机构地区: 广西师范大学化学化工学院省部共建药用资源化学与药物分子工程教育部重点实验室
出 处: 《应用化学》 2012年第5期510-514,共5页
摘 要: 基于多靶向策略设计合成了氧化异阿朴菲-褪黑素杂合化合物,测试了它们的抗胆碱酯酶性能及相应的抑制动力学、抗氧化能力和抑制乙酰胆碱酯酶诱导的β-淀粉样蛋白(Aβ)聚集能力。实验结果表明,所合成的化合物对乙酰胆碱酯酶具有中等强度抑制力,其抑制IC50值在微摩尔浓度水平,属于非竞争性抑制剂;对乙酰胆碱酯酶诱导的Aβ淀粉样蛋白聚集的抑制率达到79.3%~84.7%;抗氧化能力是trolox的1.1~1.5倍。 Two oxoisoaporphine-melatonin hybrids(compound 2a and 2b) have been designed,synthesized and tested for their ability to inhibit acetylcholinesterase,butyrylcholinesterase,acetylcholinesterase-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 potencies ranging from 79.3% to 84.7%,and significant antioxidant properties with peroxyl radical absorbance capacities ranging from 1.1-to 1.5-fold the value of trolox.