当前位置: X-MOL 学术J. Radiat. Res. Appl. Sci. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Physicochemical features and structural analysis of xanthine oxidase as a potential therapeutic target to prevent gout
Journal of Radiation Research and Applied Sciences ( IF 1.7 ) Pub Date : 2020-09-17 , DOI: 10.1080/16878507.2020.1812807
Muhammad Zohaib Nawaz 1 , Qurat-ul Ain 1 , Sara Zahid 1 , Tooba Zulfiqar 1 , Syed Awais Attique 1 , Muhammad Bilal 2 , Huda Ahmed Alghamdi 3 , Wei Yan 4 , Hafiz M. N. Iqbal 5
Affiliation  

The high uric acid level in blood can cause gouty arthritis. In the uric acid cycle, purines are converted to uric acid and the process is controlled through series of enzymes, of which, xanthine oxidase (XO) is a key enzyme responsible for the oxidation of xanthine to uric acid. XO has been used as a potential therapeutic target to control uric acid deposition, ultimately preventing gout. Various inhibitors of XO are being used as drugs to prevent uric acid deposition by inhibiting the overactivity of the enzyme. In this study, a molecular docking approach was used to evaluate the pharmacological properties and drug suitability of thirteen reported inhibitors of XO. All the inhibitors analyzed here were found suitable as oral drug candidates to cure gout by inhibiting the expression of XO with varying efficiencies except phytic acid. Fisetin, which is present in considerable amounts in different fruits and vegetables including strawberries, apple, cucumber, and onion, was scrutinized as the most efficient inhibitor of XO and suitable oral drug candidate amongst all reported inhibitors studied here. In conclusion, our study provides additional insights into the interaction properties and bioavailability of known putative inhibitors of XO as potential drug candidates to relieve gout.



中文翻译:

黄嘌呤氧化酶作为预防痛风的潜在治疗靶标的理化特征和结构分析

血液中高尿酸水平会引起痛风性关节炎。在尿酸循环中,嘌呤被转化为尿酸,并通过一系列酶控制该过程,其中黄嘌呤氧化酶(XO)是负责将黄嘌呤氧化为尿酸的关键酶。XO已被用作控制尿酸沉积,最终预防痛风的潜在治疗靶标。XO的各种抑制剂被用作药物,通过抑制酶的过度活性来防止尿酸沉积。在这项研究中,使用了一种分子对接方法来评估13种已报告的XO抑制剂的药理特性和药物适用性。发现这里分析的所有抑制剂都适合作为口服痛风药,通过除植酸以外的各种效率抑制XO的表达来治愈痛风。非瑟定 在研究的所有报道的抑制剂中,其被大量审查为最有效的XO抑制剂和合适的口服药物候选物,其大量存在于各种水果和蔬菜中,包括草莓,苹果,黄瓜和洋葱。总之,我们的研究为已知的XO抑制剂作为缓解痛风的潜在候选药物的相互作用特性和生物利用度提供了更多见解。

更新日期:2020-09-18
down
wechat
bug