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Xanthine oxidase inhibitory kinetics and mechanism of ellagic acid: In vitro, in silico and in vivo studies.
IET Nanobiotechnology ( IF 2.3 ) Pub Date : 2023-05-08 , DOI: 10.1049/nbt2.12135
Jianmin Chen 1, 2 , Zemin He 1 , Sijin Yu 1 , Xiaozhen Cai 1 , Danhong Zhu 1 , Yanhua Lin 1
Affiliation  

Ellagic acid (EA), which is widely distributed in many foods, has been found to possess inhibitory activity against xanthine oxidase (XO). However, there is ongoing debate about the difference in XO inhibitory activity between EA and allopurinol. Additionally, the inhibitory kinetics and mechanism of EA on XO are still unclear. Herein, the authors systematically studied the inhibitory effects of EA on XO. The authors' findings showed that EA is a reversible inhibitor with mixed-type inhibition, and its inhibitory activity is weaker than allopurinol. Fluorescence quenching experiments suggested that the generation of EA-XO complex was exothermic and spontaneous. In silico analysis further confirmed that EA entered the XO catalytic centre. Furthermore, the authors verified the anti-hyperuricemia effect of EA in vivo. This study elucidates the inhibition kinetics and mechanism of EA on XO, and lays a theoretical foundation for the further development of drugs and functional foods containing EA for the treatment of hyperuricemia.

中文翻译:

鞣花酸的黄嘌呤氧化酶抑制动力学和机制:体外、计算机和体内研究。

鞣花酸(EA)广泛存在于许多食品中,已被发现对黄嘌呤氧化酶(XO)具有抑制活性。然而,关于 EA 和别嘌呤醇之间 XO 抑制活性的差异一直存在争议。此外,EA 对 XO 的抑制动力学和机制仍不清楚。在此,作者系统地研究了EA对XO的抑制作用。作者的研究结果表明,EA是一种可逆的抑制剂,具有混合型抑制作用,其抑制活性弱于别嘌呤醇。荧光猝灭实验表明EA-XO复合物的生成是放热且自发的。计算机分析进一步证实 EA 进入了 XO 催化中心。此外,作者在体内验证了EA的抗高尿酸血症作用。
更新日期:2023-05-08
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