Center for the Study of Human Health, Emory University, 1557 Dickey Drive, Atlanta, Georgia 30322, United States.
Molecular and Systems Pharmacology Program, Laney Graduate School, Emory University, 615 Michael Street, Whitehead 115, Atlanta, Georgia 30322, United States.
Chem Rev. 2021 Mar 24;121(6):3495-3560. doi: 10.1021/acs.chemrev.0c00922. Epub 2020 Nov 9.
The crisis of antibiotic resistance necessitates creative and innovative approaches, from chemical identification and analysis to the assessment of bioactivity. Plant natural products (NPs) represent a promising source of antibacterial lead compounds that could help fill the drug discovery pipeline in response to the growing antibiotic resistance crisis. The major strength of plant NPs lies in their rich and unique chemodiversity, their worldwide distribution and ease of access, their various antibacterial modes of action, and the proven clinical effectiveness of plant extracts from which they are isolated. While many studies have tried to summarize NPs with antibacterial activities, a comprehensive review with rigorous selection criteria has never been performed. In this work, the literature from 2012 to 2019 was systematically reviewed to highlight plant-derived compounds with antibacterial activity by focusing on their growth inhibitory activity. A total of 459 compounds are included in this Review, of which 50.8% are phenolic derivatives, 26.6% are terpenoids, 5.7% are alkaloids, and 17% are classified as other metabolites. A selection of 183 compounds is further discussed regarding their antibacterial activity, biosynthesis, structure-activity relationship, mechanism of action, and potential as antibiotics. Emerging trends in the field of antibacterial drug discovery from plants are also discussed. This Review brings to the forefront key findings on the antibacterial potential of plant NPs for consideration in future antibiotic discovery and development efforts.
抗生素耐药性危机需要创造性和创新性的方法，从化学鉴定和分析到生物活性评估。植物天然产物（NPs）代表了一种有前途的抗菌先导化合物来源，可以帮助填补药物发现管道，以应对日益严重的抗生素耐药性危机。植物 NPs 的主要优势在于其丰富而独特的化学多样性、它们在世界范围内的分布和易于获取、它们具有多种不同的抗菌作用模式，以及从它们中分离出的植物提取物已被证明具有临床疗效。虽然许多研究试图总结具有抗菌活性的 NPs，但从未进行过具有严格筛选标准的全面综述。在这项工作中，系统地回顾了 2012 年至 2019 年的文献，通过关注其生长抑制活性，重点强调了具有抗菌活性的植物衍生化合物。本综述共包括 459 种化合物，其中 50.8%为酚类衍生物，26.6%为萜类化合物，5.7%为生物碱，17%归类为其他代谢物。进一步讨论了 183 种化合物的抗菌活性、生物合成、结构-活性关系、作用机制及其作为抗生素的潜力。还讨论了植物中抗菌药物发现领域的新兴趋势。本综述突出了植物 NPs 的抗菌潜力的关键发现，以供未来抗生素发现和开发工作考虑。
