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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。
As bacteria become more resistant to antibiotics, it is increasingly important to find a new antimicrobial agent. Reducing the permeability of bacterial cell membranes to drug molecules is an important factor causing the pathogenic bacteria to develop resistance. One of the ways to overcome membrane-mediated resistance is to utilize iron-carrier-antibiotic conjugates. Iron carrier is a small molecule iron ion chelate secreted by bacteria. After being chelated with iron ion, iron carrier is recognized by specific adventitial receptors and transported to the cytoplasm for bacterial utilization. Synthetic iron-carrier-antibiotic conjugates are recognized by specific outer membrane receptors and then actively transported across the outer membrane into the cytoplasm. When the iron-carrier-antibiotic conjugates reach the cytoplasm, they kill the microorganisms by releasing the drug, which stops further access to iron ions, and the conjugate itself can act as an antibacterial agent. This review summarizes the progress of iron-antibiotic conjugates as a new antibacterial agent, which will help to provide a theoretical basis for further research and development of new antibacterial drugs and have potential significance for the treatment of resistant bacterial diseases.