Department of Chemistry, Chemistry Research Laboratory, The University of Oxford, 12 Mansfield Road, Oxford OX1 3TA, UK.
Trends Pharmacol Sci. 2016 Aug;37(8):689-701. doi: 10.1016/j.tips.2016.05.001. Epub 2016 Jun 4.
Natural products have historically been of crucial importance in the identification and development of antibacterial agents. Interest in these systems has waned in recent years, but the rapid emergence of resistant bacterial strains has forced their re-evaluation as a route to identify novel chemical skeletons with antibacterial activity for elaboration in drug development. This overview examines the current situation, highlights new natural product systems which have been found, together with re-examination of some old ones, and new technologies for their identification. While natural products certainly have the potential to re-emerge as a key start-point in antibacterial drug discovery, reports of new or reinvestigated structures need to be supported with sufficient quality chemical (solubility, stability), biochemical (including toxicity in particular, along with target information) and microbiological [minimum inhibitory concentration (MIC) and resistance frequency] validation data to assist in the identification of promising hit structures and to avoid wasted effort from trawling over already cultivated territory. This is particularly important in a resource-limited research environment.
天然产物在抗菌剂的鉴定和开发中历来具有至关重要的作用。近年来，人们对这些系统的兴趣有所减弱，但耐药菌株的迅速出现迫使人们重新评估它们作为一种途径，以确定具有抗菌活性的新型化学骨架，从而在药物开发中进行阐述。这篇综述考察了当前的情况，强调了已发现的新天然产物系统，以及对一些旧系统的重新检查，以及用于鉴定它们的新技术。虽然天然产物确实有可能重新成为抗菌药物发现的关键起点，但需要用足够质量的化学（溶解度、稳定性）、生化（包括特别是毒性，以及目标信息）和微生物学[最小抑菌浓度（MIC）和耐药频率]验证数据来支持新的或重新研究的结构报告，以帮助确定有前途的命中结构，并避免在已经开发的领域中浪费精力。在资源有限的研究环境中，这一点尤其重要。
