Syntheses and evaluation of novel isoliquiritigenin derivatives as potential dual inhibitors for amyloid-beta aggregation and 5-lipoxygenase
Syntheses and evaluation of novel isoliquiritigenin derivatives as potential dual inhibitors for amyloid-beta aggregation and 5-lipoxygenase
复制标题
新型异甘草素衍生物作为淀粉样蛋白聚集和 5-脂氧合酶潜在双重抑制剂的合成和评价
DOI：
10.1016/j.ejmech.2013.05.015
复制
发表时间：
2013-08-01
影响因子：
6.7
通讯作者：
Huang, Zhi-Shu
中科院分区：
文献类型：
--
作者：
Chen, Yi-Ping;Zhang, Zi-Ying;Huang, Zhi-Shu
合成了一系列新的异甘草素（isoliquiritigenin，ISL）衍生物，并对其作为淀粉样蛋白β（A β）聚集和5-脂氧合酶（5-LO）双重抑制剂进行了评价。发现所有这些合成化合物均有效抑制A β（1-42）聚集，其IC 50值范围为2.2 +/- 1.5 μ M至23.8 +/- 2.0 μ M。这些衍生物也显示出对5-LO的抑制活性，其IC 50值范围为6.1 +/- 0.1 μ M至35.9 +/- 0.3 μ M。研究了它们的构效关系（SAR）和抑制机理。本研究为进一步开发ISL衍生物作为治疗阿尔茨海默病（AD）的多功能药物提供了潜在的重要信息。(C)2013年Elsevier Masson SAS。All rights reserved.
A series of new isoliquiritigenin (ISL) derivatives were synthesized and evaluated as dual inhibitors for amyloid-beta (A beta) aggregation and 5-lipoxygenase (5-LO). It was found that all these synthetic compounds inhibited A beta (1-42) aggregation effectively with their IC50 values ranged from 2.2 +/- 1.5 mu M to 23.8 +/- 2.0 mu M. These derivatives also showed inhibitory activity to 5-LO with their IC50 values ranged from 6.1 +/- 0.1 mu M to 35.9 +/- 0.3 mu M. Their structure activity relationships (SAR) and mechanisms of inhibitions were studied. This study provided potentially important information for further development of ISL derivatives as multifunctional agents for Alzheimer's disease (AD) treatment. (C) 2013 Elsevier Masson SAS. All rights reserved.