Antibacterial Activity and Possibly Made of Action of Isoquinoline-3-Carboxylic Acid

Zhiyuan Xu, Haixin Ding, Fu Xin, Xu Yan, Zhu Fadi, Huochun Ye, Zhang Yuan Yuan, Yongxia Guo, Zhang Jing, Feng Gang
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Abstract

Due to the urgent need to develop innovative, environmentally sustainable bactericides, we use the natural product isoquinoline as a lead compound to discover highly active bactericides from isoquinoline derivatives. In this paper, the antibacterial activity of 49 isoquinoline derivatives was evaluated against three plant bacteria in vitro. Among all the derivatives, isoquinoline-3-carboxylic acid (IQ3CA) demonstrated significant antibacterial activity against Ralstonia solanacearum ( Rs), Acidovorax citrulli ( Ac), X. oryzae pv. oryzicola ( Xoc), X. campestris pv. campestris ( Xcc), P. carotovorum subsp. carotovorum ( Pcc), and X. fragariae ( Xf), with EC50 values ranging from 8.38 to 17.35 μg/mL. Furthermore, IQ3CA exhibited a potent protective effect against Ac, with an efficacy of 68.56% at 200 μg/mL, which was not significantly different from that of the positive control kasugamycin (72.48%) and was superior to that of the positive control thiosen copper (64.62%). The scanning electron microscopy observations revealed that treatment of Ac cells with IQ3CA at a concentration of 25 μg/mL resulted in a curved and sunken cell morphology, along with destroyed cell membrane integrity. Additionally, the motility and exopolysaccharides production of Ac were inhibited, and biofilm formation was prevented. These results suggest that IQ3CA holds promise as a lead compound with antibacterial properties against plant diseases.
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异喹啉-3-羧酸的抗菌活性和可能的作用机制
由于迫切需要开发创新的、环境可持续的杀菌剂,我们以天然产物异喹啉为先导化合物,从异喹啉衍生物中发现了高活性杀菌剂。本文评估了 49 种异喹啉衍生物对三种植物细菌的体外抗菌活性。在所有衍生物中,异喹啉-3-羧酸(IQ3CA)对 Ralstonia solanacearum(Rs)、Acidovorax citrulli(Ac)、X.oryzae pv. oryzicola ( Xoc)、X. campestris pv. campestris ( Xcc)、P. carotovorum subsp.此外,IQ3CA 对 Ac 具有很强的保护作用,在 200 μg/mL 浓度下的有效率为 68.56%,与阳性对照卡苏霉素(72.48%)相比差异不大,优于阳性对照硫代森铜(64.62%)。扫描电子显微镜观察发现,用浓度为 25 μg/mL 的 IQ3CA 处理 Ac 细胞后,细胞形态出现弯曲和凹陷,细胞膜完整性遭到破坏。此外,Ac 的运动和外多糖生成也受到抑制,生物膜的形成也被阻止。这些结果表明,IQ3CA有望成为一种具有抗菌特性的植物病害先导化合物。
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