School of Pharmacy, Laboratory of Bioprospection of Antimicrobial Molecules (LABIMAN), Federal University of Ceará, Fortaleza, CE, 60430-372, Brazil.
Drug Research & Development Center, Federal University of Ceará, Fortaleza, CE, 60430-275, Brazil.
Future Microbiol. 2024 Jan;19:91-106. doi: 10.2217/fmb-2023-0160. Epub 2024 Jan 31.
is a human pathogen responsible for high mortality rates. The development of new antimicrobials is urgent. The authors evaluated the activity of hydralazine along with its synergism with other drugs and action on biofilms. With regard to action mechanisms, the authors evaluated cell viability, DNA damage and molecular docking. MIC and minimum bactericidal concentration values ranged from 128 to 2048 μg/ml. There was synergism with oxacillin (50%) and vancomycin (25%). Hydralazine reduced the viability of biofilms by 50%. After exposure to hydralazine 2× MIC, 58.78% of the cells were unviable, 62.07% were TUNEL positive and 27.03% presented damage in the comet assay (p < 0.05). Hydralazine showed affinity for DNA gyrase and TyrRS. Hydralazine is a potential antibacterial.
是一种人类病原体，可导致高死亡率。急需开发新的抗菌药物。作者评估了肼屈嗪的活性及其与其他药物的协同作用和对生物膜的作用。关于作用机制，作者评估了细胞活力、DNA 损伤和分子对接。MIC 和最小杀菌浓度值范围为 128 至 2048μg/ml。与苯唑西林（50%）和万古霉素（25%）有协同作用。肼屈嗪使生物膜的活力降低了 50%。在暴露于肼屈嗪 2×MIC 后，58.78%的细胞失去活力，62.07%的细胞呈 TUNEL 阳性，27.03%的细胞在彗星试验中出现损伤（p<0.05）。肼屈嗪显示出与 DNA 拓扑异构酶和 TyrRS 的亲和力。肼屈嗪是一种有潜力的抗菌药物。
