Tizoxanide exhibits a broad spectrum of bioactivities, including antimicrobial, antiviral, antiprotozoan, and antitumor properties. It inhibits Giardia lamblia recombinant nitroreductase 1 in Escherichia coli with more than 75% inhibition at 5 μM, and shows activity against Clostridium difficile with MIC50 of 0.06 μg/mL and MIC90 of 0.125 μg/mL. Against Mycobacterium tuberculosis H37Rv, it has a Minimum Inhibitory Concentration (MIC) of 16.0 μg/mL in liquid medium after 7 days. It demonstrates antiviral efficacy against HCV genotypes 1a and 1b with EC50 values ranging from 150.0 nM to 2.0 μM and cytotoxicity in human cells with CC50 values of 14,000.0 nM to 92,000.0 nM, along with high selectivity indices.
It also exhibits potent antiviral activity against HBV with EC50 values of 150.0 nM and 460.0 nM and low toxicity (CC50 > 100,000.0 nM). For HBV-infected HepG2(2.2.15) cells, it inhibits extracellular and intracellular viral DNA with EC90 values of 0.58 μM and 1.2 μM respectively. Against Trichomonas vaginalis, it has an IC50 of 211.0 nM and displays antiprotozoan activity against various pathogens, including Giardia intestinalis and Leishmania mexicana.
The compound shows antimicrobial activity against Mycobacterium tuberculosis in both replicating and non-replicating states with a MIC of 60,380.0 nM, and against Staphylococcus epidermidis with a MIC of 8.0 μg/mL. It has been reported to exert antitumor growth inhibition across multiple human cancer cell lines with GI50 values ranging from 3,000 nM to 40,000 nM.
Additionally, Tizoxanide inhibits IL-6 induced STAT3 transcriptional activity in HEK-Blue IL-6 cells, showing 60% inhibition at 10 μM and an IC50 of 8,900.0 nM, while exhibiting 12.7% cytotoxicity in HeLa cells. In animal models, it has a rapid elimination half-life of 0.7 hours in Sprague-Dawley rats when administered via oral gavage. Furthermore, it demonstrates binding affinity with human plasma proteins at 97.5% and a favorable selectivity index, indicating potential therapeutic applications across various medical conditions..
Note: Summary generated by AI. Data source: ChEMBL 