Eco-Friendly Biomaterial Research Center, Korea Research Institute of Bioscience and Biotechnology, Jeongeup 580-185, Republic of Korea.
Bioorg Med Chem. 2010 Nov 1;18(21):7668-74. doi: 10.1016/j.bmc.2010.07.073. Epub 2010 Aug 6.
We evaluated the ability of six polyphenols isolated from the roots of Glycyrrhiza uralensis to inactivate rotaviruses, specially G5P[7] and G8P[7]. Upon finding that all polyphenols possessed anti-rotavirus activity, we evaluated whether these properties were attributable to direct inhibition of the binding of rotavirus to cells and/or to inhibition of viral replication. Using the virucidal assay, we found that all six compounds directly inhibited rotavirus binding, with activity being dependent on the type of virus. The 50% effective inhibitory concentrations (EC(50)) of the six compounds were 18.7-69.5 μM against G5P[7] and 14.7-88.1 μM against G8P[7], respectively. Five of the six compounds inhibited hemagglutination activity. Moreover, the CPE inhibition assay showed that five compounds inhibited viral replication with EC(50) values of 12.1-24.0 μM against G5P[7] and 12.0-42.0 μM against G8P[7], respectively. RT-PCR showed that the compounds suppressed viral RNA synthesis in TF-104 cells. Interestingly, the anti-rotavirus activities of four compounds were attributable to inhibition of both viral absorption and viral replication. These results suggest that compounds isolated from the roots of G. uralensis may be potent anti-rotavirus agents in vivo, acting by inhibiting both viral absorption and viral replication.
我们评估了从甘草根中分离得到的 6 种多酚抑制轮状病毒,特别是 G5P[7]和 G8P[7]的能力。在发现所有多酚都具有抗轮状病毒活性后,我们评估了这些特性是否归因于直接抑制轮状病毒与细胞的结合和/或抑制病毒复制。使用病毒灭活测定法,我们发现这 6 种化合物都能直接抑制轮状病毒的结合,其活性取决于病毒的类型。这 6 种化合物对 G5P[7]的 50%有效抑制浓度(EC(50))分别为 18.7-69.5 μM,对 G8P[7]的 EC(50)分别为 14.7-88.1 μM。这 6 种化合物中的 5 种抑制了血凝活性。此外,CPE 抑制试验表明,这 5 种化合物能抑制病毒复制,对 G5P[7]的 EC(50)值为 12.1-24.0 μM,对 G8P[7]的 EC(50)值为 12.0-42.0 μM。RT-PCR 显示这些化合物能抑制 TF-104 细胞中的病毒 RNA 合成。有趣的是,4 种化合物的抗轮状病毒活性归因于对病毒吸附和病毒复制的双重抑制。这些结果表明,从甘草根中分离得到的化合物可能是体内有效的抗轮状病毒药物,通过抑制病毒吸附和病毒复制发挥作用。