首页> 外文期刊>Journal of Ethnopharmacology: An Interdisciplinary Journal Devoted to Bioscientific Research on Indigenous Drugs >Tetrahydroamentoflavone (THA) from Semecarpus anacardium as a potent inhibitor of xanthine oxidase.
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Tetrahydroamentoflavone (THA) from Semecarpus anacardium as a potent inhibitor of xanthine oxidase.

机译:拟南芥(Semcarpus anacardium)的四氢黄酮(THA),是一种强力的黄嘌呤氧化酶抑制剂。

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ETHNOPHARMACOLOGICAL RELEVANCE: Seed of Semecarpus anacardium L. is widely used in Indian traditional medicine; Ayurveda and Sidha, for treatment of inflammatory disorders and gout. AIM OF THE STUDY: The present study was aimed at isolation of a compound for its potential to inhibit xanthine oxidase (XO), over expression of which lead to inflammation and gout. MATERIALS AND METHODS: Activity guided fractionation of S. anacardium seed was conducted using liquid-liquid partition and preparative HPLC. The fractions were evaluated for their XO inhibition and antioxidant activity. The ethyl acetate fraction with the highest XO activity yielded a biflavonoid compound tetrahydroamentoflavone (THA). Lineweaver-Burk (LB) plot for the XO inhibition of THA and allopurinol was constructed from the kinetic data. RESULTS: IC values of THA and allopurinol for XO inhibition were 92 and 100 nM respectively and their corresponding values for K(i) were 0.982 and 0.612 muM respectively. CONCLUSION: THA was a potent XO inhibitor which could be considered as a drug candidate or chemopreventive agent, after establishing its pharmacological and clinical evaluation. The study results appear to support the claim of the traditional medicine with respect to the efficacy of S. anacardium seed against inflammation and gout.
机译:人种药理关系:七叶树种子在印度传统医学中被广泛使用。阿育吠陀和西达,用于治疗炎症和痛风。研究目的:本研究旨在分离具有抑制黄嘌呤氧化酶(XO)潜力的化合物,该化合物的过度表达会导致炎症和痛风。材料与方法:采用液-液分配法和制备型HPLC进行活性指导下的拟南芥种子分级分离。评价级分的XO抑制和抗氧化活性。 XO活性最高的乙酸乙酯馏分产生双黄酮类化合物四氢精酮黄酮(THA)。从动力学数据构建了对THA和异嘌呤醇XO抑制作用的Lineweaver-Burk(LB)图。结果:THA和别嘌呤醇抑制XO的IC值分别为92和100 nM,其对应的K(i)值分别为0.982和0.612μM。结论:THA是一种有效的XO抑制剂,在建立其药理和临床评价后,可被视为候选药物或化学预防剂。该研究结果似乎支持了传统医学关于炭疽菌种子对炎症和痛风的功效的主张。

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