常春藤皂苷元-半酯-AZT衍生物的合成及抗病毒蛋白酶活性  

Conjugates of Hederagenin Hemiester Derivatives with AZT as Virus Protease Inhibitors

作　　者：郝永佳 危英 周英 刘青 谌芬 向琴 张华 於祥 吴继春 杨虹 HAO Yong-jia;WEI Ying;ZHOU Ying;LIU Qing;SHEN Fen;XIANG Qin;ZHANG Hua;YU Xiang;WU Ji-chun;YANG Hong(College of Pharmacy, Guizhou University of Traditional Chinese Medicine, Guiyang 550025, China)

机构地区：[1]贵州中医药大学药学院,贵州贵阳550025

出　　处：《合成化学》2021年第9期741-746,共6页Chinese Journal of Synthetic Chemistry

基　　金：国家自然科学基金资助项目(81760758);贵州省教育厅创新群体项目(黔教合KY字[2021]018);中药民族药活性分子发现与研究中心项目(3411-4110000520364);贵州省科技计划项目(黔科合基础-ZK(2021)一般561)。

摘　　要：以常春藤皂苷元为原料,合成了5个常春藤皂苷元-半酯-AZT复合物,其结构经^(1)H NMR、^(13)C NMR和ESI-MS表征。并对所有目标分子体外抗HIV-1和HCV NS3/4A蛋白酶的活性进行了初步评价,化合物5显示较强的抗HCV NS/4A蛋白酶的活性,IC_(50)=5.8μM,其余化合物IC_(50)为10.6~42.3μM。所有衍生物无抗HIV蛋白酶活性,揭示该类衍生物选择性抑制HCV NS3/4A蛋白酶。Five Hederagenin-Hemiester-Zidovudine derivatives(1~5)were synthesized,using Hederagenin as raw material.Their structures were characterized by ^(1)H NMR,^(13)C NMR and ESI-MS.The antivirus activities of 1~5 were investigated by using HIV-1 and HCV NS3/4A proteases.The results indicated that 5 exhibited potent anti HCV NS3/4A protease activity with IC_(50) values of 5.8μM,other compounds show moderate inhibition with IC_(50) values were from 10.6 to 42.3μM.All derivatives no inhibition against HIV protease suggestion selective inhibit HCV NS3/4A protease.

关 键 词：常春藤皂苷元 半酯 HIV-1蛋白酶 HCV NS3/4A蛋白酶 活性 合成 

分 类 号：O625[理学—有机化学]