In comparison with ciprofloxacin, levofloxacin and moxifloxacin, antimicrobial activity of nemonoxacin against ciprofloxacin-susceptible/-resistant methicillin-susceptible Staphylococcus aureus (MSSA) and methicillin-resistant Staphylococcus aureus (MRSA) was determined with the availability to select resistant mutants evaluated. Minimum inhibitory concentrations and mutant prevention concentrations of quinolones were determined by agar dilution method, that concentrated bacterial cells were spread onto Mueller–Hinton agar plates containing antibacterials at different concentrations. Selection index (SI) was calculated. Minimum inhibitory concentration and mutant prevention concentration of nemonoxacin were 0.063 and 0.25 μg/mL for ciprofloxacin-susceptible MSSA and those were 0.5 and 4.0 μg/mL for ciprofloxacin-resistant MSSA, lower than observations of three fluoroquinolones distinctly. SI of nemonoxacin and moxifloxacin were similar, with narrower mutant selective window than levofloxacin and ciprofloxacin. Minimum inhibitory concentration and mutant prevention concentration of nemonoxacin were 0.25 and 2.0 μg/mL for ciprofloxacin-susceptible MRSA, which were 0.5 and 16.0 μg/mL for ciprofloxacin-resistant MRSA. Values were lower than those determined from fluoroquinolones. Nemonoxacin presents good antimicrobial activity against clinical isolates of S. aureus, especially for ciprofloxacin-resistant strains. But stepwise mutant accumulation of ciprofloxacin-resistant MRSA can be hardly inhibited by nemonoxacin with pharmacokinetic parameters considered.
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Adam HJ, Laing NM, King CR, Lulashnyk B, Hoban DJ, Zhanel GG (2009) In vitro activity of nemonoxacin, a novel non-fluorinated quinolone, against 2,440 clinical isolates. Antimicrob Agents Chemother 53:4915–4920
Arjona A (2009) Nemonoxacin: quinolone antibiotic. Drug Future 34:196–203
Black MT, Stachyra T, Platel D et al (2008) Mechanism of action of the antibiotic NXL101, a novel nonfluoroquinolone inhibitor of bacterial type II topoisomerases. Antimicrob Agents Chemother 52:3339–3349
Bradbury BJ, Pucci MJ (2008) Recent advances in bacterial topoisomerase inhibitors. Curr Opin Pharmacol 8:574–581
Chen S, Cui S, McDermott PF et al (2007) Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica Serovar Typhimurium to fluoroquinolones and other antimicrobials. Antimicrob Agents Chemother 51:535–542
Chen YH, Liu CY, Lu JJ, King CHR, Hsueh PR (2009) In vitro activity of nemonoxacin (TG-873870), a novel non-fluorinated quinolone, against clinical isolates of Staphylococcus aureus, enterococci and Streptococcus pneumoniae with various resistance phenotypes in Taiwan. J Antimicrob Chemother 64:1226–1229
Chung DT, Tsai CY, Chen SJ et al (2010) Multiple-dose safety, tolerability, and pharmacokinetics of oral nemonoxacin (TG-873870) in healthy volunteers. Antimicrob Agents Chemother 54:411–417
Dong Y, Zhao X, Domagala J, Drlica K (1999) Effect of fluoroquinolone concentration on selection of resistant mutants of Mycobacterium bovis BCG and Staphylococcus aureus. Antimicrob Agents Chemother 43:1756–1758
Drlica K (2003) The mutant selection window and antimicrobial resistance. J Antimicrob Chemother 52:11–17
Drlica K, Zhao X, Blondeau JM, Hesje C (2006) Low correlation between minimal inhibitory concentration (MIC) and mutant prevention concentration (MPC). Antimicrob Agents Chemother 50:403–404
Giraud E, Baucheron S, Cloeckaert A (2006) Resistance to fluoroquinolones in Salmonella: emerging mechanisms and resistance prevention strategies. Microbes Infect 8:1937–1944
Gould IM, David MZ, Esposito S et al (2012) New insights into meticillin-resistant Staphylococcus aureus (MRSA) pathogenesis, treatment and resistance. Int J Antimicrob Agents 39:96–104
Hsu MS, Liao CH, Liu CY, Yang CJ, Huang YT, Hsueh PR (2011) In vitro susceptibilities of clinical isolates of ertapenem-non-susceptible Enterobacteriaceae to nemonoxacin, tigecycline, fosfomycin and other antimicrobial agents. Int J Antimicrob Agents 37:276–278
Kontou P, Manika K, Chatzika K et al (2013) Pharmacokinetics of moxifloxacin and high-dose levofloxacin in severe lower respiratory tract infections. Int J Antimicrob Agents 42:262–267
Lai CC, Tan CK, Lin SH et al (2009) Comparative in vitro activities of nemonoxacin, doripenem, tigecycline and 16 other antimicrobials against Nocardia brasiliensis, Nocardia asteroides and unusual Nocardia species. J Antimicrob Chemother 64:73–78
Lai CC, Liu WL, Ko WC et al (2011) Multicenter study in Taiwan of the in vitro activities of nemonoxacin, tigecycline, doripenem, and other antimicrobial agents against clinical isolates of various nocardia species. Antimicrob Agents Chemother 55:2084–2091
Lauderdale TL, Shiau YR, Lai JF, Chen HC, King CHR (2010) Comparative in vitro activities of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, and other quinolones against clinical isolates. Antimicrob Agents Chemother 54:1338–1342
Li CR, Li Y, Li GQ et al (2010) In vivo antibacterial activity of nemonoxacin, a novel non-fluorinated quinolone. J Antimicrob Chemother dkq341
Odenholt I, Löwdin E, Cars O (2003) Postantibiotic, postantibiotic sub-MIC, and subinhibitory effects of PGE-9509924, ciprofloxacin, and levofloxacin. Antimicrob Agents Chemother 47:3352–3356
Paphitou NI (2013) Antimicrobial resistance: action to combat the rising microbial challenges. Int J Antimicrob Agents 42(Suppl 1):S25–S28
Stass H, Dalhoff A, Kubitza D, Schühly U (1998) Pharmacokinetics, safety, and tolerability of ascending single doses of moxifloxacin, a new 8-methoxy quinolone, administered to healthy subject. Antimicrob Agents Chemother 42:2060–2065
Tan CK, Lai CC, Liao CH et al (2009) Comparative in vitro activities of the new quinolone nemonoxacin (TG-873870), gemifloxacin and other quinolones against clinical isolates of Mycobacterium tuberculosis. J Antimicrob Chemother 64:428–429
Tang X, Huang Y, Wen Q, Liu Z (2005) Bioequivalence of ciprofloxacin tablets in healthy volunteers. Chin Pharmacol Bull 21:1116–1119 (in Chinese)
Theuretzbacher U (2011) Resistance drives antibacterial drug development. Curr Opin Pharmacol 11:433–438
Trucksis M, Hooper DC, Wolfson JS (1991) Emerging resistance to fluoroquinolones in staphylococci: an alert. Ann Intern Med 114:424–426
Turkmani A, Psaroulaki A, Christidou A, Chochlakis D, Tabaa D, Tselentis Y (2008) In vitro-selected resistance to fluoroquinolones in two Brucella strains associated with mutational changes in gyrA. Int J Antimicrob Agents 32:227–232
van Rensburg DJ, Perng RP, Mitha IH et al (2010) Efficacy and safety of nemonoxacin versus levofloxacin for community-acquired pneumonia. Antimicrob Agents Chemother 54:4098–4106
Zhang L, Li J, Lv Y et al (2001) Pharmacokinetic study of levofloxacin in Chinese healthy volunteers. Chin Pharm J 36:834–837 (in Chinese)
Zhao X, Drlica K (2001) Restricting the selection of antibiotic -resistant mutant bacteria: a general strategy derived from fluoroquinolone studies. Clin Infect Dis 33(Suppl3):S147–S156
Zhao X, Eisner W, Perl-Rosenthal N, Kreiswirth B, Drlica K (2003) Mutant prevention concentration of garenoxacin (BMS-284756) for ciprofloxacin-susceptible or -resistant Staphylococcus aureus. Antimicrob Agents Chemother 47:1023–1027
Zhou J, Dong Y, Zhao X et al (2000) Selection of antibiotic resistance: allelic diversity among fluoroquinolone-resistant mutations. J Infect Dis 182:517–525
The authors showed great gratitude to the staff from Department of Respiratory Diseases, People’s Liberation Army General Hospital and Department of Respiratory Diseases, Second Artillery General Hospital.
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Li, Z., Liu, Y., Wang, R. et al. Antibacterial activities of nemonoxacin against clinical isolates of Staphylococcus aureus: an in vitro comparison with three fluoroquinolones. World J Microbiol Biotechnol 30, 2927–2932 (2014). https://doi.org/10.1007/s11274-014-1720-2
- Methicillin-susceptible Staphylococcus aureus
- Methicillin-resistant Staphylococcus aureus
- Mutant prevention concentration