Nitroxoline

Nitroxoline is an 8-hydroxyquinoline that has diverse biological activities, including antibacterial, antiproliferative, and bromodomain interaction-inhibiting properties.^1,2,3,4 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).¹ It also inhibits biofilm formation of certain strains of multidrug-resistant (MDR) A. baumannii and P. aeruginosa, as well as methicillin-resistant S. aureus (MRSA) and S. epidermidis (MRSE) with minimum biofilm eradication concentration (MBEC) values of 46.9, 1,500, 188, and 125 μM, respectively.² 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).³ 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.⁴

WARNING This product is not for human or veterinary use.

1. Sobke, A., Makarewicz, O., Baier, M., et al. Empirical treatment of lower urinary tract infections in the face of spreading multidrug resistance: In vitro study on the effectiveness of nitroxoline. Int. J. Antimicrob. Agents 51(2), 213-220 (2018).

2. Abouelhassan, Y., Yang, Q., Yousaf, H., et al. Nitroxoline: A broad-spectrum biofilm-eradicating agent against pathogenic bacteria. Int. J. Antimicrob. Agents 49(2), 247-251 (2017).

3. lazovic, J., Guo, L., Nakashima, J., et al. Nitroxoline induces apoptosis and slows glioma growth in vivo. Neuro. Oncol. 17(1), 53-62 (2015).

4. Jiang, H., Xing, J., Wang, C., et al. Discovery of novel BET inhibitors by drug repurposing of nitroxoline and its analogues. Org. Biomol. Chem. 15(44), 9352-9361 (2017).