Qun Tang, Zhou Tiantian, Hao Jiongkai, Wang Chunmei, Zhang Keyu, Xu Jing, Wang Xiaoyang, Zhou Wen
Shanghai Veterinary Research Institute, Chinese Academy of Agricultural Sciences 200241 Shanghai China
School of Chinese Materia Medica, Guangdong Pharmaceutical University 440113 Guangzhou China.
RSC Med Chem. 2023 Jul 10;14(8):1446-1471. doi: 10.1039/d3md00116d. eCollection 2023 Aug 16.
With the increasing prevalence of untreatable infections caused by antibiotic-resistant bacteria, the discovery of new drugs from natural products has become a hot research topic. The antibacterial activity of anthraquinones widely distributed in traditional Chinese medicine has attracted much attention. Herein, the structure and activity relationships (SARs) of anthraquinones as bacteriostatic agents are reviewed and elucidated. The substituents of anthraquinone and its derivatives are closely related to their antibacterial activities. The stronger the polarity of anthraquinone substituents is, the more potent the antibacterial effects appear. The presence of hydroxyl groups is not necessary for the antibacterial activity of hydroxyanthraquinone derivatives. Substitution of di-isopentenyl groups can improve the antibacterial activity of anthraquinone derivatives. The rigid plane structure of anthraquinone lowers its water solubility and results in the reduced activity. Meanwhile, the antibacterial mechanisms of anthraquinone and its analogs are explored, mainly including biofilm formation inhibition, destruction of the cell wall, endotoxin inhibition, inhibition of nucleic acid and protein synthesis, and blockage of energy metabolism and other substances.
随着由抗生素耐药细菌引起的难以治疗的感染日益普遍，从天然产物中发现新药已成为一个热门研究课题。广泛分布于中药中的蒽醌类化合物的抗菌活性备受关注。在此，对作为抑菌剂的蒽醌类化合物的结构与活性关系（SARs）进行综述和阐释。蒽醌及其衍生物的取代基与其抗菌活性密切相关。蒽醌取代基的极性越强，其抗菌效果越显著。羟基蒽醌衍生物的抗菌活性并非必需羟基的存在。二异戊烯基的取代可提高蒽醌衍生物的抗菌活性。蒽醌的刚性平面结构降低了其水溶性并导致活性降低。同时，探讨了蒽醌及其类似物的抗菌机制，主要包括抑制生物膜形成、破坏细胞壁、抑制内毒素、抑制核酸和蛋白质合成以及阻断能量代谢等物质。
