柚皮苷双席夫碱的合成及生物活性研究  

Studies on synthesis and bio-activity of naringin bis-Schiff base

作　　者：郭莉霞 孙斌 GUO Li-xia;SUN Bin(key Laboratory of Natural Medicine Research of Chongqing Education Commission,Chongqing 400067,China;College of Environment and Resources,Chongqing Technology and Business University,Chongqing 400067,China)

机构地区：[1]重庆高校天然药物研究重点实验室,重庆400067 [2]重庆工商大学环境与资源学院,重庆400067

出　　处：《化学研究与应用》2019年第8期1454-1461,共8页Chemical Research and Application

基　　金：国家自然基金项目(81603173)资助;重庆市科学委员会研究项目(cstc2018jcyjAX0754)资助;重庆高校市级重点实验室开放课题项目(CQCM-2017-09,CQCM-2016-09)资助

摘　　要：将柚皮苷与1,3-丙二胺缩合得到一种柚皮苷双席夫碱。通过Th T实验、MTT实验、SOD检测以及细胞内ROS检测考察了该化合物生物活性。实验结果发现,该化合物能有效阻止Cu2+诱导的Aβ1-42聚集、抑制Aβ1-42介导的神经毒性,与未修饰的柚皮苷相比,生物活性明显提高;该化合物能减少经Cu2+-Aβ1-42处理的PC12细胞中的ROS以及提高Cu2+-Aβ1-42处理的PC12细胞中SOD活性。这一研究工作显示,柚皮苷双席夫碱可能是一种具有潜在治疗阿尔茨海默病的药物。A bis-Schiff base was prepared by condensation of 1,3-propylennediamine and naringin in a mixture solvent of ethanol and methanol.The biological activities of this compound were investigated by Th T assay,MTT assay,determination of SOD activity assay and intracellular determination of ROS assay.The results showed that this bis-Schiff base could effectively prevent Cu2+induced the aggregation of Aβ1-42,inhibit Cu2+-Aβ1-42 mediated cytotoxicity of PC12 cells,comparing with unmodified naringin,the Schiff bases had better bio-activities. This compound also could effectively attenuate the production of ROS in Cu2+-Aβ1-42-treated PC12 cells and elevate the SOD activity in Cu2+-Aβ1-42-treated PC12 cells.This work might lead to the development of future drugs for treatment of Alzheimer’s disease.

关 键 词：席夫碱 柚皮苷 阿尔茨海默病 beta-淀粉样多肽 抗氧化 

分 类 号：O614.121[理学—无机化学]