• Title/Summary/Keyword: Anti-E+c

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Synthesis of Pyrazoloquinolines as Gastric $H^+/K^+$-ATPase Inhibitors

  • G. D. Kalayanov;Kang, S. K.;Cheon, H.G.;Lee, S.G.;Yum, E. K.;Kim, S. S.;Choi, J.-K.
    • Bulletin of the Korean Chemical Society
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    • v.19 no.6
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    • pp.667-671
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    • 1998
  • A series of 1-aryl-lH-pyrazolo[4,3-c]quinolines and 2-aryl-2H-pyrazolo[4,3-c]quinolines are prepared by reacting 3-acyl-4-chloroquinolines in ethanol or 3-acyl-4(lH)-quinolone in acetic acid with appropriate hydrazines as possible anti-ulcer agents. A regiospecific synthesis of 1-aryl-lH-pyrazolo[4,3-c]quinolines is also achieved. The central pyridine ring could be easily reduced by catalytic hydrogenation.

Antioxidant and Anti-Inflammatory Activities of Extracts from Eugenia caryophyllata Thunb. (정향 열수 및 에탄올 추출물의 항산화 및 항염 효과)

  • Oh, Hee-Kyung
    • Journal of the Korean Society of Food Culture
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    • v.31 no.5
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    • pp.481-488
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    • 2016
  • The objective of this study was to investigate the antioxidant and anti-inflammatory activities of Eugenia caryophyllata Thunb. water and 70% ethanol extracts. The content of total polyphenol was significantly higher in water extract than in 70% ethanol extract. The DPPH radical scavenging activity of water extract was similar to that of Vit. C at a concentration of $1,000{\mu}g/mL$. The ABTS radical scavenging activities of water and 70% ethanol extract were similar to that of Vit. C at a concentration of $1,000{\mu}g/mL$. SOD-like activity of water extract was higher than that of 70% ethanol extract at a concentration of $1,000{\mu}g/mL$ but lower than that of Vit. C. The DPPH radical scavenging activity, ABTS radical scavenging activity, and SOD-like activity increased as concentrations of water and 70% ethanol extracts increased. Cell cytotoxicity was not observed at all concentrations except at $100{\mu}g/mL$ concentration of water extract. Inhibitory activity on NO production effect of water extract was significantly higher than that of 70% ethanol extract. These results show that E. caryophyllata Thunb. has potent biological activities, and their activities were different depending on extraction solvent.

Physicochemical Characteristics of Antidementia Acetylcholinesterase Inhibitor-containing Methanol Extract from Sorghum bicolor and Industrial Application (항치매성 Acetylcholinesterase저해물질을 함유하고 있는 수수 메탄올 추출물의 특성 및 산업적 응용)

  • Song, Jung-Eun;Lee, Jong-Soo
    • The Journal of Natural Sciences
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    • v.19 no.1
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    • pp.45-55
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    • 2008
  • Alzheimer's disease is charaterized by the acetylcholine depletion, amyloid b-protein aggregation and neurofibrillary tangles. The prevention of the breakdown of acetylcholine by acetylcholinesterase (AChE) inhibitor has the best clinically therapeutic efficacy for Alzheimer's disease patients. To develop new antidementia alternative drugs or nutraceuticals, methanol extracts of Sorghum bicolor was screened from various extracts of cereals and legumes as a potent AChE inhibitor-containing extract in previous paper. In this paper, physicochemical properties of the methanol extracts was investigated. The methanol extracts was soluble by water, methanol and DMSO and had 215 nm and 282nm of maximum absorption spectra. It was also stable at 20-$100^{\circ}C$ and pH 2.0-10.0 for 1 hr. Test product was prepared by using methanol extracts from Sorghum bicolor and changes of its quality during storge at $20^{\circ}C$ and $40^{\circ}C$ were investigated. It was very stable for 8 weeks at $40^{\circ}C$.

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Selection and Mechanism of Anti-Obesity Agents from Natural Products Based on Anti-Angiogenesis (신생혈관형성억제작용을 기반으로 한 항비만제제의 선별 및 작용기전)

  • Shin, Jin-Hyuk;Lee, Jin-Hee;Kang, Kyeong-Wan;Hwang, Jae-Ho;Han, Kyeong-Ho;Shin, Tai-Sun;Kim, Min-Yong;Kim, Jong-Deog
    • KSBB Journal
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    • v.24 no.2
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    • pp.122-130
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    • 2009
  • Anti-angiogenic mechanism was examined for anti-obesity agents with the extract of P.radix, P.semen, S.hebra and C.furctus through anti-cell adhesion effect and western blot. Cell adhesion molecules, VCAM-1 was supressed with the order of P.radix (0.2 ppm, 125%) > P.semen (0.5 ppm, 100%) > S.hebra (5.0 ppm, 114%) > C. furctus (5.0 ppm, 111.8%), ICAM-1 was inhibited by P.radix (0.25 ppm, 130%) > P.semen (0.5 ppm, 100%) > S.hebra (5.0 ppm, 138%) > C. furctus (5.0 ppm, 66.7%), E-Selectin was also supressed P.radix (0.25 ppm, 100%) > P.semen (1.0 ppm, 128%) > S.hebra (5.0 ppm, 120%) > C. furctus (5.0 ppm, 100.7%). And signal molecules, VE-cadherin was supressed by P.radix and S.hebra, ${\beta}$-catenin was inhibited by P.radix, and Akt was supressed all these 4 kinds of natural products. These P.radix, P.semen, S.hebra and C.furctus were showed the possibility of anti-obesity agents based on anti-angiogenesis.

Cloning of Xanthine Oxidase Gene from Mouse Liver cDNA Library

  • Lee, Chu-Hee;Lee, Sang-Il;Nam, Doo-Hyun;Heo, Geun
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1994.04a
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    • pp.261-261
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    • 1994
  • Bovine milk xanthine oxidase (E.C.1.1.3.22, XO) purchased from Sigma Chemical Co. had the three protein fragments below 150 kDa on 7.5% SDS-PAGE, which did not show enzyme activity. To remove these fragments, the enzyme preparation was further purified through Sephadex G-200 column chromatography. Two peaks exhibiting enzymatic activity were separated very closely to the void volume, which were revealed as two different enzyme forms, dimeric and monomeric, confirmed by activity staining on native PAGE. Anti sera-against each of the two enzyme forms were raised by subcutaneous injection at multiple sites on the back of rabbits during 4 weeks. On the immunodiffusion test, it was found that both of the antisera of the two forms could react with each other, which implied that their epitopes were identical In the Western blot analysis of mouse liver cytosol fraction, it was found that rabbit anti-XO antibody bound well with the protein band of monomeric mouse liver XO of about 150kDa. Based on this result, mouse liver cDNA 1 ibrary was screened by in situ hybridizat ion wi th rabbi t anti -XO antibody as probe. Through the immunological screening, recombinant phages giving positive signal by the production of XO were selected and further purified. To validate these clones, purified phages were lysogenized in E. coli Y1089 and their lysates were analysed for enzyme activity and immunoreactivity, It was verified that lysates of the purified recombinant phage lysogens exhibited the enzymatic activity as well as bound wi th XO antibody, when induced by IPTG. The above results assert that selected recombinant phage carries mouse liver XO gene.

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A Case Study on Caisson Foundation Grouting in Geo-Ga Bridge (거가대교 케이슨기초 그라우트 충전 사례연구)

  • Bae, Kyung-Tae;Cha, Kyung-Seob;Kim, Young-Jin;Park, Chung-Whan;Jeong, Gyeong-Hwan
    • Proceedings of the Korean Geotechical Society Conference
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    • 2010.03a
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    • pp.1046-1050
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    • 2010
  • During construction of a sea-crossing bridge grouting was used to fill densely the space between the bottom of caisson and the ground. This grout mixture was mixed with an anti-washout admixture after locating accurately the pre-cast caisson on three concrete landing pads. This method differs significantly from the costly conventional method, for bridge foundations offshore, where concrete is placed in situ after excavating inside of a temporary concrete coffering wall. To verify the grouting method in advance, the full-scale field tests were performed twice on land. After identifying the fluidity of the grout material to be filled, finding some possible problems with the main construction and revising the original design, the main construction has been continuing successfully with 20 caissons completed to date. The purpose of this paper is to introduce for the first time in Korea the grouting method including the automatic and the manual monitoring system based on the main construction of the caisson foundation.

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A Study on Welding Residual Stress by Numerical Simulation on friction Stir Welding

  • Bang, H.S.;Kim, H.J.;Go, M.S.;Chang, W.S.;Lee, C.W.
    • International Journal of Korean Welding Society
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    • v.2 no.1
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    • pp.62-66
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    • 2002
  • The Friction Stir Welding (FSW) is a new joining method that was developed at The Welding Institute (TWI) in England in 1991. It applied heating by the rotational friction and material plastic flow. It was developed as a new joining method to solve the problems of epochally in the welding of Al alloys. In the study, 6000series of Alloy composed of Al-Mg-Si, one of the Al alloys that are utilized for shipbuilding and construction, is selected as a specimen and the numerical is executed against the welded zone of FSW. The material used in this study had the unique properties of strength and anti-corrosion, but since the welded joint of this material is easily softened by the welding heat, FSW is executed and the numerical analysis is carried out around the joint. To examine the mechanical behaviors and properties, F.E.M analysis is executed and the developed thermal-elastic-plastic finite analysis are used.

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Anti-atherosclerotic Effect of Green Tea in Poluynsaturated Fatty Acids-treated Apo E KO Mice (식이불포화지방산을 섭취한 Apo E KO Mice에서의 녹차의 항동맥경화억제 효과)

  • Kim, Hyo-Sook;Lee, Myoung-Sook
    • Journal of Nutrition and Health
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    • v.44 no.6
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    • pp.465-473
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    • 2011
  • Dietary fatty acids are under intense research to identify anti-atherogenic mechanisms, so we investigated green tea powder (GT) as a protector against atherogenesis originating from lipid peroxidation such as 4-hydroxynonemal (4-HNE) and malondialdehyde (MDA) in different dietary fatty acid-treated apo E KO mice. Growth rate and dietary efficiency were lower in apo E KO mice with or without LA compared to wild type. Plasma total cholesterol (TC) and triacylglycerol (TG) did not correspond to values in other tissues, but TG in heart tissue decreased significantly by GT after linoleic acid (LA) or docosahexaenoic acid (DHA) was administered. LA induced apoptosis as evidenced by changes in aorta morphology and immunohistochemistry. Lipid peroxides (LPO) was increased in apo E KO mice with or without LA corresponding to the accumulation of 4-HNE or MDA in the proximal aorta above the atria. GT consumption tended to reduce the primary causal mechanism of atherogenic phenomena such as oxidizability in both LA and DHA treated atherogenic mice. A high polyunsaturated fatty acids (PUFA) diet involved the changes on stress-induced apoptotic signaling by increasing caspase 3, cytochrome c, and nuclear factor-${\kappa}B$ in the heart tissue, but decreasing the bcl-2 protein. However, GT remarkably reduced the expression of apoptotic signaling, in contrast to the PUFA diet. Therefore, the potential of GT as an anti-atherosclerotic dietary antioxidant was tested in this study.

The Effect of Bangpungtongsung-San on Model of Allergic Rhinitis (알러지성 비염 병태 모델에 대한 방풍통성산(防風通聖散)의 항알러지 효과)

  • Kim, Hee-Jeong;Park, Owe-Suk;Kim, Keoo-Seok;Cha, Jae-Hoon;Kim, Yoon-Bum
    • The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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    • v.19 no.1
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    • pp.21-30
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    • 2006
  • Background and Objective : Allergic rhinitis is a IgE-mediated hypersensitive reaction at nasal mucosa. In oriental medicine, Bangpungtongsung-San is clinically widely used for the treatment of the allergic rhinitis. The objective of this study is to investigate the effects of Bangpungtongsung-San on allergic rhinitis experimentally. Material and Methods : BALB/c mouse were divided into there groups: intact, control, experimental groups. Control and experimental group were induced allergic rhinitis by Ovalbumin as· the method of Levin and Vaz. Experimental group was orally administered the Bangpungtongsung-San for 28days. Total IgE, Interleukin-4, Interleukin-5 and $Interferon-{\gamma}$ were measured at three groups. The statistical significance was examined by Independent Samples T test. Results : 1. The experimental group shows increase of $IFN-{\gamma}$ by 17% compared with control group but there was no statistical significance. 2. The experimental group shows increase of IL-4 and IL-5 compared with control group but there was no statistical significance. 3. The experimental group shows increase of Total IgE and diminution of OVA-specific IgE by 32% compared with control group but there was no statistical significance. Conclusion : The effect of Bangpungtongsung-San on allergic rhinitis is not immunological but seems to be anti-imflammatory and anti-stress effect.

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