• Title/Summary/Keyword: R&D activity

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2D-QSAR and HQSAR Analysis on the Herbicidal Activity of New Cyclohexanedione Derivatives (새로운 Cyclohexanedione계 유도체의 제초활성에 관한 2D-QSAR 및 HQSAR 분석)

  • Kim, Yong-Chul; Hwang, Tae-Yeon;Sung, Nack-Do
    • The Korean Journal of Pesticide Science
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    • v.12 no.1
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    • pp.9-17
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    • 2008
  • QSARs (Quantitative structure-activity relationships) between a series of new cyclohexanedione derivatives (5-benzofuryl-2-[1-(alkoxyimino)-alkyl]-3-hydroxycyclohex-2-en-1-ones) and their herbicidal activity against Rice plant (Oryza sativa L.) and Barnyard grass (Echinochloa crus-galli.) were discussed quantitatively using 2D-QSAR and holographic (H) QSAR methods. Generally, the HQSAR models have better predictability and fitness than the 2D-QSAR models. The herbicidal activities against Barnyard grass with 2D-QSAR II model were dependent upon Balaban indice (BI) of molecule and hydrophobicity of $R_1$ and $R_3$ group. And also, the $R_3=ethyl$ group, according to the information of the optimized HQSAR IV model, was more contribute to the herbicidal activities against Rice plant, while the 5-(cyclohex-3-enyl)-2,3-dihydrobenzofuran ring part was not contribute to the herbicidal activities against two plants.

Antiplatelet Action of Ilexoside D, a Triterpenoid Saponin from Ilex pubescens

  • Lee, Dug-Keun;Lee, Hye-Sun;Huh, Min-Do;Lee, Chul-Hoon;Lee, Young-Su;Kim, Hyun-Su;Han, Yong-Nam
    • Archives of Pharmacal Research
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    • v.14 no.4
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    • pp.352-356
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    • 1991
  • The anti-platelet activity of ilexoside D isolated from the roots of Ilex pubescens Hook. et Arn. was investigated in in vitro and ex vivo models of platelet aggregation induced by ADP, thrombin or collagen in rats. In vitro ilexoside D inhibited more effectively platelet aggregation induced by ADP and thrombin than by collagen as compared with aspirin. Ex vivo ilexoside D also inhibited platelet aggregation induced by ADP and collagen, but not by thrombin, and the inhibitory action of ilexoside D was more effective than that of aspirin. However, in vitro ilexoside D inhibited very poorly the generation of malonyldialdehyde, which is known to be concomitantly released with thromboxane $A_2$ during platelet aggregation. These results suggest that the anti-platelet activity of ilexoside D may not be responsible for prostaglandin synthesis in platelets.

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Effect of Melothria heterophylla Extract on Expression of Matrix Metalloproteinase-1 in Human Skin Fibroblasts (백렴 추출물의 Matrix Metalloproteinase-1 발현 저해 효과)

  • Cho , Young-Ho;Sim , Gwan-Sub;Kim , Jin-Hui;Park , Sung-Min;Lee , Bum-Chun;Pyo , Hyeong-Bae;Yun , Yeo-Pyo;Park , Hum-Dai
    • YAKHAK HOEJI
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    • v.48 no.6
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    • pp.358-363
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    • 2004
  • Matrix metalloproteinases (MMPs) are known to play an important role in photoaging by mediating the degradation of extracellular matrix proteins. In this study, to develop a n ew anti-aging agent, we investigated the antioxidant activity and the inhibitory effect of Melothria heterophylla extract on expression of MMP-1 in UVA-irradiated human dermal fibroblasts and MMP-1 activity. The M.heterophylla extract was found to scavenge radicals and reactive oxygen species (ROS) with the $SC_{50}$ values of $13{\mu}g/ml$ against 1,1-diphenyl-2-picrylhydrazyl (DPPH) radicals and $20{\mu}g/ml$ against superoxide radicals in the xanthine/xanthine oxidase system, respectively. UVA-induced MMP-1 expression was reduced about 80% by $100{\mu}g/ml$ of the M.heterophylla extract but MMP-1 Mrna expression was not inhibited. Therefore, we conclude that the M.heterophylla extract significantly inhibits MMP-1 expression at the protein level. Also, the M.heterophylla extract inhibited MMP-1 activity in a dose dependent manner. From these results, we suggest that the M.heterophylla extract can be used as a new anti-aging agent by antioxidant activity, regulation of UVA-induced MMP-1 production, and inhibition of MMP-1 activity.

New Anti-aging & Moisturizer Ingredients of Exopolysaccharides by Grifola frondosa

  • Bae, Jun-Tae;Lee, Bum-Chun;Yoon, Eun-Jeong;Kim, Jin-Hwa;Lee, Dong-Hwan;Pyo, Hyeong-Bae;Choe, Tae-Boo
    • Proceedings of the SCSK Conference
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    • 2003.09a
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    • pp.35-49
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    • 2003
  • In this study, in an attempt to search for functional cosmetic ingredients from higher fungal, we have produced exopolysaccharides (GF-l, approximately carbohydrate 75%, protein 25%) and polysaccharide (GF-2) of mycelium extract, by submerged culture of Grifolafrondosa. For applications in anti-aging cosmetic field, we investigated the diverse biological activities. Antioxidant activity and inhibition of Matrixmetalloproteinases (MMPs) were investigated enzymatic assays by measuring the superoxide scavenging activity using xanthine-xanthine oxidase system and the proteolytic activity of MMPs using EnzChek Collagenase/Gelatinase kits, respectively. GF-l polysacchairde showed inhibition of superoxide radical by 90% at a concentration of 0.2% (w/v) and inhibition of collagenase by 45% at 0.2% (w/v). GF-2 polysaccharide of mycelium extract also exhibited good antioxidant activity. However, MMPs inhibition activity was relatively lower level compared to GF-l polysaccharides. The treatment of human dermal fibroblast (HDF) with GF-l and GF-2 polysaccharides increased the proliferation of fibroblast by approximately 23-25% at a concentration of 0.5% (w/v), also showed collagen synthesis increase in HDF by about 50% at 0.5% (w/v) compared to that of untreated control. We also report the moisturizing effects of polysaccharides in cosmetic products (O/W emulation) and its own ingredient, in vitro and in vivo. The GF-1 polysaccharide showed higher moisturizing ability than sodium hyaluronate, which is the most commonly used moisturizers ingredient. These results suggest the GF-l polysaccharide, protein-bound polysaccharide, may be used as an ingredient for new moisturizing and anti-aging cosmeceuticals.

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Synthesis and Antimicrobial Activity of 7-[(3-Methylthio or 3-Methylthiomethyl) -3-pyrrolinyl]quinolone-3-carboxylic Acids (7-[(3-메틸티오 또는 3-메틸티오메틸)-3-피롤리닐]퀴놀론-3-카르복실산의 합성과 항균작용)

  • Lee, Jae-Wook;Son, Ho-Jung;Lee, Kyu-Sam;Yu, Young-Hyo;Kim, Dae-Young
    • YAKHAK HOEJI
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    • v.38 no.5
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    • pp.520-524
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    • 1994
  • A number of 7-[(3-methylthio or methylthiomethyl)-3-pyrrolinyl] quinolone-3-carboxylic acids were synthesised by condensation of 7-fluoro substituted quinolone-3-carboxylic acid with 3-methylthio-3-pyrroline or 3-methylthiomethyl-3-pyrroline. The in vitro antimicrobial activity of them were tested against twenty species of Gram-positive or Gram-negative microorganisms. It showed remarkable antibacterial activity, particularly against Gram-positive microoganisms. Among those 1-cyclopropyl-6,8-difluoro-7-[(3-methylthiomethyl) -3-pyrrolinyl]-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid(12a) and 1-cycl opropyl-6-fluoro-8-chlore-7-[(3-methylthiomethyl)-3-pyrrolinly]-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid(12b) showed the most potent in vitro antibacterial activity.

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3D-QSAR Analysis on the Antitrypanosomal Activity of Phenoxy, Phenylthio or Benzyloxy Group Substituted Quinolone Analogues (Phenoxy, Phenylthio 및 Benzyloxy-기가 치환된 Quinolone 유도체들의 항트리파노소마 활성에 대한 3D-QSAR 분석)

  • Myung, Pyung-Keun;Kang, Na-Na;Kim, Sang-Jin;Sung, Nack-Do
    • YAKHAK HOEJI
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    • v.54 no.4
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    • pp.288-294
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    • 2010
  • Three dimensional quantitative-structure relationships (3D-QSARs) models between structures of phenoxy, phenylthio or benzyloxy substituted quinolone analogues and their antitrypanosomal activity against Chagas disease (Trypanosoma cruzi) were derived and discussed quantitatively using comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA) methods. The optimized CoMFA 1 model ($q^2$=0.528 and $r^2$=0.964) showed the best statistical results. According to the optimized CoMFA 1 model, the antitrypanosomal activities were dependent on the steric (60.0%) and electrostatic (36.2%) factors of quinolone derivatives. From the contour maps, it is predicted that the activity will be increased when sterically favored groups were located in $R_4$ and $R_5$ position and sterically disfavored groups were located in $R_2$ position. Also, the positively charged groups on $R_2$ would be able to increase the antitrypanosomal activities.

Relationships among Physical Activity Level, Health-promoting Behavior, and Physiological Variables in Korean University Students

  • Bang, Kyung-Sook;Song, Min Kyung;Park, Se-Eun;Kim, Hyungkyung
    • Perspectives in Nursing Science
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    • v.15 no.1
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    • pp.11-17
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    • 2018
  • Purpose: Many Korean college students suffer from physical inactivity and mental health problems. However, it has not been sufficiently reported how this lack of exercise and health-related behavior affect their health. The present study was performed to identify the relationships among physical activity level, health-promoting behavior, and physiological variables in Korean undergraduate and graduate students. Methods: Participants were 115 undergraduate and graduate students from one university in Seoul. The Pearson's correlation analysis was performed using SPSS for Windows. Results: Physical activity level had significant positive correlations with health-promoting behavior (r=.32, p=.001) and exercise self-efficacy (r=.25, p=.008), and health-promoting behavior had a significant correlation with depression (r=-.33, p<.001) and exercise self-efficacy (r=.44, p<.001). Additionally, physical activity level had significant correlations with triglyceride (r=-.20, p=.034) and vitamin D (r=.20, p=.029) levels. The high density cholesterol level had significant negative correlations with systolic blood pressure (r=-.33, p<.001), diastolic blood pressure (r=-.29, p=.002), and vitamin D (r=-.20, p=.035) levels. Conclusion: Physical activity level or health-promoting behavior had significant relationships with the health status of college students. Strategies need to be developed to improve health-promoting behaviors among college students.