拓扑异构酶II催化抑制剂对爱泼斯坦-巴尔病毒的抗病毒活性
Antiviral activity of topoisomerase II catalytic inhibitors against Epstein-Barr virus.
作者信息
Wu Ting, Wang Yan, Yuan Yan
机构信息
Institute of Human Virology, Ministry of Education, Zhongshan School of Medicine, Sun Yat-Sen University, Guangzhou 510080, China; Key Laboratory of Tropical Disease Control, Ministry of Education, Zhongshan School of Medicine, Sun Yat-Sen University, Guangzhou 510080, China.
Institute of Human Virology, Ministry of Education, Zhongshan School of Medicine, Sun Yat-Sen University, Guangzhou 510080, China; Guanghua School of Stomatology, Sun Yat-Sen University, Guangdong Provincial Key Laboratory of Stomatology, Guangzhou, China.
出版信息
Antiviral Res. 2014 Jul;107:95-101. doi: 10.1016/j.antiviral.2014.05.003. Epub 2014 May 10.
Herpesviruses require several cellular proteins for their lytic DNA replication including topoisomerase II (Topo II). Thus, Topo II could be an effective drug target against herpesviral infection. In this study, we examined several Topo II catalytic inhibitors for their potentials in blocking EBV replication and becoming efficacious antiviral agents. Topo II catalytic inhibitors in general exhibited marked inhibition of EBV lytic replication and minimal cytotoxicity. In particular, (+)-rutamarin, with the best selectivity index (SI>63) among the inhibitors tested in this study, is effective in inhibiting EBV DNA replication and virion production but shows little adverse effect on cell proliferation, suggesting its potential to become an efficacious and safe drug for the treatment of human diseases associated with EBV infection.
疱疹病毒的裂解性 DNA 复制需要多种细胞蛋白，包括拓扑异构酶 II（Topo II）。因此，Topo II 可能是抗疱疹病毒感染的有效药物靶点。在本研究中，我们检测了几种 Topo II 催化抑制剂阻断 EBV 复制并成为有效抗病毒药物的潜力。一般来说，Topo II 催化抑制剂对 EBV 裂解性复制表现出显著抑制作用，且细胞毒性极小。特别是，（+）-鲁他马林在本研究测试的抑制剂中具有最佳的选择性指数（SI>63），能有效抑制 EBV DNA 复制和病毒粒子产生，但对细胞增殖几乎没有不良影响，表明它有潜力成为治疗与 EBV 感染相关人类疾病的有效且安全的药物。
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