Chemical modification of fortimicins. IV. Preparation of 4,2'-Di-N-substituted fortimicin B derivatives.
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Biomedical subjects
Publications and source records attributed to K Kitaura.
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The mode of action of nanaomycin A on Gram-positive such as Staphylococcus aureaus, Bacillus cereus and Streptococcus faecalis was investigated. Nanaomycin A inhibited the biosyntheses of protein, DNA, RNA and cell-well peptidoglycan to a similar extent. It increased the oxygenous respiration of S. aureus cells at the minimal inhibitory concentration. The cells preincubated with nanaomycin A showed stimulation of proton influx after addition of N,N'-dicyclo-hexylcazrbodiimide, an inhibitor of Ca++, Mg++-ATPase. Nanaomycin A seems to interfere with the cytoplasmic or to inhibit coupling of oxidative phosphorylation, followed by secondary inhibitory effect on protein, nucleic acids and cell-wall peptidoglycan biosyntheses.
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Acute toxicity of nanaomycin A was tested in mice and rats. It was found that the antibiotic was well absorbed topically so that topical LD50 was approximately the same as intravenous LD50 in mice. The therapeutic effect of nanaomycin A and siccanin against experimental cutaneous Trichophyton mentagrophytes infection in guinea pigs was investigated. Topically applied formulation of nanaomycin A was very effective in improving the condition of lesions and in preventing fungal growth in the infected tissues. Nanaomycin A and siccanin were comparable in activity in experiments.
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A simplified bioassay system for antibiotics has been presented. Glass tubes with open ends and pits are filled with agar medium containing test microbes by immersing vertically into the agar medium while it is warm. These agar tubes are inserted in test solutions and incubated. The growth-inhibitory zones appear in respective tubes due to upward diffusion of the antibiotic. The heights of such zones from the bottom of agar tubes are measured.
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