生物活性 | |||
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描述 | Nalidixic acid sodium salt, a quinolone antibiotic, is effective against both gram-positive and gram-negative bacteria. Nalidixic acid acts in a bacteriostatic manner in lower concentrations and is bactericidal in higher concentrations. Nalidixic acid inhibits a subunit of DNA gyrase and topoisomerase IV and reversibly blocks DNA replication in susceptible bacteria. Nalidixic acid is against with Escherichia coli, Pasteurella spp., Klebsiella pneuiiioniae, Aerobacter aeroyenes, Proteus spp., Salmonella spp., Shigella spp. and Brucella spp. with MIC values of 5.0-12.5 μg/ml, 0.5-2.5 μg/ml, 0.8-25.0 μg/ml, 1.0-25.0 μg/ml, 1.25-30.0 μg/ml, 8-3.2 μg/ml, and 7.5-10.0 μg/ml, respectively. Maximal activity is observed against systemic infections caused by E. coli, A. aerobacter, Proteus mirabilis, Shigella fkxneri, the ED50 values are 25 mg/kg, 60 mg/kg, 50 mg/kg, and 62 mg/kg, respectively. The acute toxicity (LD50) of Nalidixic acid in mice following oral and parenteral administration is: oral, 3300 mg/kg; intravenous, 176 mg/kg; and subcutaneous, 500 mg/kg[3]. The MIC of nalidixic acid was 700 μg/mL against P. aeruginosa. The present findings suggest that the morphology and protein expression of P. aeruginosa is greatly affected by nalidixic acid[4]. Nalidixic acid is metabolized by hydroxylation to 7-hydroxymethylnalidixic acid and then by oxidation to 7-carboxynalidixic acid. The half-lives of the two elimination phases of nalidixic acid are 0.75 and 2.5 h[5]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.93mL 0.79mL 0.39mL |
19.67mL 3.93mL 1.97mL |
39.34mL 7.87mL 3.93mL |
参考文献 |
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[2]Anna Fàbrega, et al. Mechanism of Action of and Resistance to Quinolones. Microb Biotechnol |