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Natural products as inspiration for the development of bacterial antibiofilm agents.
Natural Product Reports ( IF 10.2 ) Pub Date : 2020-07-01 , DOI: 10.1039/d0np00022a Roberta J Melander 1 , Akash K Basak , Christian Melander
Natural Product Reports ( IF 10.2 ) Pub Date : 2020-07-01 , DOI: 10.1039/d0np00022a Roberta J Melander 1 , Akash K Basak , Christian Melander
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Natural products have historically been a rich source of diverse chemical matter with numerous biological activities, and have played an important role in drug discovery in many areas including infectious disease. Synthetic and medicinal chemistry have been, and continue to be, important tools to realize the potential of natural products as therapeutics and as chemical probes. The formation of biofilms by bacteria in an infection setting is a significant factor in the recalcitrance of many bacterial infections, conferring increased tolerance to many antibiotics and to the host immune response, and as yet there are no approved therapeutics for combatting biofilm-based bacterial infections. Small molecules that interfere with the ability of bacteria to form and maintain biofilms can overcome antibiotic tolerance conferred by the biofilm phenotype, and have the potential to form combination therapies with conventional antibiotics. Many natural products with anti-biofilm activity have been identified from plants, microbes, and marine life, including: elligic acid glycosides, hamamelitannin, carolacton, skyllamycins, promysalin, phenazines, bromoageliferin, flustramine C, meridianin D, and brominated furanones. Total synthesis and medicinal chemistry programs have facilitated structure confirmation, identification of critical structural motifs, better understanding of mechanistic pathways, and the development of more potent, more accessible, or more pharmacologically favorable derivatives of anti-biofilm natural products.
中文翻译：
天然产物作为细菌抗生物膜剂开发的灵感。
天然产物历来是具有多种生物活性的多种化学物质的丰富来源，并且在包括传染病在内的许多领域的药物发现中发挥着重要作用。合成化学和药物化学已经并将继续成为实现天然产物作为治疗剂和化学探针潜力的重要工具。感染环境中细菌形成的生物膜是许多细菌感染难治性的一个重要因素，从而增加了对许多抗生素和宿主免疫反应的耐受性，但迄今为止，还没有批准的治疗方法来对抗基于生物膜的细菌感染。干扰细菌形成和维持生物膜能力的小分子可以克服生物膜表型赋予的抗生素耐受性，并有可能与常规抗生素形成联合疗法。已从植物、微生物和海洋生物中鉴定出许多具有抗生物膜活性的天然产物，包括：鞣花酸苷、金缕梅单宁、carolacton、skyllamycins、promysalin、吩嗪、bromoageliferin、flustramine C、meridianin D 和溴化呋喃酮。全合成和药物化学项目促进了结构确认、关键结构基序的识别、对机制途径的更好理解以及抗生物膜天然产物的更有效、更容易获得或更药理学上更有利的衍生物的开发。
更新日期：2020-07-01
中文翻译：
天然产物作为细菌抗生物膜剂开发的灵感。
天然产物历来是具有多种生物活性的多种化学物质的丰富来源，并且在包括传染病在内的许多领域的药物发现中发挥着重要作用。合成化学和药物化学已经并将继续成为实现天然产物作为治疗剂和化学探针潜力的重要工具。感染环境中细菌形成的生物膜是许多细菌感染难治性的一个重要因素，从而增加了对许多抗生素和宿主免疫反应的耐受性，但迄今为止，还没有批准的治疗方法来对抗基于生物膜的细菌感染。干扰细菌形成和维持生物膜能力的小分子可以克服生物膜表型赋予的抗生素耐受性，并有可能与常规抗生素形成联合疗法。已从植物、微生物和海洋生物中鉴定出许多具有抗生物膜活性的天然产物，包括：鞣花酸苷、金缕梅单宁、carolacton、skyllamycins、promysalin、吩嗪、bromoageliferin、flustramine C、meridianin D 和溴化呋喃酮。全合成和药物化学项目促进了结构确认、关键结构基序的识别、对机制途径的更好理解以及抗生物膜天然产物的更有效、更容易获得或更药理学上更有利的衍生物的开发。
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