铁载体-抗生素耦合物:一种新型的抗菌制剂

Siderophore-antibiotic conjugates: the new antimicrobial agents

摘要:

随着细菌对抗生素耐药性的增强，寻找一种新型抗菌制剂越来越重要。细菌细胞外膜对药物分子的通透性降低是引起致病菌产生耐药性的一个重要因素，克服膜介导耐药性的方法之一是利用铁载体-抗生素耦合物。铁载体是细菌分泌的一种小分子铁离子螯合物，与铁离子螯合后被特定的外膜受体识别并转运至胞浆内供细菌利用。人工合成的铁载体-抗生素耦合物被特定外膜受体识别后主动转运跨过外膜进入胞质内。当铁载体-抗生素耦合物到达细胞质，它们通过释放药物杀死微生物，这可以阻止进一步获取铁离子，并且耦合物自身也可以作为一种抗菌剂。本文综述了铁载体-抗生素耦合物作为一种新型抗菌制剂的研究进展，有助于为进一步研发新型抗菌药物提供理论基础，对治疗耐药性细菌性疾病具有潜在的重要意义。

Abstract:

To find novel antimicrobial agents are becoming more and more important, since microbial pathogens have increased the resistance to antibiotic. One of reasonable factors is bacteria decreased the membrane permeability to drugs. Siderophore is a small molecular compound secreted by bacteria. After chelating iron, the Siderophore complex was bound by specific outer membrane receptor and transported into the cell. Similarly, the synthesized Siderophore-antibiotic conjugates can be recognized by bacteria and transported into the cell. As soon as the conjugates was transported into the cell, the antibiotic was released and killed the bacteria. Moreover, the conjugates also can prevent the bacteria get more iron. In this paper, we described the research progress of Siderophore-antibiotic conjugates as a novel antimicrobial agents. It will provide a theoretical basis for development of new antimicrobial agents and can help treat disease caused by antibiotic resistant disease.