Liu Xiaojia, Liu Yuan, Song Meirong, Zhu Kui, Shen Jianzhong
National Key Laboratory of Veterinary Public Health and Safety, College of Veterinary Medicine, China Agricultural University, No. 2 Yuanmingyuan West Road, Beijing 100193, China.
Antibiotics (Basel). 2024 Sep 13;13(9):882. doi: 10.3390/antibiotics13090882.
The rise in antibiotic-resistant bacteria highlights the need for novel antimicrobial agents. This study presents the design and synthesis of a series of rhein (RH)-derived compounds with improved antimicrobial properties. The lead compound, RH, exhibited a potent antibacterial activity against () isolates, with minimum inhibitory concentrations (MICs) ranging from 8 to 16 μg/mL. RH disrupted bacterial membrane stability, hindered metabolic processes, and led to an increase in reactive oxygen species (ROS) production. These mechanisms were confirmed through bacterial growth inhibition assays, membrane function assessments, and ROS detection. Notably, RH outperformed the parent compound RH and demonstrated bactericidal effects in . The findings suggest that RH is a promising candidate for further development as an antimicrobial agent against Gram-positive pathogens, addressing the urgent need for new therapies.
抗生素耐药细菌的增加凸显了新型抗菌剂的必要性。本研究介绍了一系列具有改善抗菌特性的大黄酸（RH）衍生化合物的设计与合成。先导化合物RH对（）分离株表现出强效抗菌活性，最低抑菌浓度（MIC）范围为8至16μg/mL。RH破坏细菌膜稳定性，阻碍代谢过程，并导致活性氧（ROS）产生增加。这些机制通过细菌生长抑制试验、膜功能评估和ROS检测得到证实。值得注意的是，RH优于母体化合物RH，并在（）中表现出杀菌作用。研究结果表明，RH作为一种针对革兰氏阳性病原体的抗菌剂具有进一步开发的潜力，满足了对新疗法的迫切需求。
