Köhler T, Pechère J C, Plésiat P
Department of Genetics and Microbiology, Centre Médical Universitaire, Geneva, Switzerland.
Cell Mol Life Sci. 1999 Nov 30;56(9-10):771-8. doi: 10.1007/s000180050024.
Multidrug efflux systems endow on bacterial cells the ability to limit the access of antimicrobial agents to their targets. By actively pumping out antibiotic molecules, these systems prevent the intracellular accumulation necessary for antibiotics to exert their lethal activity. Drug efflux appears to be one of the most widespread antibiotic resistance mechanisms among microorganisms, since it has been demonstrated to occur in many Gram-positive and Gram-negative bacteria including medically important species like staphylococci, streptococci, enterobacteria and opportunistic pathogens like Pseudomonas aeruginosa. Efflux pumps can be specific for only one substrate or accommodate a more or less wide range of noxious products. Export of structurally unrelated compounds confers a multidrug-resistance phenotype on bacterial cells. Therapeutically critical levels of resistance can be achieved by overexpression of efflux systems, especially in those species such as P. aeruginosa which possess a low outer membrane permeability. It is suspected that the dual physiological function of active efflux systems is both the secretion of intracellular metabolites and the protection against a variety of harmful substances that the microorganism may encounter in its natural environment.
多药外排系统赋予细菌细胞限制抗菌剂接近其靶点的能力。通过主动泵出抗生素分子,这些系统可防止抗生素发挥致死活性所必需的细胞内积累。药物外排似乎是微生物中最广泛存在的抗生素耐药机制之一,因为已证明它存在于许多革兰氏阳性菌和革兰氏阴性菌中,包括医学上重要的物种,如葡萄球菌、链球菌、肠杆菌以及像铜绿假单胞菌这样的机会致病菌。外排泵可以只对一种底物具有特异性,或者容纳或多或少范围广泛的有害产物。结构不相关化合物的输出赋予细菌细胞多药耐药表型。通过外排系统的过表达可达到治疗上关键的耐药水平,尤其是在那些外膜通透性低的物种,如铜绿假单胞菌中。据推测,主动外排系统的双重生理功能既是细胞内代谢产物的分泌,也是针对微生物在其自然环境中可能遇到的各种有害物质的保护作用。