应用化学2012，Vol.29Issue(5)：510-514,5.DOI:10.3724/SP.J.1095.2012.00281
氧化异阿朴菲-褪黑素杂合体的合成、抗β淀粉样蛋白聚集及抗氧化活性
Synthesis, Inhibition of β-Amyloid Aggregation and Antioxidation of Oxoisoaporphine-Melatonin Hybrids
摘要
Abstract
Two oxoisoaporphine-melatonin hybrids( compound 2a and 2b) have been designed, synthesized and tested for their ability to inhibit actylchoiinesterase, butyrylcholinesteiase, acetylekolinesierase-induced β-amyloid(Aβ) aggregation. Their inhibitory mechanism and antioxidant properties were also studied. The synthetic compounds(2a and 2b) exhibited moderate AChE inhibitory activity with IC50 values in the micromolar range in most cases. Non-competitive binding mode was found for these derivatives- Moreover , the compounds (2a and 2b) exhibit high acetylcholinesterase-induced Aβ antiaggregating activity with inhibitory patencies ranging from 79. 3% to 84.1% , and significant anlioxidant properties with peroxyl radical absorbance capacities ranging from 1. 1- to 1. 5-fold the value of trolox.关键词
氧化异阿朴菲衍生物/褪黑素/胆碱酯酶/抗氧化/抗Aβ聚集Key words
oxoisoaporphine derivatives, melatonin, cholinesterase, antioxidant, Aβ antiaggregating分类
化学化工引用本文复制引用
唐煌,钟书明,赵丽珍,赵海涛..氧化异阿朴菲-褪黑素杂合体的合成、抗β淀粉样蛋白聚集及抗氧化活性[J].应用化学,2012,29(5):510-514,5.基金项目
广西自然科学基金资助项目(083095) （083095）
广西研究生教育创新计划项目(2010106020703M68) （2010106020703M68）
