Zhao Liping, Zhang Hui, Zha Li, Zhou Xicheng, Yang Meng
The Second Affiliated Hospital of Jiaxing University, Jiaxing 314000 Zhejiang, China.
Haiyan People's Hospital, Jiaxing 314300 Zhejiang, China.
Lett Appl Microbiol. 2025 Jul 2;78(7). doi: 10.1093/lambio/ovaf086.
Drug repurposing, offers promising opportunities to address infections caused by multidrug-resistant bacteria. This study was to evaluate the bactericidal activity, anti-biofilm properties, and potential mechanisms of the antihistamine drug ebastine against Staphylococcus aureus. The minimum inhibitory concentrations of ebastine against standard and clinical S. aureus isolates were determined using the broth microdilution method. The MIC values ranged from 2 to 8 µg·mL-1, indicating good activity against clinical drug-resistant strains. Time-kill curve analyses revealed a dose-dependent bactericidal effect. Regarding anti-biofilm activity, ebastine significantly inhibited biofilm formation at higher concentrations and demonstrated a moderate ability to eradicate preformed biofilms. Mechanistic studies revealed that ebastine exerted the antimicrobial effects by causing disruption to bacterial membrane integrity and inducing reactive oxygen species generation. Furthermore, safety evaluations showed that ebastine exhibited limited toxicity to mammalian cells, with negligible hemolytic effects and good overall safety profiles. This study provided new insights into the potential applications of ebastine in the field of antimicrobial therapy, highlighting its promise as a non-traditional antibacterial agent.
药物重新利用为解决多重耐药菌引起的感染提供了有前景的机会。本研究旨在评估抗组胺药依巴斯汀对金黄色葡萄球菌的杀菌活性、抗生物膜特性及潜在机制。采用肉汤微量稀释法测定依巴斯汀对标准菌株和临床分离的金黄色葡萄球菌的最低抑菌浓度。最低抑菌浓度值范围为2至8μg·mL-1，表明对临床耐药菌株具有良好活性。时间杀菌曲线分析显示出剂量依赖性杀菌作用。关于抗生物膜活性，依巴斯汀在较高浓度下显著抑制生物膜形成，并表现出适度的根除已形成生物膜的能力。机制研究表明，依巴斯汀通过破坏细菌膜完整性和诱导活性氧生成发挥抗菌作用。此外，安全性评估表明，依巴斯汀对哺乳动物细胞毒性有限，溶血作用可忽略不计，总体安全性良好。本研究为依巴斯汀在抗菌治疗领域的潜在应用提供了新见解，突出了其作为非传统抗菌剂的前景。
