• 제목/요약/키워드: Xanthine

검색결과 828건 처리시간 0.025초

Topomer CoMFA Analysis of Xanthine Oxidase inhibitors

  • Santhosh Kumar, N
    • 통합자연과학논문집
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    • 제10권4호
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    • pp.192-196
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    • 2017
  • Xanthine Oxidase is an enzyme, which oxidizes hypoxanthine to xanthine, and xanthine to uric acid. It is widely distributed throughout various organs including the liver, gut, lungs, kidney, heart, brain and plasma. It is involved in gout pathogenesis. Hence, in the present study, topomer based Comparative Molecular Field Analysis (topomer CoMFA) was performed on a series of Xanthine oxidase antagonist named 2-(indol-5-yl) thiazole derivatives. The best topomer CoMFA model was obtained with significant cross-validated correlation coefficient ($q^2$ = 0.572) and non cross-validated correlation coefficients ($r^2$ = 0.937). The model was evaluated with six external test compounds and its $r^2{_{pred}}$ was found to be 0.553. The steric and electrostatic contribution map show that presence of bulky and electropositive group in indole thiazole ring is necessary for improving the biological activities of the compounds. The generated topomer CoMFA model could be helpful for future design of novel and structurally related xanthine oxidase antagonists.

수원 5호 메밀의 유리라디칼 소거 및 Xanthine oxidase 활성 저해 (Free radical Scavenging Activities and Inhibitory Effects on Xanthine oxidase of Buckwheat (Suwon No. 5))

  • 서형주;정수현;김영순;이성동
    • 한국식품영양과학회지
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    • 제26권3호
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    • pp.411-416
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    • 1997
  • To examine the free radical scavenging activities from buckwheat, Suwon No. 5 was extracted with various solvents. The seed of Suwon No. 5 had a high contents of carbohydrate, but the vegetable of that had a 31.4% of protein, 28.6% of ash and 25.7% carbohydrate as moisture free basis. Phenols contents of vegetable extracts had higher than those of seed extracts. Acetone extract of vegetable showed the greatest electron donating ability. Butanol and acetone extracts of vegetable showed high inhibitory effect on lipid peroxidation. Acetone extract of vegetable has also excellent activity in the superoxide radical scavenging activity by xanthine/xanthine oxidase-cytochrome c reduction system. The inhibitory effects of extracts on xanthine oxidase were measured. Acetone extract had the strongest inhibitory effect on xanthine oxidase and $IC_{50}$ was 2.2$\mu\textrm{g}$.

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Effect of Heat-treated Ceruloplasmin on the Hepatic xanthine Oxidase Activity and Type Conversion

  • Huh, Keun;Shin, Uk-Seob;Lee, Sang-Il
    • Archives of Pharmacal Research
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    • 제18권1호
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    • pp.56-59
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    • 1995
  • The effect of ceruloplasmin or copper ion on hepatic xanthine oxidase activity and type conversion was investigated using rat liver in vitro. It was observed that ceruloplasmin increased xanthine oxidase type conversion depending on duration of its storage. Xanthine oxidase (type O) activity and type conversion in incubation mixture was increased by the addition of heated celuroplasmin in a temperature dependent manner. The type conversioin of xanthine oxidase induced by heated ceruloplasmin was retumed to normal by the tratment with DTT or penicillamine. The effect of copper ion on type conversion of xanthine oxidase was similar to that of heated ceruloplasmin.

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소의 갑상선에 있는 크산친 옥시다아제에 관한연구 [제2보] 효소의 조성과 특성- (Studies on Xanthine Oxidase from Bovine Thyroid Glands -[Part 2] Composition and Some Properties-)

  • 이효사
    • Applied Biological Chemistry
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    • 제21권3호
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    • pp.137-143
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    • 1978
  • 소의 갑상선에 있는 xanthine oxidase 효소도 flavin adenine dinucleotide(FAD), 모리브덴 및 철을 cofactor로서 가지고 있었으며 그 비율은 1 : 0.36 : 1.6이었다 갑상선 xanthine oxidase의 분자량은 gel filtration과 gel electrophoresis방법으로 측정하였을 때 우유에서 추출한 xanthine oxidase의 분자량과 큰 차이가 없었다. 그 효소의 활성도는 pH7.8에서 가장 높았고 isoelectric point는 electrofocusing으로 측정하였을 때 pH 6.2 였다. SDS-polyacrylamide gel electrophoresis 실험 결과는 소의 갑상선에서 추출된 xanthine oxidase가 세개의 subunit로 분해되었음을 지적했고, 최소 단위분자량 65,000정도의 polypeptide 4개로서 완전한 xanthine oxidase 한 분자를 구성하고 있을 가능성을 보였다. 갑상선 호소의 absorption spectrum을 우유에서 추출된 효소와 비교하였을 때 상당한 상이점을 나타내었다.

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바위솔 추출물의 항산화활성 및 암세포 증식억제 (The activity of antioxidants and suppression of cancer cell proliferation in extracts of Orostachys japonicus A. Berger)

  • 김충현;박재호;임종국;이건주;정규영;정형진
    • 한국약용작물학회지
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    • 제11권1호
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    • pp.31-39
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    • 2003
  • 바위솔의 추출물로부터 항산화 활성 및 동물 항암세포를 이용한 생물학적 특성을 조사 해 본 결과는 다음과 같다. 생육지별 DPPH 프리라디칼 소거 및 xanthine/xanthine oxidase 억제 활성비교에서 재배지에서 수확한 시료의 활성이 $6.07(IC_{50}:{\mu}g/m{\ell})$로 가장 높았다 생육시기별 DPPH 프리라디칼 소거 및 xanthine/xanthine oxidase 억제의 활성은 9월 수확물이 가장 활성이 높았다. 실리카겔 컬럼크로마토그래피를 이용한 항산화물질 분리결과에서 S-4 분획물의 DPPH와 xanthine oxidase 억제활성이 $5.02(IC_{50}\;:\;{\mu}g/m{\ell})$$6.18(IC_{50}:{\mu}g/m{\ell})$을 나타냄으로써 높은 분리효율를 보였다. 항산화활성이 가장 높았던 LH-4 분획물의 주요화합물은 GC/MS에 의하여 지방산, 폴리페놀화합물 및 페놀유도체로 동정되었으며 alpha-androsta-7,14-diene과 1,2,3-benzenetriol이 주 물질이었다. POD 및 SOD 활성은 생육지간에 재배지, 산, 바닷가 순으로, 생육시기간에는 시기가 늦을수록 높게 나타났다 SOD 동위효소의 밴드수는 전 생육지, 전 생육시기에서 공히 2개의 밴드가 나타났으나, 그 세기는 재배지와 9월의 수확물이 가장 높은 활성을 나타내었다. 정제된 LH-4 분획물은 HL-60 세포의 종양증식을 억제시켰으며 종양유발유전자와 IPTG로 콜로니 형성을 유도한 암세포(2-12 cells)에서 분획물 400ppm 처리와 negative control 처리간의 colony형성은 유의차가 없었다.

Effects of $\beta$-Mercaptoethanol on Lipid Peroxidation and Fertilization Ability In Vitro by Xanthine-Xanthine Oxidase System in Pig

  • Sa S.J.;H.T. Cheong;B.K. Yang;Kim, C.I.;Park, C.K.
    • 한국동물번식학회:학술대회논문집
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    • 한국동물번식학회 2002년도 춘계학술발표대회 발표논문초록집
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    • pp.74-74
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    • 2002
  • This study was undertaken to evaluate the effects of β-mercaptoethanol on lipid peroxidation and fertilization ability in vitro by xanthine (X)-xanthine oxidase (XO) system in boar spermatozoa frozen-thawed. When spermatozoa were inseminated in medium with X and/or XO, the penetration rates in all conditions were higher in medium with that than without β-mercaptoethanol. However, significant differences were not observed between medium with and without β-mercaptoethanol. The lipid peroxidation of sperm was evaluated on the basis of malondialdehyde (MDA) production. (omitted)

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Phenolic Compounds with Antioxidant Activity on DPPH Free Radical Scavenging and Inhibition of Xanthine/Xanthine Oxidase from the Flowers of Chrysanthemum morifolium

  • Chung, Ha-Sook
    • Preventive Nutrition and Food Science
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    • 제11권3호
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    • pp.198-203
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    • 2006
  • The flowers of Chrysanthemum morifolium (Compositae) were investigated for their biofunctional components. Antioxidant compounds were identified from the flower of Chrysanthemum morifolium, through activity-guided fractionation and repeated column chromatographic separations. The structures of the isolated compounds were characterized as chlorogenic acid (1), luteolin (2) and quercitrin (3) by the analysis of physico-chemical and spectral data. Their antioxidant effects were evaluated by assaying for 1,1-diphenyl-2-picrylhydrazyl free radical scavenging activity and inhibition of xanthine/xanthine oxidase activity.

The Effect of Hydrogen Peroxide-Treated Metallothionein on the Hepatic Xanthine Oxidase Activity

  • Huh, Keun;Shin, Uk-Seob;Lee, Sang-Il
    • BMB Reports
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    • 제28권6호
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    • pp.490-493
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    • 1995
  • We investigated the effect of hydrogen peroxide-treated metallothionein on the hepatic xanthine oxidase activity in vitro. When the metallothionein was preincubated with 1 mM of hydrogen peroxide, the activity of xanthine oxidase and type conversion were elevated dose-dependently by the addition of metallothionein into the reaction mixture. While increasing the treatment of hydrogen peroxide to the $50{\mu}g$of metallothionein, the xanthine oxidase activity and type conversion ratio were remarkably elevated dose dependently compared to the control. When cadmium ion was added to the reaction mixture, the increasing pattern of the enzyme activity was similar to the effect of hydrogen peroxide-treated metallothionein. DTT or penicillamine restored the increasing activity and type conversion of xanthine oxidase by the cadmium ion to the control level.

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Comparative Molecular Similarity Index Analysis on 2-(indol-5-yl)thiazolederivatives as Xanthine Oxidase(XO)inhibitors

  • Nagarajan, Santhosh Kumar;Madhavan, Thirumurthy
    • 통합자연과학논문집
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    • 제9권3호
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    • pp.190-198
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    • 2016
  • Xanthine Oxidase is an enzyme, which oxidizes hypoxanthine to xanthine, and xanthine to uric acid. It is widely distributed throughout various organsincluding the liver, gut, lung, kidney, heart, brain and plasma. It is involved in gout pathogenesis. In this study, we have performed Comparative Molecular Field Analysis (CoMSIA) on a series of 2-(indol-5-yl) thiazole derivatives as xanthine oxidase (XO) inhibitors to identify the structural variations with their inhibitory activities. Ligand based CoMSIA models were generated based on atom-by-atom matching alignment. In atom-by-atom matching, the bioactive conformation of highly active molecule 11 was generated using systematic search. Compounds were aligned using the bioactive conformation and it is used for model generation. Different CoMSIA models were generated using different alignments and the best model yielded across-validated $q^2$ of 0.698 with five components and non-cross-validated correlation coefficient ($r^2$) of 0.992 with Fisher value as 236.431, and an estimated standard error of 0.068. The predictive ability of the best CoMSIA models was found to be $r{^2}_{pred}$ 0.653. The study revealed the important structural features required for the biological activity of the inhibitors and could provide useful for the designing of novel and potent drugs for the inhibition of Xanthine oxidase.

버섯류로부터 항통풍성 Xanthine oxidase 저해물질의 탐색 (Screening of Anti-gout Xanthine Oxidase Inhibitor from Mushrooms)

  • ;송정화;서건식;노형준;유영복;이종수
    • 한국균학회지
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    • 제38권1호
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    • pp.85-87
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    • 2010
  • 버섯으로부터 새로운 항통풍성 소재를 개발하여 이를 대체의약의 소재나 건강 기능성 제품 개발에 응용할 수 있는 자료를 얻고자 12종의 국내 버섯 자실체들의 물 추출물을 제조하여 이들의 항통풍성 xanthine oxidase 저해 활성을 측정하였다. 시료 버섯 가운데 신령 버섯 자실체의 물 추출물이 가장 높은 72.9%의 저해 활성을 보였고 이 저해 물질은$30^{\circ}C$에서 24시간 추출하였을 때 가장 많이 용출 되었다.