格尔德霉素衍生物TC-GM的合成及体外抗病毒活性研究  

Synthesis and antiviral activities of geldanamycin analog TC-GM in vitro

作　　者：李春鑫[1] 山广志[1] 樊博[1] 陶佩珍[1] 赵立勋[1] 蒋建东[1] 李玉环[1] 李卓荣[1] 

机构地区：[1]中国医学科学院北京协和医学院医药生物技术研究所,北京100050

出　　处：《药学学报》2011年第6期683-687,共5页Acta Pharmaceutica Sinica

基　　金：国家"重大新药创制"科技重大专项资助项目(2009ZX09301-003);国家自然科学基金资助项目(30772600;30472076)

摘　　要：本文以发现新型抗病毒结构化合物为目的,将不同作用机制的抗病毒活性化合物格尔德霉素和拉米夫定化学偶联得到新结构化合物TC-GM。分别采用p24抗原、斑点杂交法以及细胞病变法(CPE)测定了TC-GM对HIV-1、HBV、HSV和CoxB病毒的抑制活性。结果显示,TC-GM具有与格尔德霉素相似的广谱抗病毒特性,对HIV-1、HBV、HSV 1型和2型、CoxB6等病毒的复制均具有抑制作用,并且抗HIV-1和HBV的活性较强。In order to find antiviral compounds with novel structures,geldanamycin and lamivudine with different antiviral mechanisms were conjunctively synthesized to acquire a new compound TC-GM,and the antiviral activity of TC-GM was measured.The antiviral activity against HIV-1 was examined by p24 antigen ELISA kit.The activity against HBV was examined by dotblot.The activity against HSV and CoxB virus was examined by CPE.TC-GM exhibited broad-spectrum antiviral activities similarly like geldanamycin.TC-GM inhibited the replication of different viruses,including HIV-1,HBV,HSV 1 and 2,CoxB6.TC-GM showed more potent inhibitory activity against HIV-1 and HBV than other detected virus.

关 键 词：TC-GM 合成 抗病毒 格尔德霉素 拉米夫定 

分 类 号：R916[医药卫生—药学]