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Phenylpropenoids from Bupleurum fruticosum as Anti-Human Rhinovirus Species A Selective Capsid Binders
Journal of Natural Products ( IF 5.1 ) Pub Date : 2017-10-17 00:00:00 , DOI: 10.1021/acs.jnatprod.7b00648
Benedetta Fois 1 , Giulia Bianco 1 , Vijay P. Sonar 1 , Simona Distinto 1 , Elias Maccioni 1 , Rita Meleddu 1 , Claudia Melis 1 , Luisa Marras 2 , Raffaello Pompei 2 , Costantino Floris 3 , Pierluigi Caboni 1 , Filippo Cottiglia 1
Affiliation  

The dichloromethane extract of the leaves of Bupleurum fruticosum was found to inhibit the replication of human rhinovirus (HRV) serotypes 14 and 39. Bioassay-guided fractionation led to the isolation of seven phenylpropenol derivatives (39), two polyacetylenes (1 and 2), and one monoterpene (10). Compounds 1 and 10 were identified as previously undescribed secondary metabolites after extensive 1D and 2D NMR experiments as well as high-resolution mass spectrometry. Compounds 2, 4, and 5 showed a selective inhibition of viral replication against HRV39 serotype, with 2 and 4 being the most active, with EC50 values of 1.8 ± 0.02 and 2.4 ± 0.04 μM. Mechanism of action studies indicated that 4 behaves not only as a capsid binder, interfering with the early phases of virus replication, but also as a late-phase replication inhibitor. Docking experiments were performed to confirm the ability of the antiviral phenylpropenoids to selectively fit into the hydrophobic pocket of VP1-HRV39.

中文翻译:

柴胡柴胡中作为抗人鼻病毒种的苯酚类衣壳结合剂

的叶子的二氯甲烷提取物柴胡fruticosum被发现抑制人鼻病毒(HRV)血清型14和39生物测定引导的分级分离导致7个phenylpropenol衍生物(的隔离的复制3 - 9),两个聚乙炔(12)和一个单萜(10)。经过广泛的1D和2D NMR实验以及高分辨率质谱分析,化合物110被鉴定为先前未描述的次级代谢产物。化合物24,和5结果显示,针对HRV39血清型的病毒复制具有选择性抑制作用,其中24最为活跃,EC 50值为1.8±0.02和2.4±0.04μM。作用机理研究表明,4不仅作为衣壳结合物,干扰病毒复制的早期阶段,而且作为晚期复制抑制剂。进行了对接实验,以确认抗病毒苯基丙烯类化合物选择性装配到VP1-HRV39疏水袋中的能力。
更新日期:2017-10-17
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