Inhibitory effect of flavonoids on human glutaminyl cyclase
Inhibitory effect of flavonoids on human glutaminyl cyclase
复制标题
黄酮类化合物对人谷氨酰胺环化酶的抑制作用
DOI：
10.1016/j.bmc.2016.03.064
复制
发表时间：
2016-05-15
影响因子：
3.5
通讯作者：
Wu, Haiqiang
中科院分区：
文献类型：
--
作者：
Li, Manman;Dong, Yao;Wu, Haiqiang
谷氨酰环化酶（QC）在阿尔茨海默病（AD）的发病机制中起重要作用，是开发新型抗AD药物的潜在靶点。本论文合成了一类新的人源性QC（hQC）抑制剂--苯酚-4 '（R1-）、C5-OH（R2-）和C7-OH（R3-）修饰的芹菜素衍生物。通过分光光度法评估对这些化合物的功效进行了研究，并评价了构效关系（SAR）。并通过分子对接分析了合成的黄酮类化合物与hQC活性位点的结合方式。(C)2016爱思唯尔有限公司版权所有。
Glutaminyl cyclase (QC) plays an important role in the pathogenesis of Alzheimer's disease (AD) and can be a potential target for the development of novel anti-AD agents. However, the study of QC inhibitors are still less. Here, phenol-4' (R1-), C5-OH (R2-) and C7-OH (R3-) modified apigenin derivatives were synthesized as a new class of human QC (hQC) inhibitors. The efficacy investigation of these compounds was performed by spectrophotometric assessment and the structure-activity relationship (SAR) was evaluated. Molecular docking was also carried out to analyze the binding mode of the synthesized flavonoid to the active site of hQC. (C) 2016 Elsevier Ltd. All rights reserved.