• Journal of Life Science
• /
• v.27 no.2
• /
• pp.139-148
• /
• 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
• /
• v.43 no.2
• /
• pp.157-164
• /
• 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.

• Food Science and Preservation
• /
• v.24 no.7
• /
• pp.1025-1033
• /
• 2017

In this study, Ledum palustre L. was extracted by 4 different methods (LPW, hot water extraction; LPA, autoclave extraction; LPU, ultrasonification extraction; LPE, 70% ethanol extraction) and LPE was fractionated by using polarity difference of each solvent and used as 4 samples (LPE/H, the n-hexane layer; LPE/E, the EtOAc layer; LPE/B, the n-BuOH layer; LPE/W, the $H_2O$ layer). Antioxidant activities of Ledum palustre L. extracts were measured by DPPH and ABTS. As a result, the DPPH and ABTS radical scavenging showed high activities with LPE (82.3%, 99.8%) and LPE/E (91.8%, 99.6%) at the concentration of $1,000{\mu}g/mL$. The anti-inflammatory activities of LPE and LPE/E were measured by the inhibitory activity against NO, $PGE_2$, TNF-${\alpha}$, IL-$1{\beta}$ and IL-6 production on LPS-stimulated Raw 264.7 macrophages. As a result of MTT assay, cell viabilities of LPE and LPE/E were more than 90% at $25{\mu}g/mL$. NO and $PGE_2$ productions were inhibited by LPE (NO: 50%, $PGE_2$: 70%) and LPE/E (NO: 57%, $PGE_2$: 73%) at the concentration of $25{\mu}g/mL$. The inhibition activities against TNF-${\alpha}$, IL-$1{\beta}$, IL-6 production were 24%, 47% and 40% at the concentration of $25{\mu}g/mL$ of LPE. In particular, LPE/E showed 51%, 57% and 62% inhibition activities at the same concentration, respectively. From the above results, it can be concluded that $1,000{\mu}g/mL$ of LPE and LPE/E have the high antioxidant activities similar with Vitamin C, and $25{\mu}g/mL$, the low concetration of LPE and LPE/E have excellent anti-inflammatory activities. Therefore, if more research about anti-aging, whitening and antimicrobial activity of Ledum palustre L. extracts is carried out in the future, it will be possible to use them as effective materials for the prevention and treatment of inflammatory diseases and in the areas of functional foods and cosmetics.

• Journal of the Society of Cosmetic Scientists of Korea
• /
• v.35 no.1
• /
• pp.47-55
• /
• 2009

In this study, the antioxidative effects, inhibitory effects on tyrosinase, and component analysis of fermented Melissa officinalis extracts were investigated. The ethyl acetate fraction of fermented extract ($8.38{\mu}g/mL$) showed the most prominent the free radical (1,1-diphenyl-2-picrylhydrazyl, DPPH) scavenging activities ($FSC_{50}$) of extract/fractions of M. officinalis. Reactive oxygen species (ROS) scavenging activities ($OSC_{50}$) of some M. officinalis extracts on ROS generated in $Fe^{3+}$-EDTA/$H_{2}O_{2}$ system were investigated using the luminol-dependent chemiluminescence assay. The ethyl acetate fraction of fermented extract ($0.63{\mu}g/mL$) showed the most prominent ROS scavenging activity. The protective effects of extract/fractions of M. officinalis on the rose-bengal sensitized photohemolysis of human erythrocytes were investigated. The M. officinalis extracts suppressed photohemolysis in a concentration dependent manner ($5\;{\sim}\;75{\mu}g/mL$). The inhibitory effect of M. officinalis extracts on tyrosinase was investigated to assess their whitening efficacy. Inhibitory effects ($IC_{50}$) on tyrosinase of some M. officinalis extracts was 50 % ethanol extract ($365{\mu}g/mL$) < ethyl acetate fraction of fermented extract ($122.43{\mu}g/mL$) < ethylacetate fraction ($94.8{\mu}g/mL$). Fractions of ethyl acetate both from ordinary and fermented M. officinalis extracts showed 2 band in TLC and 2 peak in HPLC (330 nm). In HPLC chromatogram of ethyl acetate fraction, peak 1 (51.64 %) and peak 2 (48.36 %) were identified as caffeic acid and rosmarinic acid in the order of elution time. Also, in HPLC chromatogram of ethyl acetate fraction of fermented extract, peak 1 (4.13 %) and peak 2 (95.87 %) were identified as caffeic acid and rosmarinic acid in the order of elution time. These results indicate that the component and content of ordinary and fermented extracts of M. officinalis are different. And the extract of M. officinalis can be used as an antioxidant.

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

• Journal of the Korean Society of Food Science and Nutrition
• /
• v.46 no.5
• /
• pp.572-580
• /
• 2017

The contents of phenolic compounds in water and 40% ethanol extracts from Okkwang (Castanea crenata) chestnut bur solid (OCS) were $11.24{\mu}g/50{\mu}g$ solid and $10.28{\mu}g/50{\mu}g$ solid, respectively. The 1,1-diphenyl-2-picrylhydrazyl free radical scavenging and 2,2'-azino-bis(3-ethylbenzothiazoline- 6-sulfonic acid) radical decolorization activities of water and ethanol extracts were 85% and 100% as well as 87% and 86% at a solid content of $50{\mu}g/mL$, respectively. The anti-oxidant protection factors (PFs) of water and ethanol extracts at a solid content of $200{\mu}g/mL$ were 1.22 PF and 1.45 PF, respectively. Thiobarbituric acid reactive substance were 83% in water extract and 73% in ethanol extract at a solid content of $200{\mu}g/mL$. The inhibitory activities against xanthine oxidase in water and ethanol extracts were 54% and 43% at a solid content of $200{\mu}g/mL$, respectively. The inhibitory activities against ${\alpha}$-glucosidase were 95% in water extract and 96% in ethanol extract at a solid content of $50{\mu}g/mL$. Tyrosinase inhibitory activity was 27% in ethanol extract at a solid content of $200{\mu}g/mL$. The collagenase and elastase inhibitory activities as anti-wrinkle effect were 93% and 11% in water extract as well as 94% and 56% in ethanol extract at a solid content of $200{\mu}g/mL$. Hyaluronidase inhibitory activity as anti-inflammatory effect of water and ethanol extracts were 96% and 52% at a solid content of $200{\mu}g/mL$, respectively. The results show that extracts from OCS can be used as a functional resource with antioxidant, anti-gout, carbohydrate degradation inhibitory, whitening, anti-wrinkle, and anti-inflammatory activities.

• Journal of the Society of Cosmetic Scientists of Korea
• /
• v.35 no.2
• /
• pp.125-134
• /
• 2009

In this study, the antioxidative effects, inhibitory effects on tyrosinase, and component of non-fermented and fermented Lavandula angustifolia extracts were investigated. The ethyl acetate fraction of fermented extract (5.95 ${\mu}g/mL$) showed the most prominent the free radical (1,1-diphenyl-2-picrylhydrazyl, DPPH) scavenging activity ($FSC_{50}$). Reactive oxygen species (ROS) scavenging activities ($OSC_{50}$) of L. angustifolia extracts on ROS generated in $Fe^{3+}-EDTA/H_2O_2$ system were investigated using the luminol-dependent chemiluminescence assay. The ethyl acetate fraction of fermented extract (1.45 ${\mu}g/mL$) showed the most prominent ROS scavenging activity. The protective effects of extract/fractions of L. angustifolia on the rose-bengal sensitized photohemolysis of human erythrocytes were investigated. The L. angustifolia extracts suppressed photohemolysis in a concentration dependent manner (1 ${\sim}$ 50 ${\mu}g/mL$). The inhibitory effect of L. angustifolia extracts on tyrosinase was investigated to assess their whitening efficacy. Inhibitory effects ($IC_{50}$) on tyrosinase were determined with ethyl acetate fraction of L. angustifolia extract (144.80 ${\mu}g/mL$) and ethyl acetate fraction of fermented extract (122.40 ${\mu}g/mL$). Fractions of ethyl acetate and fermented extracts showed both 3 band in TLC and 3 peaks, 2 peaks in HPLC (340 nm), respectively. In each chromatography, fractions of ethyl acetate both from non-fermented and fermented L. angusfifolia have rosmarinic acid in common. These results indicate that the component and content of non-fermented and fermented extracts of L. angustifolia are different. Both of the extract of L. angustifolia can be used as an antioxidant.

• Journal of the Society of Cosmetic Scientists of Korea
• /
• v.34 no.2
• /
• pp.83-92
• /
• 2008

In this study, the antioxidative effects, inhibitory effects on tyrosinase and elastase and components of Fagopyrum esculetum extracts were investigated. Fagopyrum esculetum used for this study is hulls and dehulled seeds. The free radical(1,1-diphenyl-2-picrylhydrazyl radical, DPPH) scavenging activities($FSC_{50}$) and reactive oxygen species(ROS) scavenging activities($OSC_{50}$) of extract/fractions from Fagopyrum esculetum were measured. The aglycone($3.5{\pm}0.0{\mu}g/mL$) and ethyl acetate fractions($0.2{\pm}0.1{\mu}g/mL$) of hulls showed the most effective scavenging activities. The protective effects on the rose-bengal sensitized photohemolysis of human erythrocytes were investigated. The ethyl acetate fraction exhibited the most prominent cellular protective effect(${\tau}_{50},\;771.7{\pm}9.9 min$ at 10 ${\mu}g/mL$). The inhibitory effect of aglycone fraction of hull and dehulled seeds on tyrosinase were examined ($53.6{\pm}0.5{\mu}g/mL,\;35.6{\pm}0.4{\mu}g/mL$, respectively). And The inhibitory effect of aglycone fraction of hull and dehulled seeds on elastase were investigated($3.7{\pm}0.4{\mu}g/mL\;and\;6.0{\pm}0.7{\mu}g/mL$ respectively). But 50% ethanol extract rarely exhibited the inhibitory activity on tyrosinase and elastase. (+)-Catechin and (-)-epicatechin were contained in ethyl acetate fraction of dehulled seeds. And ethyl acetate fraction of hull contains flavonoids of hyperin, quercetin, rutin and so on. These results indicate that extract/fractions of Fagopyrum esculentum can function as antioxidants in biological systems, particularly skin exposed to UV radiation by scavenging $^1O_2$ and other ROS, and protect cellular membranes against ROS. Fagopyrum esculentum extract could be used as a new cosmeceutical for whitening and anti-wrinkle products.

• Food Science and Preservation
• /
• v.24 no.8
• /
• pp.1129-1137
• /
• 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
• /
• v.37 no.2
• /
• pp.191-198
• /
• 2011

In this study, antioxidative effects and inhibitory effects of Geum aleppicum Jacq. extracts on tyrosinase and elastase were investigated. The ethyl acetate fraction of G. aleppicum Jacq. extract ($4.70\;{\mu}g$/mL) showed the most prominent free radical (1,1-diphenyl-2-picrylhydrazyl, DPPH) scavenging activity (FSC50). Reactive oxygen species (ROS) scavenging activities ($OSC_{50}$) of some G. aleppicum Jacq. extracts on ROS generated in $Fe^{3+}-EDTA/H_2O_2$ system were investigated using the luminol-dependent chemiluminescence assay. The ethyl acetate fraction showed the most prominent ROS scavenging activity ($0.22 \;{\mu}g$/mL). The protective effects of extract/fraction of G. aleppicum Jacq. against the rose-bengal sensitized photohemolysis of human erythrocytes were investigated. The G. aleppicum Jacq. extracts suppressed photohemolysis in a concentration dependent manner ($1{\sim}25{\mu}g$/mL), particularly the ethyl acetate fraction exhibited the most prominent celluar protective effect (${\tau}_{50}$, 416.20 min at $10 \;{\mu}g$/mL). The inhibitory effect of G. aleppicum Jacq. extracts on tyrosinase and elastase were investigated to assess their whitening and anti-winkle efficacy. The half maximal inhibitory concentration ($IC_{50}$) of the ethyl acetate fraction on tyrosinase was $95.23\;{\mu}g$/mL. The $IC_{50}$ of 50 % ethanol extract and the ethyl acetate fraction on elastase were $6.27 \;{\mu}g$/mL and $4.31 \;{\mu}g$/mL, respectively. These results indicate that extract/fraction of G. aleppicum Jacq. can function as antioxidants in biological systems, particularly skin exposed to UV radiation by scavenging $^1O_2$ and other ROS, and protect cellular membranes against ROS. Especially the ethyl acetate fraction of G. aleppicum Jacq. extracts could be applicable to new functional cosmetics for antioxidant, antiaging.