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Updated: Jan 30, 2026
Electrochemotherapy of Tumours
Published on: December 15, 2008
Anti-Diarrheal Drug Repositioning in Tumour Cell Cytotoxicity
Jihene Elloumi-Mseddi1, Dhouha Msalbi1, Raouia Fakhfakh2
1Laboratory of Molecular and Cellular Screening Processes, Centre of Biotechnology of Sfax, Sidi Mansour Road Km 6, BP 1177, 3018 Sfax, Tunisia.
Background:
Drug repositioning is becoming an ideal strategy to select new anticancer drugs. In particular, drugs treating the side effects of chemotherapy are the best candidates.
Objective:
In this present work, we undertook the evaluation of anti-tumour activity of two anti-diarrheal drugs (nifuroxazide and rifaximin).
Methods:
Anti-proliferative effect against breast cancer cells (MDA-MB-231, MCF-7 and T47D) was assessed by MTT analysis, the Brdu incorporation, mitochondrial permeability and caspase-3 activity.
Results:
Both the drugs displayed cytotoxic effects on MCF-7, T47D and MDA-MB-231 cells. The lowest IC50 values were obtained on MCF-7 cells after 24, 48 and 72 hours of treatment while T47D and MDA-MB-231 were more resistant. The IC50 values on T47D and MDA-MB-231 cells became significantly low after 72 hours of treatment showing a late cytotoxicity effect especially of nifuroxazide but still less important than that of MCF-7 cells. According to the IC50 values, the non-tumour cell line HEK293 seems to be less sensitive to cytotoxicity especially against rifaximin. Both the drugs have shown an accumulation of rhodamine 123 as a function of the rise of their concentrations while the Brdu incorporation decreased. Despite the absence of a significant difference in the cell cycle between the treated and non-treated MCF-7 cells, the caspase-3 activity increased with the drug concentrations rise suggesting an apoptotic effect.
Conclusion:
Nifuroxazide and rifaximin are used to overcome the diarrheal side effect of anticancer drugs. However, they have shown to be anti-tumour drugs which make them potential dual effective drugs against cancer and the side effects of chemotherapy.
Insights
Two anti-diarrheal drugs, nifuroxazide and rifaximin, show potent anticancer activity against breast cancer cells. These findings suggest their potential as dual-action drugs for cancer therapy and chemotherapy side effect management.
Area of Science:
- Oncology
- Pharmacology
- Drug Discovery
Background:
- Drug repositioning is a key strategy for identifying novel anticancer agents.
- Drugs targeting chemotherapy side effects are promising candidates for repositioning.
- Diarrhea is a common chemotherapy side effect, making anti-diarrheal drugs potential anticancer agents.
Purpose of the Study:
- To evaluate the anti-tumor activity of nifuroxazide and rifaximin.
- To assess the cytotoxic and apoptotic effects of these drugs on breast cancer cell lines.
Main Methods:
- MTT assay for anti-proliferative effect.
- Bromodeoxyuridine (BrdU) incorporation assay.
- Mitochondrial permeability assessment using rhodamine 123.
- Caspase-3 activity assay.
Main Results:
- Nifuroxazide and rifaximin exhibited cytotoxic effects on MCF-7, T47D, and MDA-MB-231 breast cancer cells.
- MCF-7 cells were most sensitive, with lower IC50 values compared to T47D and MDA-MB-231 cells.
- Both drugs increased caspase-3 activity, indicating induction of apoptosis, and decreased BrdU incorporation.
Conclusions:
- Nifuroxazide and rifaximin demonstrate significant anti-tumor properties.
- These anti-diarrheal drugs show potential as dual-effective agents against cancer and chemotherapy-induced diarrhea.
- Further investigation into their therapeutic potential in cancer treatment is warranted.
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