• 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.

• Natural Product Sciences
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• 제5권4호
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• pp.165-171
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• 1999

Since reactive oxygen species (ROS) play an important role in carcinogenesis and other several human diseases, antioxidants present in consumable fruits, vegetables, and beverages have received considerable attention as cancer chemopreventive agents. Thus, in order to identify antioxidants in plant extracts, potential activity was assessed by determining with inhibition of a xanthine/xanthine oxidase assay system. Approximately 170 plant extracts of Korean herbal medicines were primarily evaluated for the potential of antioxidant activity. As a result, 13 plant extracts were found to be active $(IC_{50}$<$100\;{\mu}g/ml)$. Especially, Juncus effusus, Selaginella tamariscina, Pueraria thunbergiana and Sedum albroseum showed strong inhibitory activity in this process. Further studies for the identification of active principles from these active lead plant extracts might be warranted.

• 대한의생명과학회지
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• 제27권4호
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• pp.277-282
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• 2021

Hydrocotyle is a genus of prostrate, perennial aquatic or semi-aquatic plants formerly classified in the family Apiaceae, now in the family Araliaceae. Lipoxygenases (LOX) are present in the human body and play an important role in the stimulation of inflammatory reactions. Ethanolic extracts of five Hydrocotyle species (H. ramiflora, H. maritima, H. nepalensis, H. sibthorpioides, and H. yabei) showed inhibition of 23.5~50.6% at 2.0 mg/mL. Their extracts showed LOX inhibition in half maximal effective concentration (EC₅₀) range 15.1~15.7 ㎍/mL. Hyaluronic acid is a glycosaminoglycan, a major component of the extracellular matrix Five extracts of these species inhibited less than 23.0% of Hyaluronidase (HAase) activity at a concentration of 2.0 mg/mL Xanthine oxidase (XO) is a form of xanthine oxidoreductase, a type of enzyme that generates reactive oxygen species. Five Hydrocotyle species were found to have inhibitory activity of XO at 2.0 mg/ml, with 65% having greater than 50% inhibition. H. ramiflora exhibited the highest activity with an inhibition of 80.0%. The results suggested that Lipoxygenases, Hyaluronidase, and Busan 47340, Republic of Korea from five Hydrocotyle species might be multifunctional and prevent the degradation of allergic reactions and inflammation.

• 생명과학회지
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• 제13권1호
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• pp.1-8
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• 2003

화살나무의 부위별 추출물로부터 항산화 활성 및 HL-60 세포를 이용한 생물학적 특성을 조사해 본 결과는 다음과 같았다. 화살나무 추출물의 부위별 DPPH free radical scavenging 활성은 잎, 날개, 뿌리, 종자, 줄기순으로, xanthine oxidase 억제 활성은 잎, 뿌리, 날개, 종자, 줄기 순으로 높았다 LH-20 column chromatography를 통한 정제 후의 DPPH 및 xanthine oxidase 억제활성은 잎과 줄기 추출물에서는 LH-4 분획이, 뿌리 추출물에서는 LH-5 분획이 가장 높은 활성을 나타내었다. 특히, 줄기 추출물에서 LH-4 분획물의 DPPH 및 xanthine oxidase 억제가는 각각 2.38 ${\mu}g$/$m\ell$, 5.32 ${\mu}g$/$m\ell$로 높은 활성을 나타내었다. 정제된 추출물들의 주된 화합물은 polyphenolic 화합물로 동정되었다. 생육시기간에 부위별 POD 활성은 5월의 뿌리 및 9월의 잎 조 추출물에서 가장 높았고, SOD 활성은 5월과 9월의 줄기에서만 나타났다. POD 동위효소 패턴은 잎과 줄기간에는 비슷하였으나, 뿌리에서는 다양하게 나타났다. SOD 동위효소 패턴은 POD와 비슷한 경향을 나타내었다. HL-60 세포의 증식에 대한 화살나무의 정제된 추출물은 대조구에 비해 높은 억제능을 나타내었다.

• 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.

• 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 $5.02(IC_{50}\;:\;{\mu}g/m{\ell})$와 $6.18(IC_{50}:{\mu}g/m{\ell})$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.

• Advances in Traditional Medicine
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• 제7권5호
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• pp.477-484
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• 2008

The present study was aimed at investigating the hypouricemic and xanthine oxidase inhibitory activities of the various fractions of the hydromethanolic extract of the leaves of Coccinia grandis L. Voigt (Cucurbitaceae). The leaves of this species was used in traditional medicinal system for the treatment of gout, rheumatism, jaundice, bronchitis, fever, skin eruptions, wounds, etc. The degree of xanthine oxidase inhibition was determined in vitro by measuring the increase in absorbance at 295 nm associated with uric acid formation. Among the fractions tested, the chloroform fraction exhibited highest potency ($IC_{50}$ $17.8\;{\mu}g/ml$). This was followed by the pet-ether ($IC_{50}$ $29.7\;{\mu}g/ml$), ethyl acetate ($IC_{50}$ $41.2\;{\mu}g/ml$) and residual ($IC_{50}$ $47\;{\mu}g/ml$) fractions. The $IC_{50}$ value of allopurinol was $6.1\;{\mu}g/ml$. In addition, the hypouricemic and hepatic xanthine oxidase (XO)/xanthine dehydrogenase (XDH) inhibitory activities of the fractions were examined in vivo using oxonate (280 mg/kg, i.p.) induced hyperuricemic mice. At a dose of 200 mg/kg orally for 7 days, the pet-ether, chloroform and ethyl acetate fractions produced a significant (P < 0.01) reduction in serum urate level and also inhibited hepatic XO/XDH activities when compared to hyperuricemic mice. These inhibitory effects were weaker than that observed for the standard drug, allopurinol (10 mg/kg, p.o.). Lineweaver-Burk analysis of the enzyme kinetics indicated that the mode of inhibition was of a mixed type. These results suggest that the use of Coccinia grandis leaves for the treatment of gout could be attributed to its XO inhibitory activity.

• 한국미생물·생명공학회지
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• 제40권3호
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• pp.208-214
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• 2012

본 연구는 왕겨를 이용한 항산화, 항노화에 효과적인 초액을 대량생산하여 기능성을 검증하고 왕겨초액 내의 기능성물질을 분석하여 사업화의 가능성을 타진하고자 하였다. 정제된 왕겨초액을 분획하여 기능성이 확인된 부분을 HPLC 기기를 이용하여 확인한 결과 caffeic acid 외에 7종의 polyphenol 유래물질에서 기능성을 확인하였다. 기능성 화장품소재 시험으로는 세포 생존율 측정(MTT assay), 주름개선 (collagenase inhibition assay, elastase inhibition assay), 미백(tyrosinase inhibition assay), 항산화 시험(DPPH free radical scavenging assay, SOD-like activity, xanthine oxidase inhibition assay)이 실시하였다. 피부주름형성은 콜라겐의 합성과 분해가 중요한 원인으로 작용한다고 알려져 있지만, 최근 많은 연구에서 엘라스틴의 재형성과 분해 또한 주름형성 기전에서 중요한 작용을 하는 것으로 보고되고 있다. 왕겨초액은 $100{\mu}L/mL$의 농도에서 collagenase 저해효과가 100%, elastase 저해효과가 55% 이상으로 주름개선 효과가 우수하였다. 왕겨초액은 $100{\mu}L/mL$의 농도에서 tyrosine에 대한 tyrosinase 저해효과가 80% 이상으로 미백효과가 우수하게 나타났다. DPPH radical 소거율, xanthine oxidase 저해와 SOD-like 활성을 이용하여 항산화 효과를 측정하였다. 왕겨초액 $100{\mu}L/mL$의 농도에서 DPPH radical 소거율이 80%, xanthine oxidase 저해효과가 80%, 그리고 SOD-like 활성이 100%를 나타내었다. 따라서 본 연구를 통하여 정제 왕겨초액을 이용한 산업화를 위한 가능성을 타진하여 효과가 좋음을 확인할 수 있었다. 이와 같은 결과로 왕겨초액을 이용한 기능성 화장품의 소재로 뿐만 아니라, 식품 및 의약외품의 품목허가를 통하여 고부가가치의 상품화소재로의 가능성이 있다고 사료됩니다.

• Preventive Nutrition and Food Science
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• 제16권1호
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• pp.8-11
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• 2011

In this study, we assessed the free radical scavenging and xanthine oxidase inhibitory activities of extracts isolated from the dried roots and stems (including leaves) of Angelica dahurica. The irritation response from these extracts was also assessed to determine potential cosmetic use. Both sources of A. dahurica extracts exhibited radical scavenging properties to different extents. The free radical scavenging potency ($EC_{50}$) of the stems (including leaves) of A. dahurica was 243.33 ${\mu}g/mL$, which is significantly lower (p<0.01) than that observed of the roots (1,161.79 ${\mu}g/mL$). The inhibition values ($EC_{50}$) of xanthine oxidase were as follows: 435.19 ${\mu}g/mL$ (roots) and 434.66 ${\mu}g/mL$ (stems). We noted no significant differences between the two plant parts with regard to ability to inhibit xanthine oxidase activity. After the application of A. dahurica extracts to rabbits for skin and eye irritation tests, no negative effects were observed; therefore, the extracts are considered to be non-irritating to the skin and eye.

• 한국버섯학회지
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• 제12권1호
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• pp.1-7
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• 2014

This study was initiated to investigate antioxidant, anti-acetylcholinesterase, and xanthine oxidase inhibitory activities and properties of fruiting bodies, mycelia, and fermentation culture filtrates from Phellinus igniarius. The contents of total phenols and flavonoid of fruit bodies, mycelia, and culture filtrate were 15.35-1.36 mg/g, 10.35-7.85 mg/g, and 8.25-5.36 mg/g. The 1,1-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging abilities of the extracts from the fruiting bodies, mycelia, and culture filtrates were 90.25-95.60%, 78.82-85.24%, and 76.32-82.50% at $50-400{\mu}g/mL$, respectively. The chelating ability of fruiting body extract on ferrous ions was higher than those of mycelia and culture filtrates tested. The anti-acetylcholinesterase inhibitory activity of the fruiting body extract at 400 ${mu}g/mg$ exhibited 91.10% on AChE, which is lower than that of positive control, galanthamine (94.82%). The xanthine oxidase inhibitory activities of the fruiting bodies, mycelia, and culture extract were 85.47%, 78.13%, and 72.49% at 400 ${\mu}g/mL$, respectively. Overall, the fruiting body extract has better anti-acetylcholinesterase, antioxidant and xanthine oxidase inhibitory activities than those from mycelia and culture filtrate.