• 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.

• Korean Journal of Food Science and Technology
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• v.48 no.5
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• pp.508-514
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• 2016

Effects of the ethyl acetate fraction from gomchwi (Ligularia fischeri) extract against high $glucose/H_2O_2-induced$ oxidative stress and in vitro neurodegeneration were investigated to confirm the physiological property of the extract. The ethyl acetate fraction of gomchwi extract showed the highest total phenolic contents than the other solvent fractions. An anti-hyperglycemic activity of the ethyl acetate fraction was evaluated using the ${\alpha}-glucosidase$ inhibitory assay, and the half maximal inhibitory concentration ($IC_{50}$) value for ${\alpha}-glucosidase$ was found to be $727.64{\mu}g/mL$. In addition, the ethyl acetate fraction showed excellent 2,2'-azino-bis (3-ethylbenzthiazoline-6-sulfonic acid) diammonium salt radical scavenging activity, and inhibition of malondialdehyde production. The ethyl acetate fraction also decreased intracellular reactive oxygen species, whereas neuronal cell viability against high glucose/$H_2O_2$-induced cytotoxicity was found to be increased. Finally, 3,5-dicaffeoylquinic acid as a main phenolic compound in the ethyl acetate fraction was analyzed by high-performance liquid chromatography. These results suggest that gomchwi might be a good natural source of functional materials to prevent diabetic neurodegeneration.

• Food Science and Preservation
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• v.19 no.6
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• pp.825-832
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• 2012

In this study, the quality characteristics and antioxidant activity of mulberry salad dressing prepared with yam juice during storage at $5^{\circ}C$ for four weeks were evaluated. The salad dressing was prepared with a salad base, mulberry, omija, and yam (4:4:6:1 or 4:4:6:3). Fresh yam juice was added to the salad dressing at 0, 7, and 18% levels. After four weeks storage, the pH increased whereas the acidity decreased. As the yam concentration increased, the pH increased to 3.84 and the acidity decreased to 0.14%. The Hunter color L (lightness), b (yellowness), and a (redness) values decreased over the storage period. After four weeks storage, the viscosity increased from 83.2 to 158.5 cp according to the amount of yam juice that was added. The antioxidant activity, such as the DPPH radical scavenging activity, and the total polyphenol content of the salad dressing improved as the yam concentration increased. Moreover, according to the storage time, the peroxide value did not increase. These results show that the mulberry salad dressing to which omija and fresh yam juice were added maintained its freshness with high antioxidative activity during storage.

• Korean Journal of Food Science and Technology
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• v.53 no.4
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• pp.423-433
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• 2021

This study was performed to examine the neuroprotective effect of the ethyl acetate fraction from Eucommia ulmoides oliver leaf (EFEL) on PM_2.5-induced cytotoxicity. EFEL had higher total phenolic and flavonoid contents than the other fractions. In ABTS and DPPH radical scavenging activities, the IC₅₀ of EFEL was measured as 212.80 and 359.13 ㎍/mL, respectively. To investigate the neuroprotective effect of EFEL, MTT and DCF-DA assays were performed on HT22, MC-IXC, and BV-2 cells. EFEL effectively decreased PM_2.5-induced intercellular reactive oxygen species (ROS) content and inhibited PM_2.5-induced cell death. In the results of protein expression related to cellular cytotoxicity on microglial cells (BV-2), EFEL had an improvement effect on cell apoptosis and inflammatory pathways. Rutin and chlorogenic acid were identified as the main physiological compounds. Moreover, it was expected that EFEL, including rutin and chlorogenic acid, could be functional food substances with neuroprotective effects against PM_2.5-induced oxidative stress.

• Journal of the Korean Applied Science and Technology
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• v.36 no.2
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• pp.394-406
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• 2019

The cellular senescence may be due to damage by the reactive oxygen species (ROS). This study has compared the antioxidant activity in the human cell lines of various origins, including 10S and 50S-derived normal skin fibroblasts, and 10S bone marrow, dental tissue and adipose-derived adult stem cells. After being exposed to $H_2O_2$, half inhibitory concentration ($IC_{50}$) values by cytotoxicity assay was significantly (P<0.05) lower in 50S-derived skin fibroblasts, than in 10S-derived skin fibroblasts and various adult stem cell lines. The cell population doubling time (PDT) and the cell frequency with high senescence associated-${\beta}$-galactose activity were remarkably increased in 50S-derived fibroblasts exposed to 50 ppm $H_2O_2$ for 7 days, than those of 10S-derived fibroblasts and various adult stem cell lines. Further, the expression level of antioxidant-related genes, glutathione peroxidase (GPX) and catalase (CAT), was investigated in 10S and 50S-derived skin fibroblasts, and 10S-derived various adult stem cells by reverse transcription polymerase chain reaction (RT-PCR). The expression level of GPX was higher in most of cell lines, compared to CAT, and a significantly (P<0.05) higher expression level of GPX was observed in 10S-derived skin fibroblasts and adult stem cell lines, compared to 50S-derived skin fibroblasts. We concluded that old-aged skin fibroblasts seemed to be less resistant against ROS than young-aged skin fibroblasts and adult stem cells.

• Journal of Life Science
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• v.29 no.6
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• pp.679-687
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• 2019

Litsea populifolia, a plant species of the Lauraceae family, is widely distributed in the tropical and subtropical areas of Asia. The phylogenetic relationships and botanical characteristics of L. populifolia have been reported; however, its anti-oxidative and anti-cancer activities remain unclear. In this study, we evaluated the anti-oxidative and anti-cancer effects of ethanol extracts of L. populifolia (EELP) together with the molecular mechanism of its anti-cancer activity in human lung adenocarcinoma A549 cells. EELP showed significant anti-oxidative effects with a 50% inhibitory concentration at $11.71{\mu}g/ml$, which was measured by the 2,2-diphenyl-1-picrylhydrazyl radical scavenging assay. EELP exhibited cytotoxic activity and induced cell cycle arrest at the G1 phase in A549 cells in a dose-dependent manner, whereas EELP did not have the cytotoxic effect on the normal human lung cell line IMR90. Treatment with EELP also resulted in a decreased expression of G1/S transition-related molecules-including cyclin-dependent kinase (CDK) 2, CDK6, cyclin D1, and cyclin E-both for the transcription and translation levels. EELP-induced G1 arrest was associated with the phosphorylation of checkpoint kinase 2 (CHK2), p53, cell division cycle 25 homolog A (CDC25A), and the reduction of CDC25A expression in A549 cells. Collectively, these results suggest that EELP may exert an anti-cancer effect by cell cycle arrest at the G1 phase through both p53-dependent and p53-independent (ATM/CHK2/CDC25A/CDK2) pathways in A549 cells.

• Journal of the Korean Applied Science and Technology
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• v.36 no.3
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• pp.766-778
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• 2019

In this study, Poria cocos bark were extracted by supercritical process, and anti-inflammatory, whitening, and antioxidant effects were measured in comparison with ethanol extract. Also, An effective percutaneous permeation method using a selected formulation of the extract and a drug delivery peptide was proposed. Pachymic acid, known as the anti-cancer and anti-inflammatory compound of the ventricle, is an indicator component and the HPLC analysis shows that the supercritical extract of the pericardium is more than twice that of the Poria cocos bark extract. In order to confirm antioxidative effect of Bombyx mori, DPPH scavenging ability and ABTS scavenging ability test showed that the ethanol extract of Poria cocos Back had lower concentration than the supercritical extract of Poria cocos back. However, RAW 264.7 Measurements of Nitric oxide (NO) production in cells showed lower NO production at the same concentration than the Poria cocos back ethanol extract. In addition, after 72 hours of processing of $20{\mu}g/mL$ of the Poria cocos back extract in B16 melanoma cells, both the intracellular and extracellular melanin extract were effective and the supercritical extract was lower melanin content. No toxicity was observed at the concentration of $800{\mu}g/mL$ in RAW 264.7 cells used in NO production experiments. However, in B16 melanoma cells, even at $50{\mu}g/mL$, both Poria cocos back ethanol extract and supercritical extract showed a survival rate of less than 60%. The liposome formulation and drug delivery peptides were shown to be useful for percutaneous permeation of Supercritical Extract of Poria cocos back using a liposome formulation and a drug delivery peptide. it is expected that there will be great potential for development as a variety of cosmetic materials for Poria cocos back.

• Journal of Nutrition and Health
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• v.52 no.5
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• pp.413-421
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• 2019

Purpose: Astragalus membranaceus (AM) is an important traditional medicinal herb. Pharmacological research has indicated that AM has various physiological activities such as antioxidant, anti-inflammatory, immunoregulatory, anticancer, hypolipidemic, antihyperglycemic, and hepatoprotective activities. The bioactive substances responsible for the physiological activities in AM, including many antioxidant substances, change during the roasting process. This study investigated and compared the changes in the antioxidant constituents of AM caused by roasting. Methods: DPPH (1,1-diphenyl-2-picryl hydrazyl) and $ABTS^+$ (2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt) radical scavenging activities and their total phenolic content (TPC) were measured. High-performance liquid chromatography (HPLC) analysis was performed to confirm any changes in the isoflavonoids of roasted AM (R-AM),. The cell viability of UVB-induced HDF (Human dermal fibroblast) cells treated with AM and R-AM extracts was investigated. The comet assay was used to examine the inhibitory effects of R-AM extracts on DNA damage caused by oxidative stress. Results: The DPPH and $ABTS^+$ radical scavenging activities were $564.6{\pm}20.9$ and $108.2{\pm}3.1$ ($IC_{50}$ value) respectively, from the 2R-AM. The total phenol content was $47.80{\pm}1.40mg$ GAE/g from the 1R-AM. The values of calycosin and formononetin, which are the known isoflavonoid constituents of AM, were $778.58{\pm}2.72$ and $726.80{\pm}3.45{\mu}g/g$ respectively, from the 2R-AM. Treatment of the HDF cells with R-AM ($50{\sim}200{\mu}g/mL$) did not affect the cell viability. Furthermore, the R-AM extracts effectively protected against UVB-induced DNA damage. Conclusion: The findings of this study indicate that R-AM increases its isoflavonoid constituents and protects against UVB-induced DNA damage in HDF cells.

• Food Engineering Progress
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• v.21 no.3
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• pp.225-232
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• 2017

Most of the red ginseng (RG) products contain active substances derived from hot water or alcohol extraction. Since active substances of RG are divided into two types - water-soluble and liposoluble - water or alcohol is needed as an extraction solvent and this leads the different extraction yields and components of the active substances. To overcome the limit, whole red ginseng powder can be used and consumed by consumers. In this study, the physicochemical properties and extractable active substance contents of variable-sized RG powder ($158.00{\mu}m$, $8.45{\mu}m$, and $6.33{\mu}m$) were analyzed, and dispersion stability was measured to investigate the suitable size of RG powder for industrial processing. In the results, no significant difference was found from the changes in color intensity and thiobarbutric acid tests at $4^{\circ}C$, $25^{\circ}C$, and $40^{\circ}C$ for 4 weeks. There was no significant difference on the production of antioxidants and ginsenoside among the samples (p>0.05). In dispersion stability, $RG-158.00{\mu}m$ was precipitated immediately, and the dispersion stabilities between $RG-8.45{\mu}m$ and $RG-6.33{\mu}m$ showed no significant difference. It implies that fine RG is suitable for the production process. With further study, it seemed that the physicochemical effects of RG particle sizes can be clearly revealed.

• Korean Journal of Food Science and Technology
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• v.53 no.1
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• pp.46-54
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• 2021

The biological activities of non-edible extracts of asparagus stems and roots were investigated using hot water and ethanol. The highest contents of rutin and total polyphenol were 31.74 mg/g and 20.14 mg GAE/g, respectively, in the stem hot water extract. ABTS and DPPH radical scavenging activities were 541.1±21.0 and 649.5±6.6 ㎍/mL, respectively, in stem hot water extract. All extracts were non-cytotoxic in HepG2 cells, but 200 ㎍/mL stem extracts tended to decrease the viability of RAW 264.7 cells. The highest xanthine oxidase inhibitory activity was 43.68% in the root hot water extract at 200 ㎍/mL. The expression level of MMP-9 was significantly decreased in the asparagus extracts. The highest GGT, AST, and LDH activities showed a concentration-dependent decrease in the stem ethanol extract. In conclusion, the presence of bioactive substances in the non-edible extracts of asparagus was confirmed for the development of extracts with antioxidant, hepatoprotective and anti-gout activities.