Key Laboratory of Etiology and Epidemiology of Emerging Infectious Diseases in Universities of Shandong , Taishan Medical College , Taian , Shandong 271000 , People's Republic of China.
School of Public Health , Taishan Medical College , Taian , Shandong 271000 , People's Republic of China.
J Nat Prod. 2019 May 24;82(5):1089-1097. doi: 10.1021/acs.jnatprod.8b00735. Epub 2019 May 7.
Coxsackievirus A16 (CVA16) is one of the most prevalent enteroviral pathogens associated with hand, foot, and mouth disease. In the present study, we have investigated (1) whether the bioactive compound acetylshikonin (AS) inhibits CVA16 infection in vitro and in vivo and (2) the potential antiviral mechanism(s). The results suggest that AS is nontoxic at concentrations of up to 5 μmol/L and could directly inactivate virus particles at relatively low concentrations (0.08 μmol/L), thereby rendering CVA16 incapable of cellular entry. Correspondingly, the expression of viral RNA in vitro was also reduced 100-fold ( P < 0.05) when compared to infected, untreated controls. Results from a CVA16-infected neonatal mouse model indicate that, in comparison to the virus-infected, untreated group, body weights of the mice in the virus-infected, compound-treated group increased more steadily with less severe clinical symptoms. In addition, viral loads in internal organs significantly decreased in treated animals, concomitantly with both reduced pathology and diminished expression of the proinflammatory cytokines IFN-γ and IL-6. In conclusion, AS exerted an inhibitory effect on CVA16 infection in vitro and in vivo. Our study provides a basis for further investigations of AS-type compounds to develop therapeutics to mitigate CVA-associated disease in children.
柯萨奇病毒 A16(CVA16)是与手足口病相关的最常见肠道病毒病原体之一。在本研究中,我们研究了(1)生物活性化合物乙酰紫草素(AS)是否在体外和体内抑制 CVA16 感染,以及(2)潜在的抗病毒机制。结果表明,AS 在高达 5 μmol/L 的浓度下是无毒的,并且可以在相对较低的浓度(0.08 μmol/L)下直接灭活病毒颗粒,从而使 CVA16 无法进入细胞。相应地,与感染且未处理的对照相比,体外病毒 RNA 的表达也减少了 100 倍(P < 0.05)。CVA16 感染的新生小鼠模型的结果表明,与病毒感染且未处理的组相比,病毒感染且用化合物处理的组的小鼠体重增加更稳定,临床症状较轻。此外,在治疗动物中,内部器官中的病毒载量显著降低,同时病理减少,促炎细胞因子 IFN-γ和 IL-6 的表达减少。总之,AS 对 CVA16 的体外和体内感染均具有抑制作用。我们的研究为进一步研究 AS 类化合物以开发治疗药物减轻儿童 CVA 相关疾病提供了依据。