• Title/Summary/Keyword: xanthine

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Topomer CoMFA Analysis of Xanthine Oxidase inhibitors

  • Santhosh Kumar, N
    • Journal of Integrative Natural Science
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    • v.10 no.4
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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.

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

  • 서형주;정수현;김영순;이성동
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.26 no.3
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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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    • v.18 no.1
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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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Studies on Xanthine Oxidase from Bovine Thyroid Glands -[Part 2] Composition and Some Properties- (소의 갑상선에 있는 크산친 옥시다아제에 관한연구 [제2보] 효소의 조성과 특성-)

  • Lee, Hyo-Sa
    • Applied Biological Chemistry
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    • v.21 no.3
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    • pp.137-143
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    • 1978
  • Xanthine oxidase from bovine thyroid glands was found to contain FAD, molybdenum and iron in a ratio 1:0. 36:1. 6. The molecular weight of the thyroid enzyme was similar to that of the milk enzyme when estimated by gel filtration and polyacrylamide gel electrophoresis. The optimum pH for the enzyme activity was 7.8. The pH of the isoelectric point was determined to be 6.2 by electrofocusing. Sodium dodecyl sulfatepolyacrylamide gel electrophoresis experiment indicated that the enzyme was dissociated into subunits and that the molecular weight for the smallest subunit was 65,000 daltons. Absorption spectra were dissimilar between milk and thyroid xanthine oxidase.

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

  • Kim, Chung-Hyun;Park, Jae-Ho;Lim, Jong-Kuk;Lee, Kon-Joo;Chung, Gyu-Young;Jeong, Hyung-Jin
    • Korean Journal of Medicinal Crop Science
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    • v.11 no.1
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    • pp.31-39
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    • 2003
  • The antioxidative activities and biological properties in the EtOAc extracts and purified extracts of Orostachys japonicus were measured by assay of DPPH, xanthine/xanthine oxidase and mammalian cells(2-12). Scavenging of DPPH radical and inhibition of xanthine/xanthine oxidase of EtOAc extracts were showed the highest activity in the arable land and in September. The S-4 fraction showed the highest activity among the silica-gel column chromatography fractions. LH-4 fraction showed higher activity than the other fractionsins in assay of DPPH and xanthine/xanthine oxidase. Fatty acids and phenolic compounds were identified by GC/MS and main compounds were 1,2,3-benzenetriol, alpha-androsta-7,14-diene in LH-4 fraction. The activities of POD and SOD in samples havested on different habitats were high such as arable land> intermountain> seashore. That of POD and SOD in crude extracts of late stage were higher than early stage. Isozyme bands of crude extracts samplinged in all habitats and all growing stages showed two bands and the signal intensity showed strongly according to passage of growing stage. The purified extracts of LH-4 fraction showed excellent inhibition effect in proliferation of HL-60 cells and markedly suppressed colony formation in mouse fibroblast cells. Dose response between partially purified extracts(400ppm) and negative control did not produced statistically significant reduction in colony formation.

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.
    • Proceedings of the KSAR Conference
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    • 2002.06a
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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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    • v.11 no.3
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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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    • v.28 no.6
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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
    • Journal of Integrative Natural Science
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    • v.9 no.3
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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.

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

  • Zanabaatar, Bolormaa;Song, Jung-Hwa;Seo, Geon-Sik;Noh, Hyung-Jun;Yoo, Young-Bok;Lee, Jong-Soo
    • The Korean Journal of Mycology
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    • v.38 no.1
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    • pp.85-87
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    • 2010
  • Anti-gout xanthine oxidase inhibitory activity of water extracts from various mushrooms were determined. The highest xanthine oxidase inhibitory activity was 72.9% in the water extract from fruiting body of Agaricus brazillensis and also were high in the extract from fruiting bodies of Pleurotus salmoneostramineus(60.1%), Phellinus baumii(57.7%), Agaricus bisporus(56.7%) and Hericium erinaceum(53.4%). The xanthine oxidase inhibitor was maximally extracted when Agaricus brazillensis fruiting body was treated with water at $30^{\circ}C$ for 24 h.