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New Axially Chiral Molecular Scaffolds with Antibacterial Activities against Xanthomonas oryzae pv. oryzae for Protection of Rice
Journal of Agricultural and Food Chemistry ( IF 5.7 ) Pub Date : 2022-05-11 , DOI: 10.1021/acs.jafc.2c01407 Yanlin Chen 1 , Tingting Li 1 , Zhichao Jin 1 , Yonggui Robin Chi 1, 2
Journal of Agricultural and Food Chemistry ( IF 5.7 ) Pub Date : 2022-05-11 , DOI: 10.1021/acs.jafc.2c01407 Yanlin Chen 1 , Tingting Li 1 , Zhichao Jin 1 , Yonggui Robin Chi 1, 2
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A new class of axially chiral thiazine molecules were constructed and showed promising antibacterial activities against the plant pathogen Xanthomonas oryzae pv. oryzae (Xoo). The axial chiralities of these compounds (R- or S-atropisomer) showed clear impacts on the in vitro inhibitory activities against Xoo. An optimal molecule of this class with the (S)-axially chiral configuration was identified to exhibit inhibitory activity against Xoo with an EC50 value of 4.18 μg/mL. This inhibition efficiency is superior to that of two commercial antibacterial agrochemicals, thiodiazole-copper and bismerthiazol, as the positive controls. This hit compound also performed better than the controls in our in vivo studies. Preliminary mechanistic studies via scanning electron microscopy images showed that our hit compound at a concentration of 10 μg/mL destroyed the bacterial integrity of Xoo. Label-free quantitative proteomics analysis indicated that a total of 366 differentially expressed proteins of the rice plants were significantly influenced in the presence of our hit molecule.
中文翻译：
具有抗米黄单胞菌活性的新型轴向手性分子支架 pv. 稻米保护用米
构建了一类新的轴向手性噻嗪分子，并显示出对植物病原体Xanthomonas oryzae pv 的有希望的抗菌活性。米（Xoo）。这些化合物（R-或S-阻转异构体）的轴向手性对Xoo的体外抑制活性有明显的影响。具有 ( S )-轴向手性构型的此类最佳分子被鉴定为对Xoo具有抑制活性，EC 50值为 4.18 μg/mL。这种抑制效率优于作为阳性对照的两种商业抗菌农用化学品，即硫代二唑铜和双汞噻唑。在我们的体内研究中，这种命中化合物的表现也优于对照。通过扫描电子显微镜图像进行的初步机制研究表明，我们的 10 μg/mL 浓度的命中化合物破坏了Xoo的细菌完整性。无标记定量蛋白质组学分析表明，在我们的命中分子存在下，共有 366 种水稻植物的差异表达蛋白质受到显着影响。
更新日期：2022-05-11
中文翻译：
具有抗米黄单胞菌活性的新型轴向手性分子支架 pv. 稻米保护用米
构建了一类新的轴向手性噻嗪分子，并显示出对植物病原体Xanthomonas oryzae pv 的有希望的抗菌活性。米（Xoo）。这些化合物（R-或S-阻转异构体）的轴向手性对Xoo的体外抑制活性有明显的影响。具有 ( S )-轴向手性构型的此类最佳分子被鉴定为对Xoo具有抑制活性，EC 50值为 4.18 μg/mL。这种抑制效率优于作为阳性对照的两种商业抗菌农用化学品，即硫代二唑铜和双汞噻唑。在我们的体内研究中，这种命中化合物的表现也优于对照。通过扫描电子显微镜图像进行的初步机制研究表明，我们的 10 μg/mL 浓度的命中化合物破坏了Xoo的细菌完整性。无标记定量蛋白质组学分析表明，在我们的命中分子存在下，共有 366 种水稻植物的差异表达蛋白质受到显着影响。
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