Center for Research and Development of Fine Chemicals, Guizhou University, Guiyang 550025, China.
School of Pharmacy, Guizhou University, Guiyang 550025, China.
Int J Mol Sci. 2022 Oct 8;23(19):11947. doi: 10.3390/ijms231911947.
pv. belongs to the Gram-negative species, causing citrus canker that seriously affects the fruit yield and quality of many rutaceae plants. Herein, we found that compound 2-(butyldisulfanyl) quinazolin-4(3)-one exhibited remarkable anti- activity in vitro with a half effective concentration (EC) of 2.6 μg/mL, while the positive controls thiodiazole-copper with 57 μg/mL and bismerthiazol with 68 μg/mL and this compound showed great anti-citrus canker activity in vivo. This active compound also was confirmed to reduce biofilm formation, increase the level of reactive oxygen species, damage the morphological structure of the bacteria, and cause bacterial death. Proteomics and RT-qPCR analysis results indicated that this compound down-regulated the expression of enzymes in the MEP (2-methyl-D-erythritol 4-phosphate) pathway and might achieve destructive ability of . Overall, this study indicates that such derivatives could be a promising scaffold to develop novel bactericides to control citrus canker.
PV. 属于革兰氏阴性种，引起柑橘溃疡病，严重影响多种芸香科植物的果实产量和质量。在此，我们发现化合物 2-（丁基二硫基）喹唑啉-4（3）-酮在体外表现出显著的活性，半数有效浓度（EC）为 2.6μg/mL，而阳性对照噻二唑-铜为 57μg/mL，双咪鲜胺为 68μg/mL，该化合物在体内表现出很强的抗柑橘溃疡病活性。该活性化合物还被证实能减少生物膜的形成，增加活性氧的水平，破坏细菌的形态结构，导致细菌死亡。蛋白质组学和 RT-qPCR 分析结果表明，该化合物下调了 MEP（2-甲基-D-赤藓醇 4-磷酸）途径中酶的表达，可能具有破坏作用。总的来说，这项研究表明，此类衍生物可能成为开发新型杀菌剂来控制柑橘溃疡病的有前途的支架。
