Martins Marta, Dastidar Sujata G, Fanning Seamus, Kristiansen Jette E, Molnar Joseph, Pagès Jean-Marie, Schelz Zsuzsanna, Spengler Gabriella, Viveiros Miguel, Amaral Leonard
Unit of Mycobacteriology, Instituto de Higiene e Medicina Tropical, Universidade Nova de Lisboa, Rua da Junqueira 96, 1349-008 Lisboa, Portugal.
Int J Antimicrob Agents. 2008 Mar;31(3):198-208. doi: 10.1016/j.ijantimicag.2007.10.025. Epub 2008 Jan 3.
Multidrug resistance in Gram-negative bacteria is now known to be primarily caused by overexpression of efflux pumps that extrude unrelated antibiotics from the periplasm or cytoplasm of the bacterium prior to their reaching their intended target. This review focuses on a variety of agents that have been shown to be efflux pump inhibitors (EPIs) and which, if used as 'helper compounds' in combination with antibiotics to which the organism is initially resistant, may produce the required cure. Although not all of the EPIs may serve a helper role owing to their toxicity, they may nevertheless serve as lead compounds.
现在已知革兰氏阴性菌中的多药耐药性主要是由外排泵过度表达引起的，这些外排泵会在无关抗生素到达细菌的周质或细胞质中的预定靶点之前，将其从细菌中排出。本综述重点关注了多种已被证明是外排泵抑制剂（EPI）的药物，如果将它们作为“辅助化合物”与生物体最初耐药的抗生素联合使用，可能会实现所需的治愈效果。尽管并非所有的EPI都因其毒性而能起到辅助作用，但它们仍可能作为先导化合物。
