• Journal of Integrative Natural Science
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• v.8 no.4
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• pp.258-266
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• 2015

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, lung, kidney, heart, brain and plasma. It is involved in gout pathogenesis. In this study, we have performed Comparative Molecular Field Analysis (CoMFA) 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 CoMFA 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 CoMFA models were generated using different alignments and the best model yielded a cross-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 CoMFA models was found to be $r^2_{pred}$0.653. The CoMFA study revealed that the $R_3$ position of the structure is important in influencing the biological activity of the inhibitors. Electro positive groups and bulkier substituents in this position enhance the biological activity.

• Food Science and Preservation
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• v.13 no.5
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• pp.616-622
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• 2006

This study was intended to analyze the contents of polyphenol compounds and vitamin C, and the inhibitory activities of xanthine oxidase and tyrosinase to measure physiological efface of various extract of Lespedeza bicolor. The vitamin C content was $26.42{\pm}0.08mg/100g$. The content of phenolic compounds included in the flesh L bicolor was $1.14{\pm}0.02mg/g$. The ethanol extract by reflux method and water extracts by the microwave-assisted method showed the highest content as 154.95 mg/g and 145.17 mg/g, respectively. The xanthine oxidase inhibitory tate of water extracts was the highest value of 87.85% at the concentration of 1,000 ug/mL. All kinds of extracts showed the highest inhibitory activity for the xanthine oxidase at the concentration of 1,000 ug/mL and a decreasing pattern of the inhibitory race over the concentration of 1,000 ug/mL. The tyrosinase inhibitory rate was increased with an increment of the extract concentrations, and the activity of ethanol extracts was the highest as 55.22% at the concentration of 3,000 ug/mL.

• 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.

• YAKHAK HOEJI
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• v.43 no.6
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• pp.756-761
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• 1999

Lipid peroxidation mediated by hydroxyl radicals which are generated during myocardial ischermia has suggested as a possible mechanism of ischemic myocardial damage. Recently, it has been reported that anti-arrhythmic action of lidocaine, a local anesthetic, is attributed to its "membrane-stabilizing" properties through scavenging free radicals, thus, inhibiting lipid peroxidation. Aldehyde oxidase and xanthine oxidase which catalyze the oxidation of many purine, pyrimidine and pteridine derivatives are known as free radical generating systems. In this experiment, we studied the effect of lidocaine and procainamide on the hepatic aldehyde and xanthine oxidase activity and antioxidative activities. It was found that lidocaine and procainamide inhibited both NADPH-dependent and independent lipid peroxidation. Both of tested compounds were found to be ineffective in inhibiting xanthine oxidase. Lidocaine and procainamide, however, inhibited aldehyde oxidase activity in vitro as well as in vivo. Based on the above results, lidocaine and procainamide could be employed as a therapeutic agent for aldehyde oxidaserelated disease.d disease.

• The Journal of Dong Guk Oriental Medicine
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• v.6 no.1
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• pp.91-106
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• 1997

The purpose of this study is to observe tile protective effect of Leeganpunsusan on serum reaction and hepatic tissue in galactosamine treated rats. In this study, the experimental rats divided three group(Normal, Control and sample group). Under the same condition, normal and control groups were administered water, sample group was administered Leeganpunsusan for 15 days. The last day, both normal and control goups were injected to abdomen with galactosamine. The rates of lipid peroxide, SOD(activity) and xanthine oxidase(activity) were measured. The results were obtained as follows : Effects of the extract of Leeganpnnsusan on the hepatic lipid peroxidation, xanthine oxidase activity in VITRO, as compared with control group were significantly decreased with the level of concentration of extract prepared from Leeganpunsusan. In VIVO, the hepatic content of lipid peroxide, the rate of type changing(type D to O) and xanthine oxidase activity were significantly decreased in galactosamine-treated rats. Effect of on the hepatic cytosolic superoxide dismutase activity was significantly increased.

• Applied Biological Chemistry
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• v.49 no.2
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• pp.114-124
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• 2006

The objective of this research was to evaluate the ability of water and 80% ethanol extracts from one hundred eight mulberry leaves (Morus alba L.) to influence the inhibitory activity of angiotensin converting enzyme (ACE) and xanthine oxidase (XOase). The total phenol contents were that water extracts of ten species (Kakjayongsan (Morus alba L.), Daejungsun (Morus alba L.) etc.) and 80% ethanol extracts of twenty three species (Waryoung (Morus alba L.), Hasusang (Morus alba L.) etc.) showed more than 15 mg/g. The inhibitory activity on angiotensin converting enzyme (ACE) were that ten species (YamanakkadakKaskke (Morus alba L.), Mijiro (Morus alba L.) etc.) showed 100% inhibition rate both of water extracts and 80% ethanol extracts. The rest, water extracts of thirty four species (Cheongilppong (Morus alba L.) etc.) and 80% ethanol extracts of thirty four species (Wonjukojo (Morus alba L.) etc.) showed inhibitory activity (above 90%) on ACE. Also, to search of xanthine oxidase (XOase) inhibition were that water extracts of five species (Cheongsipjosaeng (Morus alba L.), Suwon 3 (Morus alba L.) etc.) and 80% ethanol extracts of Jeokmok (Morus alba L.) showed inhibitory activity (above 50%) on XOase. This result revealed, strong biological activity in spite of has a little total phenol contents. These water and 80% ethanol extracts from mulberry leaves (Morus alba L.) are expected good candidate for development into anti-hypertentive and anti-gout sources.

• 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.

• Biomedical Science Letters
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• v.12 no.4
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• pp.439-442
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• 2006

To evaluate the postmortem changes in activities of oxygen free radical metabolizing enzymes, the rats were sacrificed with cervical dislocation and were kept in an incubator at $25^{\circ}C$, 70% of humidity for 12 hours. The activities of aniline hydroxylase, catalase, glutathione-S-transferase and superoxlde dismutase were decreased with the time. On the other hand, the activity and type conversion ratio (type D ${\to}$type O) of hepatic xanthine oxidase (XO) were gradually increased. From these changes of XO, the estimation of death time (mathematical equation) could be determined with the least square method. To clarify the cause of increasing XO activity, enzyme kinetics were examined. The Km values of XO were decreased with the time. In conclusion, the determination of liver XO activity might be used for the estimation of death time in the early postmortem period.

• The Korea Journal of Herbology
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• v.22 no.4
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• pp.101-108
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• 2007

Objectives : To compare the anti-oxidant effects of Ligusticum chuanxiang and Cnidium officinale extracts and their mixture with Angelica gigas, we investigated the anti-oxidative activities using rat liver tissues. Methods : We investigated the anti-oxidative activities by analysis of lipid peroxidation, xanthine oxidase activity, aldehyde oxidase activity, hydroxyl radical scavenging activity, superoxide dismutase activity and catalase activity in rat liver tissues. Results : Both Ligusticum chuanxing and Cnidium offieinale inhibited the lipid peroxidation compared to the control, there is no significant differences between two groups. Cnidium officinale showed strong inhibitory effects on xanthine oxidase and aldehyde oxidase activities compared with that of Ligusticum chuanxing. Ligusticum chuanxing and Cnidium officinale were scavenged the hydroxy radicals, and increased SOD and catalase activities. These results suggested that Ligusticum chuanxing and Cnidium officinale were showed antioxidant activity, especially Cnidium officinale showed higher activity than Ligusticum chuanxing. Conclusions: These results suggest that Ligusticum chuanxing could be replaced by Cmdium afficinale in clinical trial.

• Journal of Environmental Health Sciences
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• v.16 no.1
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• pp.67-74
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• 1990

An effect of carbon tetrachloride (CCl$_{4}$) was studied on the xanthine oxidase(XOD)activity of small intestine in male rats. Concomitantly a cause of increasing small intestine XOD was focused on an effect of actinomycin D and the kinetics of partial purified XOD frdm small intestine in CCl$_{4}$ intoxicated rats. An injection of CCl$_{4}$ to the rats showed an increase of small intestine XOD. In the pretreatment of actinomycin D before injection of CCl$_{4}$ to the rats, the XOD activities of small intestine were significantly decreased. In the partial purified enzyme preparation, the small intestine XOD in CCl$_{4}$ intoxicated rats showed the more increased Km and Vmax value with xanthine as substrate than that of control group.