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从根中提取的香叶木素对黄嘌呤氧化酶的抑制作用及抗 LDL 氧化作用

Xanthine Oxidase Inhibition and Anti-LDL Oxidation by Prenylated Isoflavones from Root.

机构信息

Division of Applied Life Science (BK21 Plus), IALS, Gyeongsang National University, Jinju 52828, Korea.

College of Food and Biological Engineering, Qiqihar University, Qiqihar 161006, China.

出版信息

Molecules. 2020 Jul 6;25(13):3074. doi: 10.3390/molecules25133074.

Abstract

Xanthine oxidase is a frontier enzyme to produce oxidants, which leads to inflammation in the blood. Prenylated isoflavones from were found to display potent inhibition against xanthine oxidase (XO). All isolates (-) inhibited XO enzyme with IC ranging 7.836.4 μM. The most active isoflavones (-, IC = 7.814.8 μM) have the structural feature of a catechol motif in B-ring. Inhibitory behaviors were disclosed as a mixed type I mode of inhibition with < . Binding affinities to XO enzyme were evaluated. Fluorescence quenching effects agreed with inhibitory potencies (ICs). The compounds (-) also showed potent anti-LDL oxidation effects in the thiobarbituric acid-reactive substances (TBARS) assay, the lag time of conjugated diene formation, relative electrophoretic mobility (REM), and fragmentation of apoB-100 on copper-mediated LDL oxidation. The compound protected LDL oxidation with 0.7 μM in TBARS assay, which was 40-fold more active than genistein (IC = 30.4 μM).

摘要

黄嘌呤氧化酶是一种产生氧化剂的前沿酶,会导致血液中的炎症。从 中发现的prenylated 异黄酮对黄嘌呤氧化酶(XO)显示出强大的抑制作用。所有分离物(-)均以 IC 范围为 7.8-36.4 μM 的方式抑制 XO 酶。最活跃的异黄酮(-,IC = 7.8-14.8 μM)具有 B 环中环丙基二酮基的结构特征。抑制行为被揭示为一种混合的 I 型抑制模式, < 。评估了与 XO 酶的结合亲和力。荧光猝灭效应与抑制效力(IC)一致。化合物(-)在硫代巴比妥酸反应物质(TBARS)测定中也显示出强大的抗 LDL 氧化作用,共轭二烯形成的滞后时间,相对电泳迁移率(REM)和铜介导的 LDL 氧化中 apoB-100 的片段化。在 TBARS 测定中,化合物 以 0.7 μM 保护 LDL 氧化,其活性是染料木素(IC = 30.4 μM)的 40 倍。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/37eb/7411605/8eb562b454ee/molecules-25-03074-g001.jpg

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