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Design, Synthesis, and Antimicrobial Activity Evaluation of Novel Isocryptolepine Derivatives against Phytopathogenic Fungi and Bacteria
Journal of Agricultural and Food Chemistry ( IF 5.7 ) Pub Date : 2024-09-16 , DOI: 10.1021/acs.jafc.4c03976
Yan-Yan Ding 1 , Ya-Rui Jin 1 , Xiong-Fei Luo 1 , Shao-Yong Zhang 2 , Tian-Li Dai 1 , Li Ma 1 , Zhi-Jun Zhang 1 , Zheng-Rong Wu 2 , Cheng-Xin Jin 1 , Ying-Qian Liu 1, 2, 3
Affiliation  

This research adopted the Fischer indole synthesis method to continue constructing a novel drug-like chemical entity based on the guidance of isocryptolepine and obtained four series of derivatives: Y, Da, Db, and Dc. The antimicrobial activity of these derivatives against plant pathogens was further evaluated. The results showed that Dc-2 had the best antifungal effect against Botrytis cinerea, and its EC50 value was up to 1.29 μg/mL. In addition, an in vivo activity test showed that the protective effect of Dc-2 on apples was 82.2% at 200 μg/mL, which was better than that of Pyrimethanil (45.4%). Meanwhile, it was found by scanning electron microscopy and transmission electron microscopy that the compound Dc-2 affected the morphology of mycelia. The compound Dc-2 was found to damage the cell membrane by PI and ROS staining. Through experiments such as leakage of cell contents, it was found that the compound Dc-2 changed the permeability of the cell membrane and caused the leakage of substances in the cell. According to the above studies, compound Dc-2 can be used as a candidate lead compound for further structural optimization and development.

中文翻译:


新型异隐棘碱衍生物对植物病原真菌和细菌的设计、合成和抗菌活性评价



本研究采用Fischer吲哚合成法,以异隐胆碱为指导继续构建新型药物化学实体,得到了YDaDbDc四个系列的衍生物。进一步评估了这些衍生物对植物病原体的抗菌活性。结果表明, Dc-2灰葡萄孢的抗真菌效果最好,其EC 50值高达1.29 μg/mL。此外,体内活性试验表明,200μg/mL的Dc-2对苹果的保护作用为82.2%,优于嘧霉胺(45.4%)。同时,通过扫描电镜和透射电镜发现化合物Dc-2对菌丝体的形态有影响。通过PI和ROS染色发现化合物Dc-2会损伤细胞膜。通过细胞内容物渗漏等实验发现,化合物Dc-2改变了细胞膜的通透性,导致细胞内物质渗漏。根据上述研究,化合物Dc-2可作为候选先导化合物进行进一步的结构优化和开发。
更新日期:2024-09-16
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