EtOH extract had the inhibitory effect of melanin synthesis on B16F1 cells. Based on these results, we suggest that Forsythia viridissima-prescription extracts may be useful as a potential source of functional anti-aging cosmetics.

• Journal of Life Science
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• v.30 no.5
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• pp.428-433
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• 2020

In this study, we created pupal stage extracts of Apis mellifera L. drones for use in cosmetic materials. The effect of the drone pupae extract (DPE) on HDF cells was assessed for analysis of anti-wrinkle activity by collagen or collagenase gene expression, and the skin-lightening effect was studied by in vitro tyrosinase inhibition and B16F10 melanoma assay; the two cells were found to be non-cellular when the concentration of DPE was 100 ㎍/ml. Albutin concentration (positive control) in the whitening test was set at a capacity of 100 ug/ml and m-melanocyte stimulating hormone (α-MSH). A melanin-producing induction material was set at a concentration of 100 nM, and the expression of collagen type I and MMP1 collagenase was measured using HDF cells. MMP1 expression was seen to reduce in a concentration-dependent manner in treatment with DPE. Inhibiting melanin generation with B16F12 cells indicated a tendency to decrease in the DPE treatment group. Both L-Tyrosine and L-DOPA as DPE were used in an in vitro tyrosinase induction test to demonstrate the effects of tyrosinase suppression on concentrations. The higher the concentration of DPE, the greater the wrinkle reduction and whitening effect. In conclusion, it was found that DPE is an effective smoothing and whitening material by increasing collagen generation and inhibiting collagenase expression and reducing melanin production.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.47 no.4
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• pp.341-352
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• 2021

Acerola is an excellent ingredient because of its high natural vitamin C content, but it is difficult to stabilize and has hardly been studied as a cosmetic material. Therefore, this study developed a mixed liposome preparation for stabilizing acerola extract. As a safety test, the skin irritation test was evaluated by BCOP assay and HET-CAM assay. We evaluated the inhibition of tyrosinase activity, the whitening effect of melanin production, and the wrinkle effect of prochloragentype-I C-peptide production, and confirmed the possibility of functional cosmetics. In addition, a cream of liposomes containing acerola extract mixture was developed to evaluate the clinical studies of skin wrinkles and whitening. BCOP assay, HET-CAM assay and human skin primary irritation test results of liposomes containing acerola extract mixture showed no irritation and were safe from skin and eye. The result of tyrosinase activity by 75.8% at 1,000 ㎍/mL. As a result of the melanogenesis inhibition test, liposome with acerola extract showed the melanin content by 46.2% at 1,000 ㎍/mL that does not effect the viability of the B16F10 cell line. The result of collagen production test using ELISA kit, liposomes containing acerola extract mixture showed collagen synthesis ability by 152.1% at 1,000 ㎍/mL that does not affect the viability of the HS68 cell line. But it did not showed any inhibition of collagenase (MMP-1) activity at all concentrations in the MMP-1 activity inhibition test in the HS68 cell line. We performed clinical studies for the whitening and skin-wrinkle activity of cream containing acerola extract mixes liposome, was showed that the melanin contents and wrinkle was statistically significant reduction. These results suggest that liposomes containing acerola extract mixture have safe natural material, and skin wrinkle, whitening effects allowing their application in cosmetics as a natural product.