School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China.
Department of Head and Neck Surgery, Stomatological Hospital of China Medical University, Shenyang 110002, People's Republic of China.
J Agric Food Chem. 2024 Jul 3;72(26):14684-14700. doi: 10.1021/acs.jafc.4c01430. Epub 2024 Jun 21.
The overuse of antibiotics in animal farming and aquaculture has led to multidrug-resistant methicillin-sensitive (MR-MSSA) becoming a common pathogen in foodborne diseases. Ait. serves as a traditional plant antibacterial agent and functional food ingredient. A total of 30 compounds (-) were isolated from the root bark of , consisting of 20 new compounds (-). In the biological activity assay, compound demonstrated a remarkable inhibitory effect on MR-MSSA, with an MIC of 2 μg/mL. Furthermore, was found to rapidly eliminate bacteria, inhibit biofilm growth, and exhibit exceptionally low cytotoxicity. Mechanistic studies have revealed that possesses an enhanced membrane-targeting ability, binding to the bacterial cell membrane components phosphatidylglycerol (PG), phosphatidylethanolamine (PE), and cardiolipin (CL). This disruption of bacterial cell membrane integrity increases intracellular reactive oxygen species, protein and DNA leakage, reduced bacterial metabolism, and ultimately bacterial death. In summary, these findings suggest that compound holds promise as a lead compound against MR-MSSA.
在动物养殖和水产养殖中过度使用抗生素导致耐甲氧西林敏感金黄色葡萄球菌（MR-MSSA）成为食源性疾病的常见病原体。艾特作为一种传统的植物抗菌剂和功能性食品成分。从根皮中分离得到了 30 种化合物（-），其中包括 20 种新化合物（-）。在生物活性测定中，化合物对 MR-MSSA 表现出显著的抑制作用，MIC 为 2 μg/mL。此外，还发现能够快速消除细菌、抑制生物膜生长，且表现出极低的细胞毒性。机制研究表明，具有增强的膜靶向能力，与细菌细胞膜成分磷脂酰甘油（PG）、磷脂酰乙醇胺（PE）和心磷脂（CL）结合。这种破坏细菌细胞膜完整性会增加细胞内活性氧物质、蛋白质和 DNA 泄漏，降低细菌代谢，并最终导致细菌死亡。总之，这些发现表明，化合物作为治疗 MR-MSSA 的先导化合物具有很大的潜力。
