发现新型吲哚衍生物，其中含有二硫缩醛作为植物潜在的抗病毒药物。
Discovery of novel indole derivatives containing dithioacetal as potential antiviral agents for plants.
机构信息
State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Huaxi District, Guiyang 550025, China.
State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Huaxi District, Guiyang 550025, China.
出版信息
Pestic Biochem Physiol. 2020 Jun;166:104568. doi: 10.1016/j.pestbp.2020.104568. Epub 2020 Mar 28.
Thirty unreported indole derivatives containing dithioacetal moiety were synthesized and evaluated for anti-plant viral activity. Bioassay results displayed that some of the target compounds showed better activities against tobacco mosaic virus (TMV) than the commercial Ribavirin in vivo. In particular, anti-TMV curative, protective and inactivating activity of 4p were 55.1, 57.2, and 80.3%, respectively, and EC value for inactivating activity was 88.5 μg/mL. The observation of transmission electron microscope showed that 4p may have a certain destructive effect on TMV particles. To further study, microscale thermophoresis analysis result also demonstrated that 4p powerfully interacted with TMV coat protein in vitro. Hence, this study provides a strong evidence suporting that indole derivatives might be applied as new antiviral agents.
合成了 30 种含有二硫缩醛部分的未报告吲哚衍生物，并评估了它们的抗植物病毒活性。生物测定结果表明，一些目标化合物在体内对烟草花叶病毒（TMV）的活性优于商业利巴韦林。特别是，化合物 4p 对 TMV 的治疗、保护和失活活性分别为 55.1%、57.2%和 80.3%，失活活性的 EC 值为 88.5μg/mL。透射电子显微镜观察表明，4p 可能对 TMV 颗粒有一定的破坏作用。进一步研究，微量热泳动分析结果也表明，4p 能够在体外与 TMV 外壳蛋白强力相互作用。因此，这项研究提供了有力的证据支持，表明吲哚衍生物可能被用作新型抗病毒药物。
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