Department of Pharmaceutical Microbiology, Faculty of Pharmacy, Gazi University, 06330, Ankara, Türkiye.
Department of Pharmaceutical Microbiology, Faculty of Pharmacy, Istanbul University, 34116, Istanbul, Türkiye.
Curr Microbiol. 2024 Jun 23;81(8):241. doi: 10.1007/s00284-024-03761-2.
Zoliflodacin is a spiropyrimidinetrione antibiotic that acts by binding to the GyrB part of the DNA gyrase enzyme in bacteria. Its effectiveness for the treatment of Neisseria gonorrhoeae infections has been investigated extensively. Since antibiotic resistance has been reached an alarming rate worldwide, researches on new antimicrobials are considered a priority, especially in the treatment of multidrug-resistant Gram-negative bacteria, such as Klebsiella pneumonia. The aim of this study is to test and compare the effectiveness of zoliflodacin with some traditional antibiotics which are frequently preferred in the treatment of Gram-negative pathogens, primarily K. pneumonia. Additionally, its ability to prevent biofilm formation has also been determined. The minimum inhibitory concentration (MIC) values of zoliflodacin along with levofloxacin, meropenem, gentamicin, ampicillin/sulbactam and ceftazidime/avibactam were evaluated by broth microdilution method against 15 Gram-negative clinical isolates and three standard strains. Also, the synergism potential of zoliflodacin with other antibiotics was evaluated by the checkerboard method against standard strains of K. pneumonia, Pseudomonas aeruginosa, and Acinetobacter baumannii. In addition, the inhibitory effects of zoliflodacin on biofilm formation of standard strains were determined. Zoliflodacin MICs were found to be in the range of 2-64 µg/mL, and its combination with meropenem and ampicillin/sulbactam was found to be synergistic, especially against A. baumannii. Zoliflodacin significantly inhibited A. baumannii biofilm at sub-MIC values. These results indicated that zoliflodacin can be considered as an alternative against infections of Gram-negative pathogens, alone or in combination.
唑利福定是一种螺旋吡喃并嘧啶酮类抗生素，通过与细菌 DNA 回旋酶的 GyrB 部分结合而发挥作用。其治疗淋病奈瑟菌感染的有效性已得到广泛研究。由于抗生素耐药性在全球范围内已达到令人担忧的程度，因此人们认为研究新的抗菌药物是当务之急，特别是在治疗多药耐药革兰氏阴性菌（如肺炎克雷伯菌）方面。本研究旨在测试和比较唑利福定与一些传统抗生素的有效性，这些抗生素在治疗革兰氏阴性病原体方面经常被优先选用，主要是肺炎克雷伯菌。此外，还测定了其预防生物膜形成的能力。采用肉汤微量稀释法测定了唑利福定与左氧氟沙星、美罗培南、庆大霉素、氨苄西林/舒巴坦和头孢他啶/阿维巴坦对 15 株临床分离的革兰氏阴性菌和 3 株标准菌株的最低抑菌浓度（MIC）值。此外，还通过棋盘微量稀释法评估了唑利福定与肺炎克雷伯菌、铜绿假单胞菌和鲍曼不动杆菌标准菌株的其他抗生素的协同作用潜力。此外，还测定了唑利福定对标准菌株生物膜形成的抑制作用。唑利福定 MIC 值在 2-64 µg/mL 之间，其与美罗培南和氨苄西林/舒巴坦联合使用具有协同作用，特别是对鲍曼不动杆菌。唑利福定在亚 MIC 值时可显著抑制鲍曼不动杆菌生物膜的形成。这些结果表明，唑利福定可单独或联合使用作为治疗革兰氏阴性病原体感染的替代药物。
