Abstract：
The overuse of antibiotics in animal farming and aquaculture has led to multidrug-resistant methicillin-sensitive Staphylococcus aureus (MR-MSSA) becoming a common pathogen in foodborne diseases. Sophora flavescens Ait. serves as a traditional plant antibacterial agent and functional food ingredient. A total of 30 compounds (1-30) were isolated from the root bark of S. flavescens, consisting of 20 new compounds (1-20). In the biological activity assay, compound 1 demonstrated a remarkable inhibitory effect on MR-MSSA, with an MIC of 2 μg/mL. Furthermore, 1 was found to rapidly eliminate bacteria, inhibit biofilm growth, and exhibit exceptionally low cytotoxicity. Mechanistic studies have revealed that 1 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 1 holds promise as a lead compound against MR-MSSA.
摘要：
抗生素在畜牧业和水产养殖中的过度使用导致耐多药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。苦参。作为传统的植物抗菌剂和功能性食品成分。从苦参根皮中分离出化合物(1-30)30,由20种新化合物(1-20)组成。在生物活性测定中，化合物1对MR-MSSA有明显的抑制作用,MIC为2μg/mL。此外，1被发现能迅速消灭细菌，抑制生物膜生长，并表现出异常低的细胞毒性。机理研究表明，1具有增强的膜靶向能力，与细菌细胞膜成分磷脂酰甘油（PG）结合，磷脂酰乙醇胺(PE),和心磷脂（CL）。这种细菌细胞膜完整性的破坏增加了细胞内活性氧，蛋白质和DNA泄漏，减少细菌代谢，最终导致细菌死亡。总之,这些研究结果表明,化合物1有望作为抗MR-MSSA的先导化合物.
