Moxifloxacin is a fourth-generation, broad-spectrum 8-methoxyfluoroquinolone antibacterial agent. Moxifloxacin inhibits the activity of bacterial DNA topoisomerase II (DNA gyrase) and topoisomerase IV, thereby blocking bacterial DNA replication and transcription processes, ultimately leading to bacterial death. Moxifloxacin can be used in research related to respiratory tract infections, skin and skin structure infections, intra-abdominal infections, and tuberculosis (especially drug-resistant tuberculosis)[1-4].
In vitro, Moxifloxacin (5-50μg/ml) was co-treated with TNF-α (50ng/ml) in cystic fibrosis bronchial epithelial cell lines IB3 and C38 cells for 48 hours. Moxifloxacin significantly inhibited the secretion of IL-8 and IL-6; Moxifloxacin (5-20μg/ml) was co-treated with TNF-α (50ng/ml) in IB3 and C38 cells for 15-60 minutes. Moxifloxacin significantly inhibited the activation of ERK1/2, JNK, and NF-κB[5]. Moxifloxacin (0.05-1mg/ml) was used to treat immortalized human corneal endothelial cells (B4G12 cells) for 24-72 hours. Moxifloxacin induced dose-dependent cytotoxicity, increased reactive oxygen species generation and autophagy, activated caspase 2, 3, 8 pathways and induced apoptosis[6].
In vivo, Moxifloxacin (12.5, 25, 50mg/kg; once daily) was orally administered to Wistar mice for 7 days. Moxifloxacin significantly increased serum creatinine, cholesterol, high-density lipoprotein cholesterol, low-density lipoprotein cholesterol, triglyceride, urea levels and aspartate transaminase, alanine transaminase, alkaline phosphatase activities, while decreasing total bilirubin levels in mice[7]. Moxifloxacin (100mg/kg; twice daily) was intraperitoneally injected into C57BL/6N mice for 2 days. Moxifloxacin significantly reduced the numbers and concentrations of total immune cells, neutrophils, and inflammatory mediators (KC, IL-1β, IL-17A) in the lungs after infection with live or heat-killed bacteria[8].
References:
[1] Balfour JA, Wiseman LR. Moxifloxacin. Drugs. 1999 Mar;57(3):363-73; discussion 374.
[2] Al Omari MM, Jaafari DS, Al-Sou'od KA, Badwan AA. Moxifloxacin hydrochloride. Profiles Drug Subst Excip Relat Methodol. 2014;39:299-431.
[3] Miravitlles M, Anzueto A. Moxifloxacin: a respiratory fluoroquinolone. Expert Opin Pharmacother. 2008 Jul;9(10):1755-72.
[4] Khan F, Ismail M, Khan Q, et al. Moxifloxacin-induced QT interval prolongation and torsades de pointes: a narrative review. Expert Opin Drug Saf. 2018 Oct;17(10):1029-1039.
[5] Blau H, Klein K, Shalit I, et al. Moxifloxacin but not ciprofloxacin or azithromycin selectively inhibits IL-8, IL-6, ERK1/2, JNK, and NF-kappaB activation in a cystic fibrosis epithelial cell line. Am J Physiol Lung Cell Mol Physiol. 2007 Jan;292(1):L343-52.
[6] Park JH, Kim M, Chuck RS, et al. Evaluation of moxifloxacin-induced cytotoxicity on human corneal endothelial cells. Sci Rep. 2021 Mar 18;11(1):6250.
[7] Ukpo GE, Ebuehi OA, Kareem AA. Evaluation of Moxifloxacin-induced Biochemical Changes in Mice. Indian J Pharm Sci. 2012 Sep;74(5):454-7.
[8] Beisswenger C, Honecker A, Kamyschnikow A, et al. Moxifloxacin modulates inflammation during murine pneumonia. Respir Res. 2014 Jul 17;15(1):82.