Roque-Borda Cesar Augusto, Primo Laura Maria Duran Gleriani, Franzyk Henrik, Hansen Paul Robert, Pavan Fernando Rogério
São Paulo State University (UNESP), Tuberculosis Research Laboratory, School of Pharmaceutical Sciences, Araraquara, Brazil.
Universidad Católica de Santa María, Vicerrectorado de Investigación, Arequipa, Peru.
Heliyon. 2024 May 24;10(11):e31958. doi: 10.1016/j.heliyon.2024.e31958. eCollection 2024 Jun 15.
Multi-drug resistant ESKAPE pathogens (, aureus, , , , and Enterobacter species) are a global health threat. The severity of the problem lies in its impact on mortality, therapeutic limitations, the threat to public health, and the costs associated with managing infections caused by these resistant strains. Effectively addressing this challenge requires innovative approaches to research, the development of new antimicrobials, and more responsible antibiotic use practices globally. Antimicrobial peptides (AMPs) are a part of the innate immune system of all higher organisms. They are short, cationic and amphipathic molecules with broad-spectrum activity. AMPs interact with the negatively charged bacterial membrane. In recent years, AMPs have attracted considerable interest as potential antibiotics. However, AMPs have low bioavailability and short half-lives, which may be circumvented by chemical modification. This review presents recent and strategies for the modification of AMPs to improve their stability and application in preclinical experiments.
多重耐药的ESKAPE病原体(金黄色葡萄球菌、肺炎克雷伯菌、鲍曼不动杆菌、铜绿假单胞菌和肠杆菌属)是全球健康威胁。该问题的严重性在于其对死亡率的影响、治疗局限性、对公共卫生的威胁以及管理这些耐药菌株引起的感染相关的成本。有效应对这一挑战需要创新的研究方法、开发新的抗菌药物以及在全球范围内更负责任地使用抗生素。抗菌肽(AMPs)是所有高等生物先天免疫系统的一部分。它们是具有广谱活性的短链阳离子两亲性分子。AMPs与带负电荷的细菌膜相互作用。近年来,AMPs作为潜在的抗生素引起了相当大的关注。然而,AMPs的生物利用度低且半衰期短,这可以通过化学修饰来规避。本综述介绍了最近对AMPs进行修饰以提高其稳定性并应用于临床前实验的策略。