• Food Science and Preservation
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• v.24 no.8
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• pp.1129-1137
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• 2017

The fringe tree, Chionanthus retusus (Oleaceae) has been used as a natural remedy that helps a paralytic stroke, dementia, phlegm and malaria. This study was conducted to investigate the antioxidant and anti-aging activities of water extracts obtained from the flesh of C. retusus by reflux extraction at room temperature and $80^{\circ}C$, and pressure heating extraction at $110^{\circ}C$, for an increment of their practical use. The highest extraction yield from the flesh of C. retusus was 67.94% extract by pressure heating extraction at $110^{\circ}C$. The content of total polyphenol compounds was the highest by 72.71 mg/g in $80^{\circ}C$ extract by reflux extraction. The highest content of total flavonoid compounds was 7.60 mg/g at $110^{\circ}C$ extract. The results of soluble protein and reducing sugar contents showed the highest content of 4.93 mg/g and 46.77 mg/g in $110^{\circ}C$ extract, respectively. In the analysis of DPPH radical scavenging activity, all extracts showed an excellent effect of 92% in 1.0 mg/mL concentration. The highest effect of ABTS radical scavenging activity was 88.67% at $110^{\circ}C$ extraction in 1.0 mg/mL concentration. Nitrite scavenging ability was the highest as 66.16% at $110^{\circ}C$ extract at pH 1.2 and 1.0 mg/mL concentration. The results of SOD-like activity and xanthine oxidase inhibition activities showed the highest effect of 14.95% and 59.45% at $110^{\circ}C$ extract in 1.0 mg/mL, respectively. Tyrosinase inhibition activity for whitening effect was the highest of 35.31% at $85^{\circ}C$ in 1.0 mg/mL. In the analysis of anti-aging effect, collagenase and elastase inhibition activity showed the highest effects of 37.78% at $110^{\circ}C$ and 20.39% at $80^{\circ}C$, respectively. All results of antioxidant activities and anti-aging effects increased along with the concentration increases. These results indicated that the extracts extracted from the flesh of C. retusus at $80^{\circ}C$ and $110^{\circ}C$ have a large amount of useful ingredients, an excellent antioxidant activity, like as DPPH and ABTS radical scavenging activity, and anti-aging effects to develop functional products than those of $25^{\circ}C$.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.41 no.4
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• pp.391-400
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• 2015

In the present study, 50% ethanol extract, the ethyl acetate and aglycone fraction were prepared from mate (Ilex paraguariensis) and their antioxidative ability was evaluated. The yields of extract and fractions were 32.0, 4.48 and 0.82% per dried powder, respectively. Free radical scavenging activities were performed by 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay and total antioxidant capacity was estimated using luminol-dependent chemiluminescence assay. Free radical scavenging activities ($FSC_{50}$) of 50 % ethanol extract, ethyl acetate fraction and aglycone fraction were 8.83, 5.84 and $6.05{\mu}g/mL$, respectively. Their total antioxidant capacities ($OSC_{50}$) were similar to that of L-ascorbic acid ($1.72{\mu}g/mL$), known as a prominent water soluble antioxidant, in all extracts and 50% ethanol extract ($1.03{\mu}g/mL$) was the most effective. The cellular protective effects on the $^1O_2$-induced cellular damage of erythrocytes were evaluated and the results showed that all extracts were significantly higher than (+)-${\alpha}$-tocopherol at $10{\mu}g/mL$. Especially, the ${\tau}_{50}$ value of aglycone fraction was 5 times higher than (+)-${\alpha}$-tocopherol at $10{\mu}g/mL$ and $50{\mu}g/mL$. The inhibitory effects of the ethyl acetate and aglycone fractions on tyrosinase were similar to arbutin, known as the whitening agent in cosmetics. These results suggest that the extracts of mate have the applicability as antioxidant and anti-aging cosmeceutical ingredients.

• Applied Chemistry for Engineering
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• v.22 no.2
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• pp.178-184
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• 2011

In this study, the antibacterial, antioxidative and inhibitory effects of Allium cepa peel extracts on tyrosinase and elastase were investigated. MIC values of the ethyl acetate fraction of Allium cepa peel on especially, S. aureus among the skin resident flora (Staphylococcus aureus, S. aureus; Propionibacterium acnes, P. acnes; Pityrosporum ovale, P. ovale; Escherichia coli, E. coli) were 0.06%. The aglycone fraction showed more excellent free radical (1,1-diphenyl-2-picrylhydrazyl radical, DPPH) scavenging activity ($FSC_{50}=5.05{\mu}g/mL$). Reactive oxygen species (ROS) scavenging activities ($OSC_{50}$) of the ethyl acetate fraction and aglycone fraction in the luminol-dependent $Fe^{3+}-EDTA/H_2O_2$ system were 0.05 and $0.03{\mu}g/mL$, respectively. The cellular protective effect of the aglycone fraction on the rose-bengal sensitized photohemolysis of human erythrocytes exhibited more prominent (${\tau}_{50}$, 480 min at $25{\mu}g/mL$). The inhibitory effects ($IC_{50}$) of the ethyl acetate fraction and aglycone fraction on tyrosinase were 9.16 and $8.68{\mu}g/mL$, the inhibitory effect ($IC_{50}$) of the aglycone fraction on elastase was $14.12{\mu}g/mL$ The transepidermal water loss of the cream containing 0.1% ethyl acetate fraction was decreased from $8.3g/m^2h$ in control to $6.8g/m^2h$ in the subjects applied with cream containing the ethyl acetate fraction. These results indicate that extract/fractions of Allium cepa peel can function as antioxidant in biological systems, particularly skin exposed to UV radiation by scavenging $^1O_2$ and other ROS, and protect cellular membranes against ROS, and possibly as antiaging agents. Allium cepa peel extract could be used as a new cosmeceutical for whitening and anti-wrinkle products.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.34 no.3
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• pp.233-244
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• 2008

In this study, the antioxidative effects, inhibitory effects on elastase and tyrosinase, and component analysis of Psidium guajava leaf extracts were investigated. The free radical (1,1-diphenyl-2-picrylhydrazyl, DPPH) scavenging activities $(FSC_{50})$ of extract/fractions of Psidium guajava leaf were in the order: 50% ethanol extract $(7.05{\mu}g/mL)$ < ethyl acetate fraction $(3.36{\mu}g/mL)$ < deglycosylated flavonoid aglycone fraction $(3.24{\mu}g/mL)$. Reactive oxygen species (ROS) scavenging activities $(OSC_{50})$ of some Psidium guajava leaf extracts on ROS generated in $Fe^{3+}-EDTA/H_2O_2$ system were investigated using the luminol-dependent chemiluminescence assay. The order of ROS scavenging activities were 50% ethanol extract $(OSC_{50},\;2.17{\mu}g/mL)$ < ethyl acetate fraction $(0.64{\mu}g/mL)$ < deglycosylated flavonoid aglycone fraction $(3.39{\mu}g/mL)$. Aglycone fraction showed the most prominent ROS scavenging activity. The protective effects of extract/fractions of Psidium guajava leaf on the rose-bengal sensitized photohemolysis of human erythrocytes were investigated. The Psidium guajava leaf extracts suppressed photohemolysis in a concentration dependent manner $(1{\sim}10{\mu}g/mL)$, particularly deglycosylated flavonoid aglycone fraction exhibited the most prominent celluar protective effect ${\tau}_{50}\;107.5min\;at\;1{\mu}g/mL)$. Aglycone fraction obtained from the deglycosylation reaction of ethyl acetate fraction among the Psidium guajava leaf extracts, showed 1 band in TLC and 1 peak in HPLC experiments (360 nm). One component was identified as quercetin. TLC chromatogram of ethyl acetate fraction of Psidium guajava leaf extract revealed 5 bands and HPLC chromatogram showed 5 peaks, which were identified as quercetin 3-O-gentobioside (10.32%) , quercetin 3-O-${\beta}$-D-glucoside (isoquercitin, 13.30%), quercetin 3-O-${\beta}$-D-galactoside (hyperin, 11.34%), quercetin 3-O-${\alpha}$-L-arabinoside (guajavarin, 19.70%), quercetin 3-O-${\beta}$-L-rhamnoside (quercitrin, 45.33%) in the order of elution time. The inhibitory effect of Psidium guajava leaf extracts on tyrosinase were investigated to assess their whitening efficacy. Finally, their anti-elastase activities were measured to predict the anti-wrinkle efficacy in the human skin. Inhibitory effects $(IC_{50})$ on tyrosinase of some Psidium guajava leaf extracts was 50% ethanol extract $(149.67{\mu}g/mL)$ < ethylacetate fraction $(30.67{\mu}g/mL)$ < deglycosylated aglycone fraction $(17.10{\mu}g/mL)$. Inhibitory effects $(IC_{50})$ on elastase of some Psidium guajava leaf extracts was 50% ethanol extract $(6.60{\mu}g/mL)$ < deglycosylated aglycone fraction $(5.66{\mu}g/mL)$ < ethylacetate fraction $(3.44{\mu}g/mL)$. These results indicate that extract/fractions of Psidium guajava leaf can function as antioxidants in bioloigcal systems, particularly skin exposed to UV radiation by scavenging $^1O_2$ and other ROS, and protect cellular membranes against ROS. And component analysis of Psidium guajava leaf extract and inhibitory activity on elastase of the aglycone fraction could be applicable to new functional cosmetics for smoothing wrinkles.

• 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.44 no.3
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• pp.249-258
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• 2018

Airborne pollution causes oxidative damage, inflammation, and premature aging of skin. Resveratrol is a polyphenol compound that has various biological activities such as antioxidant, anti-inflammation, and anti-melanogenic activities but it is unstable to heat and light. Resveratryl triacetate (RTA) is a new cosmetic ingredient that is more stable than resveratrol and its skin safety and whitening efficacy have been reported previously. The purpose of this study was to examine the effects of resveratrol and resveratryl triacetate (RTA) on the inflammatory responses of human epidermal keratinocytes (HEKs) exposed to airborne particulate matters with a diameter of < $10{\mu}m$ (PM10). Cultured HEKs were exposed to PM10 in the absence or presence of resveratrol and RTA. Assays were undertaken to determine cell viability, the production of reactive oxygen species (ROS), and the expression of inflammatory cytokines. PM10 treatment decreased cell viability, and increased the expression of pro-inflammatory cytokines such as tumor necrosis $factor-{\alpha}$ ($TNF-{\alpha}$), $interleukin-1{\beta}$ ($IL-1{\beta}$), interleukin-6 (IL-6), and interleukin-8 (IL-8). Resveratrol and RTA reduced cell death and ROS production induced by PM10. PM10-induced mRNA expression of the inflammatory cytokines was either attenuated (IL-6), or enhanced ($IL-1{\beta}$), or unaffected ($TNF-{\alpha}$ and IL-8) by resveratrol and RTA. PM10-induced IL-6 protein expression was attenuated by resveratrol and RTA. This study suggests that resveratrol and RTA have activities regulating cell damage and inflammatory responses of the skin exposed to airborne particulate matters.

• Journal of Life Science
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• v.27 no.2
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• pp.139-148
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• 2017

The inhibition of tyrosinase, a key enzyme in mammalian melanin synthesis, plays an important role in preventing skin pigmentation and melanoma. Therefore, tyrosinase inhibitors are very important in the fields of medicine and cosmetics. However, only a few tyrosinase inhibitors are currently available because of their toxic effects on skin or lack of selectivity and stability. Therefore, we synthesized a novel series of (E)-2-(substituted benzylidene)-2,3-dihydro-1H-cyclopenta[a]naphthalen-1-one derivatives and evaluated their inhibitory effects on mushroom tyrosinase, with the aim of discovering a novel tyrosinase inhibitor. Among 19 derivatives, MHY3655 ($IC_{50}=0.1456{\mu}M$) showed the strongest inhibitory effect on tyrosinase activity compared to kojic acid ($IC_{50}=17.2{\mu}M$), a well-known tyrosinase inhibitor. In addition, MHY3655 showed competitive inhibition on Lineweaver-Burk plots. We confirmed that MHY3655 strongly interacts with mushroom tyrosinase residues through the docking simulation. Substitutions with a hydroxy group at both R2 and R4 in the phenyl ring indicated that these groups play a major role in the high binding affinity to tyrosinase. Further, MHY3655 did not show cytotoxicity at the concentrations tested in B16F10 melanoma cells. In conclusion, the novel compound MHY3655 potentially shows tyrosinase inhibitory activity, and it could be used as an ingredient in whitening cosmetics.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.43 no.2
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• pp.157-164
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• 2017

Stevia (Stevia rebaudiana) is a perennial plant of the genus Stevia, originated in South America. It stores many forms of glycosides, mainly stevioside and rebaudioside A, in which steviol is the basic structure. Steviol glycosides, widely used as sweeteners, are superior to sugar in sweetness. Recently, it has been reported that steviol glycosides are involved not only in the skin whitening and anti-inflammatory effect but also in enhancing skin barrier function through tight junction regulation. Thus, we examined anti-inflammatory effect of rebaudioside A and tried to identify its potential for improving atopic dermatitis as cosmetic ingredients. To investigate the anti-inflammatory effect, cell viability and mRNA expression level of inflammation-related cytokines were measured using mouse macrophage RAW264.7 cells. Cell counting kit 8 (CCK-8) assay was carried out to measure cell viability and the maximum concentration without cytotoxicity was set to $250{\mu}M$. A quantitative real-time RT-PCR method was used for the study of the inflammatory suppression of rebaudioside A. Rebaudioside A inhibited expression of inducible nitric oxide synthase (iNOS) up to 47% and COX-2 up to 41% compared to LPS treated condition. NO synthesis was decreased by rebaudioside A. Also, mRNA expression of interleukin (IL)-$1{\alpha}$, IL-$1{\beta}$ and IL-6 in LPS-stimulated RAW264.7 cells was decreased to 40%, 45% and 59%, respectively, as a concentration-dependent manner. In conclusion, rebaudioside A inhibited the inflammatory response by regulation of cytokine gene expression. From these results, we expect that steviol glycoside, such as rebaudioside A, can be used as a material for improving atopic dermatitis in the future.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.39 no.4
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• pp.295-302
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• 2013

In this study, the antioxidative effects and inhibitory activities of unripened fruit extract of Rubus coreanus Miquel (R. coreanus Miquel) on tyrosinase were investigated and the potential applicability as a cosmeceutical ingredients was evaluated. All experiments were performed with 50% ethanol extract, ethyl acetate fraction and aglycone fraction of unripened fruit extract of R. coreanus Miquel. The DPPH (1,1-diphenyl-2-picrylhydrazyl) scavenging activites ($FSC_{50}$) of 50% ethanol extract (6.56 ${\mu}g/mL$) and ethyl acetate fraction (6.14 ${\mu}g/mL$) of unripened fruit extract of R. coreanus Miquel were higher than (+)-${\alpha}$-tocopherol (8.98 ${\mu}g/mL$), which is known as a typical hydrophobic antioxidant. Reactive oxygen species (ROS) scavenging activities ($OSC_{50}$) of 50% ethanol extract (0.83 ${\mu}g/mL$), ethyl acetate fraction (0.84 ${\mu}g/mL$) and aglycone fraction (1.13 ${\mu}g/mL$) of R. coreanus Miquel on ROS generated in $Fe^{3+}-EDTA/H_2O_2$ system were higher than L-ascorbic acid (1.5 ${\mu}g/mL$), which is known as s typical hydrophilic antioxidant. The cellular protective effect of extract and fraction of unripened fruit extract of R. coreanus Miquel on the rose bengal sensitized photohemolysis of human erythrocytes was increased in a concentration dependent manner (1 ~ 50 ${\mu}g/mL$). And 50% ethanol extract in 50 ${\mu}g/mL$ showed the most protective effect among extracts (${\tau}_{50}$ = 296.3 min). The inhibitory effects on tyrosinase of ethyl acetate and agylcone fractions were higher than arbutin. These results indicate that unripened fruit extracts of R. coreanus Miquel can be applied to antioxidant scavenging ROS including radical as an alternative whitening agent to replace arbutin.

• Proceedings of the Korean Society of Applied Pharmacology
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• 2007.11a
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• pp.79-92
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• 2007

Oxidative stress have known to be a risk factor for the degenerative processes and closely related to a lot of diseases. It is well established that antioxidants are good in protection and therapeutic means against oxidative damage. There is increasing interest in natural antioxidants and many natural antioxidants have been found and utilized as the possible protection for various diseases and skin aging. We have screened natural antioxidant agents for cosmeceuticals, nutraceuticals, and drugs as therapeutic and preventive means against oxidative stress, and have developed a number of novel antioxidants from various natural sources. A novel melanin synthesis inhibitor, Melanocin A, isolated from the metabolite of a fungal strain Eupenicillium shearii F80695 inhibited mushroom tyrosinase and melanin biosynthesis of B16 melanoma cells with $IC_{50}$ value of 9.0 nM and MIC value of $0.9\;{\mu}M$, respectively. Melanocin A also exhibited potent antioxidant activity by scavenging of DPPH and superoxide anion radicals. UV was found to increase the level of hydrogen peroxides and other reactive oxygen species (ROS) in skin tissues. This increase in ROS may not only alter the structure and function of many genes and proteins directly but may also modulate their expressions through signal transduction pathways and, ultimately, lead to skin damage. We investigated the effect of Melanocin A on UV-induced premature skin aging. Firstly, the effect of Melanocin A on UV-induced matrix metalloproteinase (MMP)-9 expression in an immortalized human keratinocyte cell line, HaCaT in vitro was investigated. Acute UV irradiation induced MMP-9 expression at both the mRNA and protein levels and Melanocin A suppressed this expression in a dose-dependent manner. We then investigated UV-induced skin changes in hairless mice in vivo by Melanocin A. Chronic exposure of hairless mouse dorsal skin to UV increased skin thickness and induced wrinkle formation and the gelatinase activities of MMP-2 and MMP-9. Moreover, Melanocin A significantly suppressed UV-induced morphologic skin changes and MMP-2 and MMP-9 expression. These results show that Melanocin A can prevent the harmful effects of UV that lead to skin aging. Therefore, we suggest that Melanocin A should be viewed as a potential therapeutic agent for preventing and/or treating premature skin aging. Terrein is a bioactive fungal metabolite isolated from Penicillium species. Terrein has a relatively simple structure and can be easily synthesized. However, the biologic effects of terrein are comparatively unknown. We found for the first time that terrein potently inhibit melanin production in melanocytes and has a strong hypopigmentary effect in a spontaneously immortalized mouse melanocyte cell line, Mel-Ab. Treatment of Mel-Ab cells with terrein (10-100 mM) for 4 days significantly reduced melanin levels in a dose-dependent manner. In addition, terrein at the same concentration also reduced tyrosinase activity. We then investigated whether terrein influences the extracellular signal-regulated protein kinase (ERK) pathway and the expression of microphthalmia-associated transcription factor (MITF), which is required for tyrosinase expression. Terrein was found to induce sustained ERK activation and MITF down-regulation, and luciferase assays showed that terrein inhibits MITF promoter activity in a dose-dependent manner. To elucidate the correlation between ERK pathway activation and a decreased MITF transcriptional level, PD98059, a specific inhibitor of the ERK pathway, was applied before terrain treatment and found to abrogate the terrein-induced MITF attenuation. Terrein also reduced the tyrosinase protein level for at least 72 h. These results suggest that terrain reduces melanin synthesis by reducing tyrosinase production via ERK activation, and that this is followed by MITF down-regulation.