Liu Xiaojia, Shen Jianzhong, Zhu Kui
National Center for Veterinary Drug Safety Evaluation, College of Veterinary Medicine, China Agricultural University Beijing 00193 China
Beijing Key Laboratory of Detection Technology for Animal-Derived Food Safety and Beijing Laboratory for Food Quality and Safety, China Agricultural University Beijing 100193 China
RSC Med Chem. 2021 Dec 21;13(2):107-116. doi: 10.1039/d1md00351h. eCollection 2022 Feb 23.
The increasing threat to global health posed by antibiotic resistance remains a serious concern. This troublesome scenario has steered a need for the discovery and evaluation of novel antibacterial agents. Natural products are the main sources of antimicrobials used in clinical practice, serving as a rich reservoir for the discovery of new antibiotics. Pharmaceutical phenolics especially xanthones widely exist in the plant kingdom, and are important plant metabolites. They possess versatile biological activities, including antiviral, antibacterial, neurotrophic, and anticancer. In the present study, we focus on the antibacterial activities of phytoxanthones and summarize their structures and sources, categories and drug-likeness evaluations, and antibacterial activities. A total of 226 different plant xanthones are identified through the NETs screening, and most of them are distributed in family. These phytoxanthones are divided into four groups according to the intrinsic structural properties, including the most common simple xanthones and the majority of biprenylated ones. Moreover, their physicochemical parameters are calculated and the structure-activity relationships are discussed as well. These results indicate that the biprenylated xanthone derivatives may be promising antibacterial candidates and that the natural products of plants may be a poorly understood repository for the discovery of novel antibacterial agents.
抗生素耐药性对全球健康构成的威胁日益增加，仍然是一个严重问题。这种棘手的情况引发了对新型抗菌剂的发现和评估的需求。天然产物是临床实践中使用的抗菌剂的主要来源，是发现新抗生素的丰富宝库。药用酚类化合物尤其是呫吨酮广泛存在于植物界，是重要的植物代谢产物。它们具有多种生物活性，包括抗病毒、抗菌、神经营养和抗癌活性。在本研究中，我们聚焦于植物呫吨酮的抗菌活性，并总结它们的结构与来源、类别与类药性评估以及抗菌活性。通过网络筛选共鉴定出226种不同的植物呫吨酮，其中大多数分布在[具体科名未给出]科。这些植物呫吨酮根据其内在结构特性分为四类，包括最常见的简单呫吨酮和大多数双异戊烯基化的呫吨酮。此外，还计算了它们的理化参数并讨论了构效关系。这些结果表明，双异戊烯基化呫吨酮衍生物可能是有前景的抗菌候选物，并且植物天然产物可能是一个尚未被充分了解的新型抗菌剂发现宝库。
