肠道病毒71(EV71)是手足口病的主要病原体,是严重危害儿童健康的重要病毒,目前尚无针对EV71的有效药物。
近期,中国科学院广州生物医药与健康研究院彭涛课题组与中科院昆明植物所罗晓东课题组合作,通过对传统药用植物提取物进行抗病毒活性物质筛选,发现Chrysosplenetin和Penduletin对EV71具有较强的抑制活性。

抑制EV71病毒免疫组化图
在对抑制EV71的作用机制研究中发现,化合物Chrysosplenetin和Penduletin都能够有效抑制病毒RNA的合成。进一步研究表明,两种化合物对多种人肠道病毒都表现出相似的抑制活性。这些活性化合物的发现,为抗EV71药物的开发提供了先导化合物。
相关研究结果最近在线发表于《欧洲药物科学杂志》(European Journal of Pharmaceutical Sciences)。该研究得到了科技部973项目“中国特有植物和微生物药用活性物质的基础研究”的支持。
相关英文论文摘要:
Inhibition of enterovirus 71 replication by chrysosplenetin and penduletin
In recent years, enterovirus 71 (EV71) infections have caused an increasing epidemic in young children, accompanying with more severe nervous system disease and more deaths. Unfortunately, there is no specific medication for it so far. Here we investigated the anti-EV71 activity of chrysosplenetin and penduletin, two o-methylated flavonols isolated from the leaves of Laggera pterodonta. These two compounds were found to have strong activity in vitro against EV71 with low cytotoxicity. In the cytopathic effect (CPE) inhibition assays, both plaque reduction assay and virus yield inhibition assay, the compounds showed a similar 50% inhibitory concentration (IC50) value of about 0.20 μM. The selectivity indices (SI) of chrysosplenetin and penduletin were 107.5 and 655.6 in African green monkey kidney (Vero) cells, and 69.5 and 200.5 in human rhabdomyosarcoma (RD) cells, accordingly. The preliminary mechanism analysis indicates that they function not through blocking virus entry or inactivating virus directly but inhibiting viral RNA replication. In the time-of-addition assay, both compounds inhibited progeny virus production and RNA replication by nearly 100% when introduced within 4 h post infection. In addition to EV71, both compounds inhibited several other human enteroviruses with similar efficacy. These findings provide a significant lead for the discovery of anti-EV71 drug.
