• Archives of Pharmacal Research
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• 제10권1호
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• pp.36-41
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• 1987

The conversion of xanthine dehydrogenase (type D) into xanthine oxidase (type D) was significantly increased in serum and liver of all $CCI_4$ treated rats on the necrosis and early cirrhosis stage of liver tissue. In the pretreatment of prednisolone, the ratio of type O per type O + D showed the decreasing tendency in serum, but the significant decrease in liver. In vitro, the conversion of liver xanthine oxidase from type D into type O was markedly increased by following preincubation with lysosomal fraction. The type conversion of xanthine oxidase may be caused by protelytic enzymes in lysosome.

• 한국식품영양학회지
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• 제11권3호
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• pp.354-358
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• 1998

우리 나라에서 쉽게 구할 수 있고, 값이 저렴하여 대중적으로 널리 이용될 수 있는 감잎으로부터의 열탕 추출물과 함께 탄닌을 분리하여 xanthine oxidase 활성을 측정함으로써 감잎의 통풍 예방효과를 살펴보았다. 감잎의 열탕 추출물을 농도별로 살펴본 결과 열탕 추출물의 농도가 증가할수록 저해효과가 증가하여 2.0mg 첨가시 82.4%의 높은 저해효과를 나타냈으며, 감잎탄닌도 감잎의 열탕 추출물과 마찬가지로 농도에 비례해서 santhine oxidase 저해효과가 증가하는 것으로 나타났다. 한편 감잎 열탕 추출물 및 감잎 탄닌은 xanthine oxidase에 대해 경쟁적 저해를 하는 것으로 나타났다.

• 약학회지
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• 제39권5호
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• pp.521-527
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• 1995

This study was done to determine the effect of lead acetate on the activities of the hepatic cytosofic xanthine oxidase and aldehyde oxidase which were well known as oxygen free radical generating enzyme in vitro. Lead ion accelerated the formation of lipid peroxide and the increment of xanthine oxidase(type O) activity and the type conversion ratio from xanthine dehydrogenase to xanthine oxidase dose-dependently. But xanthine dehydrogenase(type D) activity was decreased. Aldehyde oxidase activity was not changed by lead ion. These data suggested that lead-induced cellular to)dcity may be concerned partially with xanthine oxidase mediated lipid peroxidation.

• 한국식품과학회지
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• 제24권6호
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• pp.558-562
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• 1992

Xanthine oxidase는 퓨린 대사에 관여하여 xanthine 혹은 hypoxanthine을 산화하여 요산을 생성하게 하는 효소이다. 이상 퓨린 대사로 인해 형성된 요산은 관절에 축적되어 통풍을 동반하는 통증을 유발한다. 본 연구는 천연물로부터 통풍치료제의 개발을 목적으로 우롱차로 부터 6종의 flavan-3-ol 화합물을 분리하였고 기기분석에 의해 화학구조를 밝혔다. 각 화합물은 (-)-epicatechin, (-)-epicatechin-3-O-gallate, procyanidan B-1, B-3, procyanidin B-3-3'-O-rhamnose procyanidin B-1-3-O-gallate 였다. Xanthine oxidase 저해 영향을 관찰한 결과 gallte가 결함된 flavan-3-ol 화합물이 저해활성이 강하였고 procyanidin B-1-3-O-gallate는 $50\;{\mu}M$에 완전한 저해효과를 나타내었고 xanthine oxidase에 경쟁적으로 저해한다는 것이 밝혀졌다.

• 한국식품영양과학회지
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• 제20권6호
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• pp.527-537
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• 1991

To evaluate an effect of liver xanthine oxidase on the induction of liver damage, carbon tetrachloride (CCl4) was intraperitoneally injected twice at 0.1ml/100g body weight to the rate fed a low (LP)or high protein diet(HP) while the control group fed LP or HP received only olive oil. The changing rate of liver xanthine oxidas activity was compared with that of a free radical generating enzyme, liver aniline hydroxylase and a scavenging enzyme, glutathions S-transferase activity between the rate fed a LP and those fed HP, and the two groups treated with CCl4. Concomitantly, the degree of liver damage which could be considered as the paramete for CCl4 metabolism in case of CCl4-intoxicated animal was observed in the present experimental conditions and the effect of allopurinol, xanthine oxidase inhibitor, on the CCl4-toxicity of rate liver was alos demostrated. On the other hand, the comparative effect of actinomycin D on the liver and serum xanthine oxidase of CCl4-treated rats fed HP with that of those fed LP and the kinetics of purifed liver enzyme from the liver of CCl4-treated rats fed HP was also compared with that of those fed LP to clarify the differences of xanthine oxidase activity between two groups. The increasing rate of liver weigth/body wt, serum levels of ALT and the decreasing rate of hepatic ALT activity and protein contents to each control group were higher in CCl4-treated rats fed HP than those fed LP. Under the animal models as indentified by the present data herein, the liver xanthine oxidase activity was higher in CCl4-treated rats fed HP than those fed LP, and the control group fed HP also showed the much higher activity xanthine oxidase than that fed LP, whereas there were no differences in the activity of hepatic aniline hydroxylase and glutathions S-transferase between the two group treated with CCl4. Although the hepatic aniline hydroxylase activity was somewhat higher in the rats fed HP than those fed LP, the increasing rate of liver xanthine oxidase to the rats fed LP was higher in those fed HP than that of liver aniline hydroxylase. The degree of liver damage identified such as liver weight and serum ALT activity was less in the CCl4-treated rats pretreated with allopurinol. These results suggest that even a system at which xanthine oxidase acts as well as the drug metabolizing enzyme may influence the acelatin of CCl4 metabolism. In addition, the purified liver xanthine oxidase from CCl4-treated rats fed HP showed decreased Km value when compared to its control group. The Km value of liver xanthine oxidase of CCl4-treated rats fed LP showed a similar Km value with its control group. Furthermore, the decreasing rate of liver and serum xanthine oxidase acitivity in CCl4-treated rats pretreated with actinomycin D to the CCl4-treated rats was higher in rats fed HP than in those fed LP. These results suggest that the inductino of xanthine oxidase in CCl4-treated rats fed HP may be greater than in those fed LP.

• 한국미생물·생명공학회지
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• 제28권2호
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• pp.92-96
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• 2000

통풍과 oxygen free radical의 독성에 관여하는 xanthine oxidase에 대한 새로운 저해물질의 탐색 및 개발을 목적으로 본 연구에서 선택분리한 Aspergillus sp. F184가 생산하는 저해물질을 분리.정제하고 구조를 결정하였으며 효소저해활성을 조사하였다. 본 균주를 배양 후 배양액을 여과하여 균체와 배양액을 분리하고 균체를 acetone으로 추출하고 감압농축하고 남은 수용액층을 배양액과 합쳐 HP-20 adsorption column chromatography, ethyl acetate 추출, silica gel column chromatography, 결정화 등을 실시하여 xanthine oxidase에 대한 저해물질을 분리, 정제하였다. 본 저해물질의 구조를 NMR 및 MS 스펙트럼을 측정하여 분석한 결과 5,6-epoxy-2-hydroxy-3-methyl-2-cyclohexene-1,4-dione으로서 terreic acid로 동정되었다. Terreic acid의 xanthine oxidase에 대한 저해활성을 조사한 결과 IC50가 1.1$\times$10-7M로서 기존의 저해제인 allopurinol과 유사하였다. 이에 terreic acid에 의한 xanthine oxidase 저해활성은 보고된 바가 없기에 새로운 통풍치료제로서의 가능성이 있음을 보고한다.

• 약학회지
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• 제38권2호
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• pp.211-217
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• 1994

Copper intoxication and disturbance of copper metabolism induced various oxygen-derived free radicals related damages. The effect of copper ion on xanthine oxidase activity and type conversion of the enzyme which is concerned to generation of reactive oxygen species, was investigated, It was observed that xanthine oxidase activity was increased by addition of copper ion in the reaction mixture in proportional to the concentration of the metal ion until $60\;{\mu}M$, while the enzyme activity was inhibited in higher concentration of copper treatment. On the other hand, xanthine dehydrogenase activity was inhibited by copper ion addition with concentration dependently. Preincubation of enzyme source with $30\;{\mu}M$ of copper ion, which concentration marked increased the xanthine oxidase activity, unchanged the enzyme activity and type conversion compare to control in vitro system. It was also observed that copper induced xanthine oxidase activity and the enzyme type conversion was protected by dithiothreitol and penicillamine. These results indicate that the increment of the type conversion of xanthine oxidase necessarilly need the presence of copper ion in enzyme assay system.

• 동아시아식생활학회지
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• 제5권3호
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• pp.215-221
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• 1995

This study was undertaken to investigate the effect of Taraxacum herba extract on the hepatic xanthine oxidase activity as a oxygen free radical generating enzyme in vitro and in vivo. It was observed that partial purified hepatic xanthine oxidase (type O) activity was strongly inhibited by the addition of Taraxacum herba n-butanol extract in vitro. The Km value of xanthine oxidase without affecting the Vmax value for xanthine was significantly increased by the addition of ta-dase (type O) activity was significantly inhibited by the treatment of Taraxacum gerba n-butanol ex-tract for 5days(over 40mg/kg, i.p), whereas, xanthine oxidase (type D) activity was not changed by the injection of Taracacum herba n-butanol extract. Meanwhile, liver weight / body weight(%), serum alanine aminotransferase activity and hepatic lipid peroxide content in Taraxacum herba n-buta-nol extract-treated rat were not changed. These findings led us to conclude that Taraxacum herba n-butanol extract may regulate the hepatic xanthine oxidase type O activity to prevent toxic effect of oxidative stress by the oxygen free radicals.

• 한국미생물·생명공학회지
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• 제19권6호
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• pp.610-613
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• 1991

Pseudomonas synxantha A3으로부터 정제된 결정화 효소를 사용하여 몇가지의 성질을 검토하였다. 본 효소에 대한 nucleoside 관련물질의 저해관계를 검토한 결과, 그 중에서 adenine, 8-azaadenine, 2-methyladenine, guanine, 8-azaguanine에 의해서 강한 저해를 받는 것으로 나타났으며, caffenine에 의해서는 저해를 받지 않았다. Adenine과 guanine은 비길항저해제로서, 그 저해상수($K_i$)는 각각 0.037mM과 0.098mM 이었다.

• 통합자연과학논문집
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• 제10권4호
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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.