生物活性 | |||
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描述 | Nitroxoline is an antibiotic that has proven to be very effective at combating biofilm infections. Nitroxoline is currently repurposed for the treatment of urinary tract infection, which active against susceptible gram-positive and gram-negative organisms commonly found in urinary tract infection. Nitroxoline showed a broad antimicrobial spectrum, with inhibition zone diameters and MICs of nitroxoline well below the EUCAST breakpoint for E. coli for most organisms (≤16mg/ml). Nitroxoline is active against the bacteria E. coli, S. aureus, E. faecalis, K. pneumoniae, and P. mirabilis in vitro (MIC90s = 4, 4, 8, 8, and 8 mg/L, respectively)[3]. Nitroxoline inhibits the growth of human U87 and U251 glioma, A549 lung, and PC3 prostate cancer cells (IC50s = 50, 6, 38, and 23 μg/ml, respectively)[4]. In vivo, it reduces tumor growth in a PTEN- and KRAS-driven glioma mouse model when administered at a dose of 80 mg/kg per day. Nitroxoline also inhibits the interaction between the first bromodomain of bromodomain-containing protein 4 (BRD4) with acetylated histone H4 with an IC50 value of 0.98 μM[5]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
5.26mL 1.05mL 0.53mL |
26.29mL 5.26mL 2.63mL |
52.59mL 10.52mL 5.26mL |
参考文献 |
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