Department of Pharmacy, University of Malakand, Khyber Pakhtoonkhwa, (KP) 18000, Pakistan,
Department of Pharmacy, University of Peshawar, Peshawar, Pakistan.
Front Biosci (Landmark Ed). 2017 Jan 1;22(4):732-756. doi: 10.2741/4513.
Efflux mediated multidrug resistance (MDR) is a major problem in the treatment of bacterial, fungal and protozoal infections in addition to cancer chemotherapy. Among other well known mechanisms, efflux pumps are significant contributors to chemo-resistance. Efflux mediated resistance generally occurs through up-regulation of genes responsible for the expression of transporter proteins extruding drugs from the cell to create intracellular sub-therapeutic concentrations leading to resistance. The rapid expansion of MDR pathogens necessitates the discovery of resistance modifying drugs, which in combination with antimicrobial or chemotherapeutic agents would tend to reinstate the action of these drugs and avert the emergence of acquired resistance. This review describes the existence of efflux pumps in prokaryotes and eukaryotes as well as their role in chemo-resistance with a special focus on natural product-derived efflux pump inhibitors.
除癌症化疗外，外排介导的多药耐药（MDR）也是治疗细菌、真菌和原生动物感染的主要问题。除了其他众所周知的机制外，外排泵也是化学抗性的重要贡献者。外排介导的耐药性通常通过负责表达将药物从细胞中排出以在细胞内产生亚治疗浓度从而导致耐药性的转运蛋白的基因的上调而发生。MDR 病原体的迅速扩张需要发现耐药性修饰药物，这些药物与抗菌或化学治疗剂联合使用，往往会恢复这些药物的作用，并防止获得性耐药性的出现。本综述描述了原核生物和真核生物中外排泵的存在及其在化学抗性中的作用，特别关注天然产物衍生的外排泵抑制剂。
