2. Academic Validation
  3. Novel Ethyl-3-Aryl-2-Nitroacrylate Derivatives as Potential T3SS Inhibitors against Xanthomonas oryzae pv. oryzae on Rice

Novel Ethyl-3-Aryl-2-Nitroacrylate Derivatives as Potential T3SS Inhibitors against Xanthomonas oryzae pv. oryzae on Rice

  • J Agric Food Chem. 2023 Jun 21;71(24):9291-9301. doi: 10.1021/acs.jafc.3c00838.
Dongni Gao 1,  Hui Li 2,  Jiang Shao 1,  Lulu He 1,  Chen Fu 1,  Hongyu Lai 1,  Dylan O'Neill Rothenberg 3,  Xiaoli Xu 4,  Gaopeng Song 2,  Xin Deng 5 6,  Zi-Ning Cui 1
Affiliations

Affiliations

  • 1 National Key Laboratory of Green Pesticide, Integrative Microbiology Research Centre, Guangdong Province Key Laboratory of Microbial Signals and Disease Control, College of Plant Protection, South China Agricultural University, Guangzhou 510642, China.
  • 2 College of Materials and Energy, South China Agricultural University, Guangzhou 510642, China.
  • 3 College of Horticulture Science, South China Agricultural University, Guangzhou 510642, China.
  • 4 Instrumental Analysis & Research Center, South China Agricultural University, Guangzhou 510642, China.
  • 5 Department of Biomedical Sciences, City University of Hong Kong, Kowloon Tong, Hong Kong SAR 999077, China.
  • 6 Shenzhen Research Institute, City University of Hong Kong, Shenzhen 518057, China.
PMID: 37285515 DOI: 10.1021/acs.jafc.3c00838
Abstract

Bacterial leaf blight (BLB) caused by Xanthomonas oryzae pv. oryzae (Xoo) is a highly destructive Bacterial disease. Traditional prevention methods have utilized Antibiotics to target Bacterial growth, which has accelerated the emergence of resistant strains. New prevention techniques are developing agents such as type III secretion system (T3SS) inhibitors that target Bacterial virulence factors without affecting Bacterial growth. To explore novel T3SS inhibitors, a series of ethyl-3-aryl-2-nitroacrylate derivatives were designed and synthesized. Preliminary screening of T3SS inhibitors was based on the inhibition of the hpa1 gene promoter and showed no effect on Bacterial growth. Compounds B9 and B10, obtained in the primary screening, significantly inhibited the hypersensitive response (HR) in tobacco and the expression of T3SS genes in the hrp cluster including key regulatory genes. In vivo bioassays showed that T3SS inhibitors obviously inhibited BLB and appeared to be more effective when combined with quorum quenching bacteria F20.

Keywords

ethyl-3-aryl-2-nitroacrylate; inhibitors; quorum quenching; synthesis; type III secretion system (T3SS).

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