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Tyrosinase Inhibitory Effect of (E)-2-(substituted benzylidene)-2,3-dihydro-1H-cyclopenta[a]naphthalen-1-one Derivatives ((E)-2-(substituted benzylidene)-2,3-dihydro-1H-cyclopenta[a]naphthalen-1-one 유도체들의 tyrosinase 활성억제 효과)

  • Lee, Eun Kyeong;Kim, Ju Hyun;Moon, Kyoung Mi;Ha, Sugyeong;Noh, Sang-Gyun;Kim, Dae Hyun;Lee, Bonggi;Kim, Do Hyun;Kim, Su Jeong;Ullah, Sultan;Moon, Hyung Ryong;Chung, Hae Young
    • 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.

Quality Characteristics and Biological Activities of Vinegars Added with Young Leaves of Akebia quinata (으름 어린잎 식초의 품질특성과 생리활성)

  • Kwon, Woo-Young;Lee, Eun-Kyoung;Yoon, Jin-A;Chung, Kang-Hyun;Lee, Kwon-Jai;Song, Byeong Chun;An, Jeung Hee
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.43 no.7
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    • pp.989-998
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    • 2014
  • We investigated the characteristics and biological activities of vinegars added with different levels (0%, 0.5%, 1%, 2%, and 3%) of young leaves of Akebia quinata. During alcohol fermentation, alcohol and total acidity contents of vinegars increased. During acid fermentation, total acidity and amino acid contents increased. Vinegar added with 3% A. quinata leaf showed the highest total sensory score. The contents of total polyphenols, flavonoids, and tannin significantly increased during fermentation according to the amount of A. quinata leaf. After 22 days of fermentation, total polyphenol, total flavonoid, and tannin contents of vinegar added with 3% A. quinata were 4,079.08 mg GAE/100 g, 2,927.08 mg CE/100 g, and 3,618.00 mg TAE/100 g, respectively. ABTS radical scavenging activity of vinegar added with 3% A. quinata was 79.63%. Anti-cancer activities of vinegar added with 3% A. quinata were 48.65% and 52.90% against MCF-7 and HepG2 cells, respectively. Vinegar added with 3% A. quinata showed anti-bacterial activities against Bacillus cereus, Shigella flexneri, Salmonella enterica, Bacillus subtilis, and Klebsiella pneumoniae. Our results demonstrate that the biological activities of vinegar added with 3% A. quinata leaf (22 days of fermentation) were excellent, and their enhanced total polyphenol, flavonoid, and tannin contents were associated with antioxidant, anti-cancer and anti-microbial activities. Thus, A. quinata can be used as a functional material in vinegar and other foods.

A MOLECULAR BIOLOGIC STUDY ON BIOCOMPATIBILITY OF METALLIC DENTAL MATERIALS USED FOR CHILDREN WITH CULTURED HUMAN GINGIVAL FIBROBLASTS (인체 섬유모세포(HGF-1) 배양에서 소아용 치과금속재의 세포친화성에 대한 분자생물학적 연구)

  • Kim, Ju-Mi;Jeong, Tae-Sung;Kim, Shin
    • Journal of the korean academy of Pediatric Dentistry
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    • v.29 no.2
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    • pp.243-254
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    • 2002
  • For the purpose of evaluating the biocompatability of 3 kinds of metallic materials frequently used in pediatric dentistry (stainless steel crown, orthodontic band, orthodontic wire), cellular and molecular studies, including cell growth and proliferation, screening of cell death with determination of types whether necrosis or apoptosis and changes in expressions of related signaling molecules were examined, using cultured human gingival fibroblasts (HGF-1), HGF-1 was cultured in Dulbecco's modified Eagle's medium. among which the 3rd to 6th generations of HGF-1 were used. The specimen were divided into stainless steel crown (R), band (B) and wire (W). The immunocytochemical study was done for the detection of anti-PCNA (proliferating cell nuclear antigen) labeling. With extracted protein, western blot was done for the detection of ERK1/2, JNK, and p38, using individual antibodies. Cultured cells proliferated, remarkably till 7 day and slightly at 11 day. There was no statistical significance in the counts of proliferating HGF-1 between control and experimental groups (p>0.05). Relative growth rates were no statistically significant difference between control and experimental groups (p>0.05). PCNA labeling indexes showing similar patterns in control and experimental groups. The expressions of ERK1 and ERK2, p38 were similar in control and experimental groups. The expression of JNK increased at 1st day, slightly decreased at 4th day and markedly increased at 7th and 11 day. Although the patterns of control and experimental groups were similar, the increased expressions of JNK at late period suggest a possible stress due to inhibited cell growth and proliferation, and worse culture condition. Conclusively, the 3 kinds of metal specimens used in this study did not induce cellular and molecular hazards during short term culture of HGF-1. But, for the better clinical stability, the establishment of long period culture and animal experiment was thought necessary.

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The Effects of Medicinal Herbs Extracts on Estrogen-like Activities and Osteoblast Proliferation and Differentiation (한약재 추출물의 에스트로겐 유사활성 및 조골세포 증식과 분화에 미치는 영향)

  • Kim, Mihyang;Kim, Bokyung;Kim, Jae-Deog;Kang, A-Ram;Lee, Chang-Eun;Seo, Jungmin;Lee, Dong-Geun;Jo, Jung-Kwon;Kim, Yuck Yong;Yu, Ki Hwan;Lee, Sang-Hyeon
    • Journal of Life Science
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    • v.27 no.4
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    • pp.456-463
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    • 2017
  • The purpose of this study was to investigate the effect of 3 types of medicinal herbs (Glycyrrhizae radix, Astragali radix and Dioscorea rhizoma) extracts on estrogen-like activities, proliferation and differentiation in osteoblast. Human breast cancer cell line MCF7 was transfected using an estrogen responsive luciferase reporter plasmid for measure the estrogen-like activity. Estrogen-like activities of extracts were in the range of 1.11~5.73 fold to that of negative control. The extract of G. radix showed the strongest estrogen-like activities. The estrogen-like activities of 50 and $500{\mu}g/ml$ extracts of G. radix were similar to that of $10^{-8}$ and $10^{-7}$ M standard solution ($17{\beta}-estradiol$), respectively. G. radix extract showed no cytotoxicity against osteoblast MC3T3-E1 cells at $1{\sim}1,000{\mu}g/ml$. The extract of A. radix showed no significant proliferation of osteoblast. However, the extract of G. radix and D. rhizome showed maximum 148% and 133% proliferation effects. The extract of G. radix also increased alkaline phosphatase activity and the maximum was 122% at $100{\mu}g/ml$ compared to that of control. The nodule formation by the method of the Alizarin red S staining increased compared to control. These results suggest that G. radix is able to perform the bone formation and prevent osteoporosis.

An Outlook on Cereal Grains Production in South Korea Based on Crop Growth Simulation under the RCP8.5 Climate Change Scenarios (RCP8.5 기후조건의 작물생육모의에 근거한 우리나라 곡물생산 전망)

  • Kim, Dae-Jun;Kim, Soo-Ock;Moon, Kyung-Hwan;Yun, Jin-I.
    • Korean Journal of Agricultural and Forest Meteorology
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    • v.14 no.3
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    • pp.132-141
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    • 2012
  • Climate change impact assessment of cereal crop production in South Korea was performed using land attributes and daily weather data at a farm scale as inputs to crop models. Farmlands in South Korea were grouped into 68 crop-simulation zone units (CZU) based on major mountains and rivers as well as existing land use information. Daily weather data at a 1-km grid spacing under the A1B- and RCP8.5 scenarios were generated stochastically to obtain decadal mean of daily data. These data were registered to the farmland grid cells and spatially averaged to represent climate conditions in each CZU. Monthly climate data for each decade in 2001~2100 were transformed to 30 sets of daily weather data for each CZU by using a stochastic weather generator. Soil data and crop management information for 68 CZU were used as inputs to the CERES-rice, CERE-barley and CROPGRO-soybean models calibrated to represent the genetic features of major domestic cultivars in South Korea. Results from the models suggested that the heading or flowering of rice, winter barley and soybean could be accelerated in the future. The grain-fill period of winter barley could be extended, resulting in much higher yield of winter barley in most CZUs than that of rice. Among the three major cereal grain crops in Korea, rice seems most vulnerable to negative impact of climate change, while little impact of climate change is expected on soybeans. Because a positive effect of climate change is projected for winter barley, policy in agricultural production should pay more attention to facilitate winter barley production as an adaptation strategy for the national food security.

Effect of Ginseng Saponin on LDL Receptor Biosynthesis (인삼사포닌의 저밀도지질단백질(LDL)수용체에 미치는 영향)

  • Joo Chung No;Lee Hee Bong;Lee Yong Woo;Kang In Chul
    • Proceedings of the Ginseng society Conference
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    • 1988.08a
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    • pp.47-54
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    • 1988
  • Cholesterol a component of all eucaryotic plasma membranes. is essential for the growth and viability of cells in higher organisms. However. too much cholesterol can be lethal because of atherosclerosis resulting from the deposition of cholesterol ester plaques. It was attempted in this study to understand the preventive effect of ginseng saponin. one of the major components of the roots of Panax ginseng C.A. Meyer. against hypercholesterolemia induced by high cholesterol diet. $^{125}I-LDL$ was injected intravenously to rabbits and rats. which were fed a high cholesterol diet with and/or without ginseng saponin for 12 days. The disappearance of the radioactivity occurred faster in the test group than the control. The effect of saponin fraction from Panax ginseng C.A. Meyer and the purified ginsenosilks. $Rb_1,\;Rb_2,\;Re\;and\;Rg_1,$ on LDL receptor biosynthesis in high cholesterol fed rat has been investigated. Analysis of LDL receptors from various organs such as liver. kidney. adrenal cortex and testis showed that the population of LDL receptors of test group significantly higher than that of the control. It was also found that liver homogenate containing ginsenosides $(10^{-3}-10^{-4}\%)$ stimulated the biosynthesis of bile acid form cholesterol. From the above results. it seemed that ginsenosides lower the cholesterol level by stimulating cholesterol metabolism. which result in the suppression of the inhibitory action of cholesterol on LDL receptor biosynthesis.

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Characterization and Purification of the Bacteriocin Produced by Bacillus licheniformis Isolated from Soybean Sauce (간장에서 분리한 Bacillus licheniformis가 생산하는 박테리오신의 특성 및 정제)

  • Jung, Sung-Sub;Choi, Jung-I;Joo, Woo-Hong;Suh, Hyun-Hyo;Na, Ae-Sil;Cho, Yong-Kweon;Moon, Ja-Young;Ha, Kwon-Chul;Paik, Do-Hyeon;Kang, Dae-Ook
    • Journal of Life Science
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    • v.19 no.7
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    • pp.994-1002
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    • 2009
  • A bacteriocin-producing bacterium identified as Bacillus licheniformis was isolated from soybean sauce. Antibacterial activity was confirmed by paper disc diffusion method, using Micrococcus luteus as a test organism. The bacteriocin also showed antibacterial activities against Bacillus sphaericus, Lactobacillus bulgaricus, Lactobacillus planiarum, Paenibacillus polymyxa, and Pediococcus dextrinicus. Optimal culture conditions for the production of bacteriocin was attained by growing the cells in an MRS medium at a pH of 6.5~ 7.0 and a temperature of 37$^\circ$C for 36$\sim$48 hr. Solvents such as chloroform, ethanol, acetone, and acetonitrile had little effect on bacteriocin activity. However, about 50% of bacteriocin activity diminished with treatment of methanol and isopropanol at the final concentration of 50% at 25$^\circ$C for 1 hr. It was stable against a pH variation range from 3.0 and 7.0, but the activity reduced to 50% at a pH range from 9.0 to 11.0. It's activity was not affected by heat treatment at 100$^\circ$C for 30 min and 50% of activity was retained after heat treatment at 100$^\circ$C for 60 min, showing high thermostability. The bacteriocin was purified to a homogeneity through ammonium sulfate precipitation, SP-Sepharose ion-exchange chromatography, and reverse-phase high-performance liquid chromatography (HPLC). The entire purification protocol led to a 75-fold increase in specific activity and a 13.5% yield of bacteriocin activity. The molecular weight of purified bacteriocin was estimated to be about 2.5 kDa by tricine-SDS-PAGE.

Anti-Oxidative and Anti-Inflammatory Activities of Euptelea Pleiosperma Ethanol Extract (Euptelea pleiosperma 에탄올 추출물의 항산화 및 항염증 활성)

  • Jin, Kyong-Suk;Park, Jung Ae;Lee, Ji Young;Kang, Ji Sook;Kwon, Hyun Ju;Kim, Byung Woo
    • Microbiology and Biotechnology Letters
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    • v.42 no.2
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    • pp.170-176
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    • 2014
  • In this study, the anti-oxidative and anti-inflammatory activities of Euptelea pleiosperma ethanol extract (EPEE) were evaluated using in vitro assays and cell culture model systems. EPEE possessed a more potent scavenging activity against 1,1-diphenyl-2-picryl hydrazyl than the ascorbic acid used as a positive control. EPEE effectively suppressed lipopolysaccharide (LPS), in addition to hydrogen peroxide induced reactive oxygen species on RAW 264.7 cells. Furthermore, EPEE induced the expression of the anti-oxidative enzyme heme oxygenase 1 (HO-1) and its upstream transcription factor, nuclear factor-E2-related factor 2 (Nrf2), dose and time dependently. The modulation of HO-1 and Nrf2 expression might be regulated by mitogen-activated protein kinases and phosphatidyl inositol 3 kinase/Akt as their upstream signaling pathways. On the other hand, EPEE inhibited LPS induced nitric oxide (NO) formation without cytotoxicity. Suppression of NO formation was the result of the down regulation of inducible NO synthase (iNOS) by EPEE. Suppression of NO and iNOS by EPEE may be modulated by their upstream transcription factor, nuclear factor ${\kappa}B$, and AP-1 pathways. Taken together, these results provide important new insights into E. pleiosperma, namely that it possesses anti-oxidative and anti-inflammatory activities, indicating that it could be utilized as a promising material in the field of nutraceuticals.

Monthly HPLC Measurements of Pigments from an Intertidal Sediment of Geunso Bay Highlighting Variations of Biomass, Community Composition and Photo-physiology of Microphytobenthos (HPLC를 이용한 근소만 조간대 퇴적물내의 저서미세조류 현존량, 군집 및 광생리의 월 변화 분석)

  • KIM, EUN YOUNG;AN, SUNG MIN;CHOI, DONG HAN;LEE, HOWON;NOH, JAE HOON
    • The Sea:JOURNAL OF THE KOREAN SOCIETY OF OCEANOGRAPHY
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    • v.24 no.1
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    • pp.1-17
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    • 2019
  • In this study, the surveys were carried out from October (2016) to October (2017) along the tidal flat of Geunso Bay, Taean Peninsula of the western edge of Korea. The sampling trips were carried out for a total of 16 times, once or twice a month. In order to investigate the monthly variation of the microphytobenthos (MPB) biomass, community composition and photo-physiology were analyzed by HPLC (High performance liquid chromatography). The total chlorophyll a (TChl a) concentrations used as an indicator of biomass of MPB in the upper 1 cm sediment layer ranged from 40.4 to $218.9mg\;m^{-2}$ throughout the sampling period. TChl a concentrations showed the maximum level on $24^{th}$ of February and remained high throughout March after which it started to declined. The biomass of MPB showed high values in winter and low values in summer. The monthly variations of Phaeophorbide a concentrations suggested that the low grazing intensity of the predator in the winter may have partly attributed to the MPB winter blooming. As a result of monthly variations of the MPB community composition using the major marker pigments, the concentrations of fucoxanthin, the marker pigment of benthic diatoms, were the highest throughout the year. The concentrations of most of the marker pigments except for chlorophyll b (chlorophytes) and peridinin (dinoflagellates) increased in winter. However, the concentrations of fucoxanthin increased the highest, and the relative ratios of the major marker pigments to TChl a except fucoxanthin decreased during the same period. The vertical distribution of Chl a and oxygen concentrations in the sediments using a fluorometer and an oxygen micro-optode Chl a concentrations decreased with oxygen concentrations with increasing depth of the sediment layers. Moreover, this tendency became more apparent in winter. The Chl a was uniformly vertical down to 12 mm from May to July, but the oxygen concentration distribution in May decreased sharply below 1 mm. The increase in phaeophorbide a concentration observed at this time is likely to be caused by increased oxygen consumption of zoobenthic grazing activities. This could be presumed that MPB cells are transported downward by bioturbation of zoobenthos. The relative ratios (DT/(DD+DT)) obtained with diadinoxanthin (DD) and diatoxanthin (DT), which are often used as indicators of photo-adaptation of MPB, decreased from October to March and increased in May. This indicated that there were monthly differences in activity of Xanthophyll cycle as well.

Effects of Microbial Fermentation on the Antioxidant Activities of Protaetia brevitarsis Larvae (미생물 발효가 흰점박이꽃무지(Protaetia brevitarsis) 유충의 항산화 활성에 미치는 영향)

  • Han Bi Kim;Hye Soo Kim;Soo Jeong Cho
    • Journal of Life Science
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    • v.33 no.12
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    • pp.1052-1061
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    • 2023
  • This study was carried out to evaluate the effect of fermentation by B. subtilis (BPLE), L. brevis (LPLE), S. cerevisiae (SPLE) and C. militaris (CPLE) on the antioxidant activity of Protaetia brevitarsis larvae fed with mushroom substrates (king oyster mushroom). The total polyphenol content of Protaetia brevitarsis larvae (PLE), BPLE, LPLE, SPLE and CPLE were 58.07±0.67, 83.33±0.98, 79.21±1.32, 61.02±0.87 and 57.90±1.02 mg GAEs/extract g, respectively. The flavonoid contents of the PLE, BPLE, LPLE, SPLE and CPLE were 17.35±1.57, 19.49±0.95, 16.90±1.57, 18.12±0.95 and 16.99±0.95 mg QEs/extract g, respectively. The DPPH radical scavenging activity showed no significant difference between the PLE, BPLE, LPLE, SPLE and CPLE at a concentration of 0.2 mg/ml. However, at a concentration of 0.4 mg/ml or more, the DPPH radical scavenging activity of the BPLE and LPLE was higher than that of the PLE. The reducing power of the BPLE and LPLE was also higher than that of the PLE, and more than twice as high at a concentration of 0.8 mg/ml or more. The ORAC value of the BPLE (79.77±0.82 uM TEs/extract g) was higher than that of the PLE (61.34±0.97 uM TEs/extract g). A WST-1 assay of the RAW 264.7 cells indicated that the PLE, BPLE, LPLE, SPLE and CPLE showed no cytotoxicity.