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格尔德霉素类似物TC-GM的体外合成及抗病毒活性

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

作者信息

Li Chun-Xin, Shan Guang-Zhi, Fan Bo, Tao Pei-Zhen, Zhao Li-Xun, Jiang Jian-Dong, Li Yu-Huan, Li Zhuo-Rong

机构信息

Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.

出版信息

Yao Xue Xue Bao. 2011 Jun;46(6):683-7.

Abstract

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.

摘要

为了寻找具有新型结构的抗病毒化合物,将具有不同抗病毒机制的格尔德霉素和拉米夫定联合合成,得到一种新化合物TC-GM,并测定了TC-GM的抗病毒活性。采用p24抗原ELISA试剂盒检测其对HIV-1的抗病毒活性。采用斑点印迹法检测其对HBV的活性。采用细胞病变效应(CPE)检测其对HSV和柯萨奇B病毒的活性。TC-GM表现出与格尔德霉素相似的广谱抗病毒活性。TC-GM抑制包括HIV-1、HBV、HSV 1和2、柯萨奇B6在内的不同病毒的复制。TC-GM对HIV-1和HBV的抑制活性比其他检测病毒更强。

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