• Journal of Integrative Natural Science
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• v.10 no.4
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• pp.202-208
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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, Hologram based Quantitative Structure Activity Relationship Study was performed on a series of Xanthine Oxidase antagonist named 2-(indol-5-yl) thiazole derivatives. The best HQSAR model was obtained using Atoms, Bonds, Connection, Hydrogen, Chirality and Donor Acceptor as fragment distinction parameter using hologram length 71 and 4 components with fragment size of minimum 2 and maximum 5. Significant cross-validated correlation coefficient ($q^2$= 0.563) and non cross-validated correlation coefficients ($r^2$= 0.967) were obtained. The model was then used to evaluate the six external test compounds and its $r^2{_{pred}}$ was found to be 0.798. Contribution map show that presence of propyl ring in indole thiazole makes big contributions for improving the biological activities of the compounds. We hope that our HQSAR model and analysis will be helpful for future design of xanthine oxidase antagonists.

• 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.

• 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$\mu\textrm{g}$.

• 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.

• The Korean Journal of Food And Nutrition
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• v.17 no.4
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• pp.347-355
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• 2004

This study was undertaken in order to evaluate effects of methanol extracts of Stachys sieboldii MIQ and its related enzyme activities in brain tissues of rats. Sprague-Dawley(SD) male rats were fed within a control group, which is a basic diet group. The experimental diet group was given 100 and 200 mg/kg to supervise 100 and 200 mg/kg body weight per day for 20 days. Lipid peroxide levels and acetylcholine esterase activity in brain tissues were slightly decreased at a dose dependent manner, in vitro. Lipid peroxide levels were also decreased at a dose dependent manner; methanolic extracts of Stachys sieboldii MIQ demonstrated significant inhibitory effects, in vivo. Monoamine oxidase and xanthine oxidase activities were significantly inhibited in the brain tissues of experimental group compared to control group and the ratio of type conversion of xanthine oxidase were decreased.

• Proceedings of the Ginseng society Conference
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• 1980.09a
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• pp.131-135
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• 1980

The influence of Panax ginseng on alcohol-induced hyperuricemia were observed. Changes of uric acid blood levels and hepatic xanthine oxidase activities were studied by means of treating alcohol intoxication with ginseng. It was found that a single dose (4 mg/Kg) of ginseng saponin administered intraperitoneally significantly inhibits the hepatic xanthine oxidase activities and decrease urate blood levels in ethanol-induced hyperuricemic mice. It was also observed that there were some difference in pharmacological aspect between Panax ginseng and allopurinol which is a potent inhibitor of xanthine oxidase from any sources.

• The Korean Journal of Mycology
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• v.43 no.2
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• pp.99-103
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• 2015

We prepared supernatants and cell-free extracts of yeasts isolated from wild flowers in Korea, and their antioxidant activity and inhibitory activities of xanthine oxidase and tyrosinase were investigated. Among them, cell-free extracts of Kuraishia capsulata UL40-2 and Sporobolomyces ruberrimus 121-Z-3 showed significantly high xanthine oxidase inhibitory activity of 46.4% and 48.3%, respectively. Starmerella bombicola 80-J-1 also showed tyrosinase inhibitory activity of 36.2% in the cell-free extract. Other antioxidant activities and tyrosinase inhibitory activities were not detected or were below 20%. Maximal production of the xanthine oxidase inhibitors were observed when Kuraishia capsulate UL40-2 and Sporobolomyces ruberrimus 121-Z-3 were cultured in the yeast extract-peptone-dextrose media at $30^{\circ}C$ for 24 hour, respectively.

• Food Science and Preservation
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• v.9 no.4
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• pp.369-374
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• 2002

This study was performed to investigate the effects of tyrosinase inhibition, xanthine oxidase inhibition and nitrite-scavenging effects of gamma-irradiated Schizandrae Fructus extracts from different solvents. Schizandrae Fructus was extracted by hot water, ethanol, acetone and methanol, and the extracts were irradiated 10, 20 and 30 kGy with gamma rays. All extracts from Schizandrae Fructus showed inhibition effect against tyrosinase. Tyrosinase inhibition effect of Schizandrae Fructus were higher in solvent extracts than hot water extracts by irradiation. The Schizandrae Fructus extracts had a higher inhibitory effect against xanthine oxidase, and the effect was not changed by irradiation. Nitrite scavenging activity, which was measured at various pH conditions (1.2, 3.0, 6.0), was the highest in Schizandrae Fructus extracts at pH 1.2 and 3.0. Hot water extracts provided higher nitrite scavenging effect than those of the methanol, ethanol and acetone extracts. Gamma-Irradiation may not influence on biological activites of the extracts when irradiated up to 30 kGy.

• Journal of the Korean Society of Food Science and Nutrition
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• v.24 no.1
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• pp.154-159
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• 1995

Inhibition of xanthine oxidase by tea extracts obtained from non-fermented tea(steamed green tea and roasted green tea), semi-fermented tea(oolong tea) and fermented tea(black tea) were investigated. The crude catechin fraciton had a hgher inhibitory effect against xanthine oxidase, and the effect was increased with the addition of tea extracts. Their inhibitory effect were hardly influenced until extracted three times with hot water. According to the investigation of catechins in the crude catechin fraction obtained from tea extracts, (-)-epicatechin-(EC), (-)-epicatechin gallate(ECg). (-)-epigallocatechin(EGC) and (-)-epigallocatechin gallate(EGCg) were 80.1$\mu\textrm{g}$/mg 113.5$\mu\textrm{g}$ /mg, 186.3$\mu\textrm{g}$/mg and 367.7$\mu\textrm{g}$/mg in steamed green tea, and 75.6$\mu\textrm{g}$/mg, 114.7$\mu\textrm{g}$/mg, 193.7 $\mu\textrm{g}$/mg and 381.9$\mu\textrm{g}$/mg in roasted green tea, and 69.4$\mu\textrm{g}$/mg, 110.0$\mu\textrm{g}$/mg, 127.1$\mu\textrm{g}$.mg and 464.9$\mu\textrm{g}$/mg in oolong tea, and 78.1$\mu\textrm{g}$/mg, 171.8$\mu\textrm{g}$/mg, 80.7$\mu\textrm{g}$/mg and 51.4$\mu\textrm{g}$/mg in black tea, respectively. Order of the content of these catechins was (-)-EGCg>(-)-EGC>(-)-ECg>(-)-EC in steamed green tea, roasted green tea and oolong tea, and was (-)-ECg>(-)-EGC>(-)-EC>(-)-EGCg in black tea. Also the concentration of catechins was hardly influeced until extracted three times. The inhibition ratio of xanthine oxidase by autherntic catechins was hardly influenced until extracted three times. The inhibition ratio of xanthine oxidase by authentic catechins was 94.9% and 87.6% by addition of 5.0$\mu\textrm{g}$/ml of (-)-EGCg and (-)-ECg, respectively. the inhibitors of xanthine oxidase were supposed to be due to (-)-ECg and (-)-EGCg in tea polyphenol compounds.

• YAKHAK HOEJI
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• v.23 no.3_4
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• pp.173-179
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• 1979

A dose, 1g/kg of ethanol produced experimental hyperuricemia in mouse. Ginseng saponins were tested for their ability to alter the hepatic xanthine oxidase activity and the blood level of uric acid in the ethanol-treated mouse. Intraperitoneal injection of ginseng saponin 4mg/kg markedly decreased the xanthine oxidase activity in the ethanol-treated mouse liver. It was also observed that ginseng saponin reduced the blood concentration of uric acid in experimentally induced hyperuricemia by alcohol treatment. In vitro, it was found that a low concentration of ginseng saponin in the reaction mixture incresed the hepatic xanthine oxidase activity, while a high concentration inhibited both enzyme preparations of normal and ethanol treated mice. In contrast with the xanthine oxidase, uricase activity was not influenced by ginseng saponin as well as in vivo. These results suggest there is a possibility that ginseng saponin may have some therapeutic effect on gout and other hyperuricemia syndrome.