4.7 Article

Ferulic acid derivatives with piperazine moiety as potential antiviral agents

期刊

PEST MANAGEMENT SCIENCE
卷 78, 期 4, 页码 1749-1758

出版社

JOHN WILEY & SONS LTD
DOI: 10.1002/ps.6794

关键词

ferulic acid; tobacco mosaic virus; cucumber mosaic virus; omics analysis; photosynthesis

资金

  1. National Natural Science Foundation of China [21867006]
  2. National Key Research and Development Program of China [2017YFD0201404]
  3. Construction Project of Key Laboratories from the Education Department of Guizhou Province [QJHKY[2018]001]
  4. Natural Science Foundation of Guizhou Province [QKHJC[2019]1435]

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By synthesizing and screening, novel ferulic acid derivatives were discovered to have excellent antiviral activity, among which compound E2 exhibited remarkable curative activities against tobacco mosaic virus and cucumber mosaic virus. The outstanding antiviral activity of compound E2 was achieved by increasing host photosynthesis, making it a potential lead structure for the development of new antiviral agents.
Background Plant virus diseases are difficult to control and severely threaten the productivity of crops, which leads to huge financial losses. To discover the new antiviral drugs, 34 novel ferulic acid derivatives with piperazine moiety were synthesized, and the antiviral activities were systematically screened as well. Results Bioassay results indicated that most of the target compounds had outstanding antiviral activities against tobacco mosaic virus (TMV) and cucumber mosaic virus (CMV) in vivo. In particular, compound E2 exhibited remarkable curative activities to TMV and CMV with EC50 values of 189.0 and 401.7 mu g/mL compared to those for ningnanmycin (387.0, 519.3 mu g/mL) and ribavirin (542.1, 721.5 mu g/mL). And then the mechanisms of compound E2 were studied by chlorophyll content, differentially expressed proteins and genes tests. Conclusion The excellent antiviral activity of compound E2 was closely associated with the increase in host photosynthesis, which was confirmed by chlorophyll content, differentially expressed proteins and genes assays. Compound E2 can be considered as a lead structure for the discovery of new antiviral agents.

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