Abstract
The MIC90 of temafloxacin (TMFX) against 13 to 50 clinical isolates of Staphylococcus aureus, methicillin-resistant S.aureus (MRSA), coagulase-negative staphylococci (CNS), Streptococcus pyogenes, other β-streptococci, Streptococcus pneumoniae, Enterococcus faecalis, Enterococcus faecium, Escherichia coli (R+), Klebsiella pneumoniae, Proteus mirabilis, Proteus vulgaris, Morganella morganii, Providencia rettgeri, Citrobacter freundii, Enterobacter cloacae, Serratia marcescens, Pseudomonas aeruginosa, Xanthomonas maltophilia, Pseudomonas cepacia, Acinetobacter calcoaceticus, ampicillinresistant Haemophilus influenzae and Bacteroides fragilis was 0.2, 0.78, 0.39, 0.78, 1.56, 1.56, 1.56, 6.25, 1.56, 0.78, 0.78, 0.78, 1.56, 12.5, 3.13, 3.13, 6.25, 6.25, 3.13, 6.25, 0.78, ≤0.013, and 3.13 μg/ml, respectively.
TMFX did not manifest cytostatic activity against cultured CHO-K1 HeLa, or human neuroblastoma IMR32 cells up to 10 μg/ml, and its cytotoxicity was the same as that of ofloxacin (OFLX). Synergy between the bactericidal effect of TMFX and serum complement was not confirmed, although living E.coli NIHJ JC-2 cells were often engulfed and digested in mouse cultured macrophages in the presence of higher than 1/8 MIC of TMFX. TMFX caused the withdrawal of axon-dendrites of redifferentiated neuroblastoma IMR32 cells at a concentration of 5μg/ml, however, its neurotoxicity was as low as that of OFLX.
