中文摘要：

HIV-1 integrase (在里面) 进主人染色体的病毒的 DNA 的调停的集成是在病毒生命周期的必要的步。导出上皮的生长因素(LEDGF/p75 ) 被发现了在这个过程作为一个细胞的余因子工作的人的透镜。LEDGF/p75-IN 相互作用因此为 anti-HIV 治疗代表一个吸引人的目标。在这研究，自然产品几乎对 HIV-1 的 LEDGF/p75 有约束力的衣袋被屏蔽在里面。24 混合物从中国的国家复合资源中心被选择并且获得。AlphaScreen 试金作为有势力 LEDGF/p75-IN 相互作用禁止者描绘了这 24 个自然产品中的 8 个。其 IC50 珍视的活跃混合物从 0.56 ～ 14.55 汯晹畬牯慯祲慬整 ? 牁汹捡瑥瑡獥瘠慩嘠华牁匭?? 敒捡楴湯吗？

英文摘要：

HIV-1 integrase （IN）-mediated integration of viral DNA into the host chromosome is an essential step in the virus life cycle. Human lens epithelium-derived growth factor （LEDGF/p75） has been found to function as a cellu- lar cofactor in this process. The LEDGF/p75-1N interaction hence represents an attractive target for anti-HIV ther- apy. In this study, natural products were virtually screened against the LEDGF/p75 binding pocket of HIV-1 IN. 24 compounds were selected and obtained from the National Compound Resource Center of China. AlphaScreen as- says characterized 8 of these 24 natural products as potent LEDGF/p75-IN interaction inhibitors. The active com- pounds whose ICs0 values ranged from 0.56 to 14.55 ~mol/L could be used as lead compounds for further investi- gation. This work confirmed that natural products are valuable resources for antiviral drug discovery.