Nifuroxazide suppresses the transcription activity of STAT1, STAT3 (IC50 = 3 μM in cells) and STAT5. It is a nitrofuran-based antidiarrheal agent that can prevent urinary tract infections.
Signal transducers and activators of transcription (STATs) are a family of transcription factors essential for the pathogenesis of many cancers. STAT3 in particular has been found to be a critical mediator in the pathogenesis of many tumors. Nifuroxazide is a potent inhibitor of STAT3 through the inhibition of STAT3 tyrosine phosphorylation. Treatment of myeloma cell lines U266 or INA6 cells with nifuroxazide for 48h resulted in a dose-dependent loss of cell viability with an EC50 of approximately 4.5 μM in both cell lines[3]. In animal experiments, intraperitoneal administration of 50 mg/kg/day nifuroxazide inhibited 4T1 (the human breast cancer cell line) tumor growth, blocked formation of pulmonary metastases without detectable toxicity and decreased Ki-67, MMP-9 and increased cleaved caspase-3 expression[4]. Oral administration of nifuroxazide at 25 mg/kg/day to diabetic rats for eight weeks attenuated diabetes induced damage in renal structure, ameliorated oxidative stress, triggered antioxidant defense, educed NF-κB nuclear translocation and cleaved caspase-3 expression and down regulated the activity of apoptotic enzymes (caspase-3/caspase-8/caspase-9) in diabetic kidney[5].
Nifuroxazide 细胞研究
细胞系
浓度
检测类型
检测时间
活动说明
数据源
human U3A cells
Function assay
1 h
Inhibition of STAT3 expressed in human U3A cells after 1 hr by luciferase reporter gene assay, EC50=3 μM
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