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新型去氢枞酸衍生物的抗毒力策略:设计、合成与抗菌评价。

Anti-Virulence Strategy of Novel Dehydroabietic Acid Derivatives: Design, Synthesis, and Antibacterial Evaluation.

机构信息

National Key Laboratory of Green Pesticide, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for R&D of Fine Chemicals of Guizhou University, Guiyang 550025, China.

出版信息

Int J Mol Sci. 2023 Feb 2;24(3):2897. doi: 10.3390/ijms24032897.

Abstract

Anti-virulence strategies are attractive and interesting strategies for controlling bacterial diseases because virulence factors are fundamental to the infection process of numerous serious phytopathogenics. To extend the novel anti-virulence agents, a series of dehydroabietic acid (DAA) derivatives decorated with amino alcohol unit were semi-synthesized based on structural modification of the renewable natural DAA and evaluated for their antibacterial activity against pv (), pv. (), and pv. (). Compound showed the most promising antibacterial activity against with an EC of 2.7 μg mL. Furthermore, compound demonstrated remarkable control effectiveness against bacterial leaf blight (BLB) in rice, with values of 48.6% and 61.4% for curative and protective activities. In addition, antibacterial behavior suggested that compound could suppress various virulence factors, including EPS, biofilm, swimming motility, and flagella. Therefore, the current study provided promising lead compounds for novel bactericides discovery by inhibiting bacterial virulence factors.

摘要

抗毒策略因其对众多严重植物病原菌的感染过程至关重要,是控制细菌疾病的一种有吸引力且有趣的策略。为了扩展新型抗毒剂,我们基于可再生天然 DAA 的结构修饰,半合成了一系列带有氨基醇单元的去氢枞酸 (DAA) 衍生物,并评估了它们对 pv ()、pv. () 和 pv. () 的抗菌活性。化合物 对 表现出最有希望的抗菌活性,EC 为 2.7 μg mL。此外,化合物 对水稻细菌性叶斑病 (BLB) 表现出显著的防治效果,治疗和保护活性分别为 48.6%和 61.4%。此外,抗菌行为表明,化合物 可以抑制多种毒力因子,包括 EPS、生物膜、泳动性和鞭毛。因此,本研究通过抑制细菌毒力因子,为新型杀菌剂的发现提供了有前景的先导化合物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/df60/9917773/acc46b027c25/ijms-24-02897-g001.jpg

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