Al-Rabia Mohammed W, Asfour Hani Z, Alhakamy Nabil A, Bazuhair Mohammed A, Ibrahim Tarek S, Abbas Hisham A, Mansour Basem, Hegazy Wael A H, Seleem Noura M
Department of Clinical Microbiology and Immunology, Faculty of Medicine, King Abdulaziz University, Jeddah, 21589, Saudi Arabia.
Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah, 21589, Saudi Arabia.
AMB Express. 2024 Aug 1;14(1):87. doi: 10.1186/s13568-024-01740-1.
Resistance to antibiotics is a critical growing public health problem that desires urgent action to combat. To avoid the stress on bacterial growth that evokes the resistance development, anti-virulence agents can be an attractive strategy as they do not target bacterial growth. Quorum sensing (QS) systems play main roles in controlling the production of diverse virulence factors and biofilm formation in bacteria. Thus, interfering with QS systems could result in mitigation of the bacterial virulence. Cilostazol is an antiplatelet and a vasodilator FDA approved drug. This study aimed to evaluate the anti-virulence activities of cilostazol in the light of its possible interference with QS systems in Pseudomonas aeruginosa. Additionally, the study examines cilostazol's impact on the bacterium's ability to induce infection in vivo, using sub-inhibitory concentrations to minimize the risk of resistance development. In this context, the biofilm formation, the production of virulence factors and influence on the in vivo ability to induce infection were assessed in the presence of cilostazol at sub-inhibitory concentration. Furthermore, the outcome of combination with antibiotics was evaluated. Cilostazol interfered with biofilm formation in P. aeruginosa. Moreover, swarming motility, biofilm formation and production of virulence factors were significantly diminished. Histopathological investigation revealed that liver, spleen and kidney tissues damage was abolished in mice injected with cilostazol-treated bacteria. Cilostazol exhibited a synergistic outcome when used in combination with antibiotics. At the molecular level, cilostazol downregulated the QS genes and showed considerable affinity to QS receptors. In conclusion, Cilostazol could be used as adjunct therapy with antibiotics for treating Pseudomonal infections. This research highlights cilostazol's potential to combat bacterial infections by targeting virulence mechanisms, reducing the risk of antibiotic resistance, and enhancing treatment efficacy against P. aeruginosa. These findings open avenues for repurposing existing drugs, offering new, safer, and more effective infection control strategies.
抗生素耐药性是一个日益严重的关键公共卫生问题,亟需采取行动加以应对。为避免因细菌生长应激而引发耐药性发展,抗毒力药物可能是一种颇具吸引力的策略,因为它们并不针对细菌生长。群体感应(QS)系统在控制细菌中多种毒力因子的产生和生物膜形成方面发挥着主要作用。因此,干扰QS系统可能会减轻细菌的毒力。西洛他唑是一种经美国食品药品监督管理局(FDA)批准的抗血小板和血管舒张药物。本研究旨在根据西洛他唑对铜绿假单胞菌QS系统可能的干扰作用,评估其抗毒力活性。此外,该研究还使用亚抑菌浓度来尽量降低耐药性发展风险,考察了西洛他唑对细菌体内诱导感染能力的影响。在此背景下,评估了亚抑菌浓度的西洛他唑存在时生物膜的形成、毒力因子的产生以及对体内诱导感染能力的影响。此外,还评估了与抗生素联合使用的效果。西洛他唑干扰了铜绿假单胞菌生物膜的形成。此外,群体游动、生物膜形成和毒力因子的产生均显著减少。组织病理学研究表明,注射经西洛他唑处理细菌的小鼠肝脏、脾脏和肾脏组织损伤消失。西洛他唑与抗生素联合使用时表现出协同效果。在分子水平上,西洛他唑下调了QS基因,并对QS受体表现出相当的亲和力。总之,西洛他唑可作为抗生素的辅助疗法用于治疗铜绿假单胞菌感染。本研究强调了西洛他唑通过靶向毒力机制、降低抗生素耐药性风险以及增强对铜绿假单胞菌的治疗效果来对抗细菌感染的潜力。这些发现为现有药物的重新利用开辟了道路,提供了新的、更安全且更有效的感染控制策略。