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/硝呋齐特 细胞实验
Cell Line
Concentration
Treated Time
Description
References
HepG2 cells
0, 0.3125, 0.625, 1.25, 2.5, 5, 10, 20, 40 μg/mL
24 or 48 hours
To evaluate the effect of Nifuroxazide on HCC cell proliferation, migration, and apoptosis, results showed that Nifuroxazide significantly inhibited cell proliferation and migration while increasing apoptosis.
Elife. 2024 Mar 5;12:RP90911.
Huh7 cells
0, 0.3125, 0.625, 1.25, 2.5, 5, 10, 20, 40 μg/mL
24 or 48 hours
To evaluate the effect of Nifuroxazide on HCC cell proliferation, migration, and apoptosis, results showed that Nifuroxazide significantly inhibited cell proliferation and migration while increasing apoptosis.
Elife. 2024 Mar 5;12:RP90911.
4T1 cells
0-20 µM
24, 48, 72 hours
To evaluate the effect of Nifuroxazide on the viability of breast cancer cells, results showed that Nifuroxazide inhibited breast cancer cell viability in a concentration- and time-dependent manner.
Cell Death Dis. 2015 Mar 26;6(3):e1701.
MCF-7 cells
0-20 µM
24, 48, 72 hours
To evaluate the effect of Nifuroxazide on the viability of breast cancer cells, results showed that Nifuroxazide inhibited breast cancer cell viability in a concentration- and time-dependent manner.
Cell Death Dis. 2015 Mar 26;6(3):e1701.
MDA-MB-231 cells
0-20 µM
24, 48, 72 hours
To evaluate the effect of Nifuroxazide on the viability of breast cancer cells, results showed that Nifuroxazide inhibited breast cancer cell viability in a concentration- and time-dependent manner.
Cell Death Dis. 2015 Mar 26;6(3):e1701.
MDA-MB-231 cells
0-20 µM
3 days
To evaluate the inhibitory effect of Nifuroxazide combined with Palbociclib on cell proliferation, the results showed that the combination significantly inhibited cell proliferation.
Cell Death Discov. 2023 Sep 26;9(1):355.
4T1 cells
0-20 µM
3 days
To evaluate the inhibitory effect of Nifuroxazide combined with Palbociclib on cell proliferation, the results showed that the combination significantly inhibited cell proliferation.
Cell Death Discov. 2023 Sep 26;9(1):355.
Nifuroxazide/硝呋齐特 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
C57BL/6 mice
H22 tumor-bearing mouse model
IntratumOral injection
200 μg/mouse
Once daily for 7 days
To evaluate the anti-tumor effect of Nifuroxazide combined with radiotherapy in H22-bearing mice, results showed that the combination therapy significantly inhibited tumor growth, prolonged survival, and enhanced T lymphocyte activation and M1 macrophage polarization.
Elife. 2024 Mar 5;12:RP90911.
Mice
Acute graft-versus-host disease (aGvHD) model
Intraperitoneal injection
200 μg/mouse
Once daily for one week
Combination with SAT05f significantly decreased the severity of aGvHD and prolonged the survival rate, reduced the activation of CD4+ effector T cells, increased Treg cells, and inhibited cytokine release.
Cell Death Dis. 2016 Dec 1;7(12):e2507
Balb/C mice
Lung metastasis model and abdominal metastasis model
Oral
25 mg/kg and 50 mg/kg
Once daily for 6 days
Nifuroxazide significantly reduced tumor metastasis in lung and abdominal metastasis models
Cell Death Dis. 2017 Jan 5;8(1):e2534
Balb/c mice
4T1 tumor model
Intraperitoneal injection
25 mg/kg/d or 50 mg/kg/d
Daily for 21 days
To evaluate the inhibitory effect of Nifuroxazide combined with Palbociclib on tumor growth and lung metastasis, the results showed that the combination significantly inhibited tumor growth and lung metastasis.
Cell Death Discov. 2023 Sep 26;9(1):355.
BALB/c mice
4T1 tumor model
Intraperitoneal injection
50 mg/kg/day
Once daily for 24 days
To evaluate the effect of Nifuroxazide on 4T1 tumor growth and pulmonary metastasis, results showed that Nifuroxazide significantly inhibited tumor growth and pulmonary metastasis without detectable toxicity.
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