基于天然产物改造的细菌生物膜清除剂研究进展

Research progress of bacterial biofilm eradication agents based on modifications of natural products

细菌生物膜广泛存在于各类细菌之中,与约80%的细菌感染有关,是细菌对现有抗生素产生耐受性和耐药性的主要原因之一。因此,开发新型抗生物膜药物具有重要意义。目前的抗生物膜剂主要有3类:生物膜形成抑制剂、生物膜分散剂和生物膜清除剂。其中,生物膜清除剂不同于另外两种,可作为单药杀死生物膜内细菌并清除生物膜,是一种具有潜力的抗菌药物。研究人员对具有抗菌活性的天然产物进行筛选与改造,发现了多种具有生物膜清除活性的化合物,如酰基缩酚酸肽、吡咯霉素、卤代吩嗪和卤代8-羟基喹啉及其衍生物等。本文按照结构和作用机制,对几种主要生物膜清除剂的研究现状进行综述。

Bacterial biofilm widely exists in all kinds of bacteria,and is related to about 80 percent of bacterial infections.It is one of the main reasons for bacterial tolerance and resistance to existing antibiotics.Therefore,there is unmet clinical need for new anti-biofilm drugs.At present,there are three kinds of anti-biofilm agents under research,including biofilm inhibitors,biofilm dispersal agents and biofilm eradication agents.Among them,the biofilm eradication agent is unique,which can not only kill bacteria in biofilm but also eliminate biofilm as a monotherapy.Based on modifications of natural products with antibacterial activity,a variety of compounds with biofilm eradicating activities have been obtained,such as,acyldepsipeptides,pyrrolomycins,halogenated phenazines and halogenated 8-hydroxyquinolines.In this review,we summarize several major biofilm eradication agents above according to their structures and mechanisms.