Enrofloxacin is a fluoroquinolone antibiotic with a broad antibacterial spectrum and high bactericidal activity against major pathogenic bacteria [1]. Enrofloxacin binds to the DNA-topoisomerase complex at the cleavage–ligation site, leading to conformational changes in the enzyme and inhibiting DNA replication through inefficient DNA ligation [2]. Enrofloxacin has been used to control bacterial infections of the mastitis, respiratory, and gastrointestinal tracts in cattle[3].
In vitro, Enrofloxacin treatment (40µg/ml) for 72 hours significantly increased the γH2Ax level in Abrams cells and led to a significant decrease in cell viability[4]. Treatment with 200µg/ml Enrofloxacin for 4 days induced the characteristic of DNA fragmentation and the condensation of apoptotic cell nuclei in canine tendon cells and chondrocytes[5]. Treatment with 200µg/ml Enrofloxacin for 24 hours induced the release of lactate dehydrogenase (LDH) and an increase in reactive oxygen species (ROS) levels in L8824 cells, disrupting mitochondrial membrane potential and promoting cell death[6].
In vivo, Enrofloxacin treatment via oral administration at a dose of 10mg/kg every 12 hours for 7 days significantly reduced lung inflammation in mice after cerebral middle artery occlusion (MCAo), increased the survival rate of mice, and prevented weight loss[7]. Oral administration of water containing 0.27mg/ml Enrofloxacin daily for 2 weeks significantly alleviated the symptoms of contact sensitivity (CS) in mice, altered the composition of the intestinal flora, and promoted anti-inflammatory responses[8].
References:
[1] Lopez-Cadenas C, Sierra-Vega M, Garcia-Vieitez J J, et al. Enrofloxacin: pharmacokinetics and metabolism in domestic animal species[J]. Current Drug Metabolism, 2013, 14(10): 1042-1058.
[2] Grabowski Ł, Gaffke L, Pierzynowska K, et al. Enrofloxacin—the ruthless killer of eukaryotic cells or the last hope in the fight against bacterial infections?[J]. International journal of molecular sciences, 2022, 23(7): 3648.
[3] Mitchell M A. Enrofloxacin[J]. Journal of Exotic Pet Medicine, 2006, 15(1): 66-69.
[4] York D, Withers S S, Watson K D, et al. Enrofloxacin enhances the effects of chemotherapy in canine osteosarcoma cells with mutant and wild‐type p53[J]. Veterinary and comparative oncology, 2017, 15(3): 1087-1100.
[5] Lim S, Hossain M A, Park J, et al. The effects of enrofloxacin on canine tendon cells and chondrocytes proliferation in vitro[J]. Veterinary research communications, 2008, 32(3): 243-253.
[6] Liu B, Cui Y, Brown P B, et al. Cytotoxic effects and apoptosis induction of enrofloxacin in hepatic cell line of grass carp (Ctenopharyngodon idellus)[J]. Fish & Shellfish Immunology, 2015, 47(2): 639-644.
[7] Hetze S, Engel O, Römer C, et al. Superiority of preventive antibiotic treatment compared with standard treatment of poststroke pneumonia in experimental stroke: a bed to bench approach[J]. Journal of Cerebral Blood Flow & Metabolism, 2013, 33(6): 846-854.
[8] Strzępa A, Majewska-Szczepanik M, Lobo F M, et al. Broad spectrum antibiotic enrofloxacin modulates contact sensitivity through gut microbiota in a murine model[J]. Journal of Allergy and Clinical Immunology, 2017, 140(1): 121-133. e3.
Enrofloxacin是一种氟喹诺酮类抗生素，具有广谱抗菌活性，对主要病原菌具有较高的杀菌活性[1]。Enrofloxacin在切割-连接位点与DNA-拓扑异构酶复合物结合，导致酶构象改变，并通过低效的DNA连接来抑制DNA复制[2]。Enrofloxacin已被用于控制牛的乳腺炎、呼吸道和胃肠道细菌感染[3]。
在体外，40µg/ml的Enrofloxacin处理Abrams细胞72小时，显著增加了γH2Ax水平，并导致细胞活力显著下降[4]。200µg/ml的Enrofloxacin处理犬肌腱细胞和软骨细胞4天，诱导了DNA片段化和凋亡细胞核浓缩的特征[5]。200µg/ml的Enrofloxacin处理L8824细胞24小时，诱导了乳酸脱氢酶（LDH）的释放和活性氧（ROS）水平的升高，破坏了线粒体膜电位并促进了细胞死亡[6]。
在体内，每12小时口服10mg/kg剂量的Enrofloxacin，连续7天，显著减轻了大脑中动脉闭塞（MCAo）后小鼠的肺部炎症，提高了小鼠的存活率，并防止了体重下降[7]。每日饮用含0.27mg/ml Enrofloxacin的水，持续2周，显著减轻了小鼠的接触敏感性（CS）症状，改变了肠道菌群的组成，并促进了抗炎反应[8]。