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Repurposing of Loperamide as a New Drug With Anticancer Activity for Human Osteosarcoma
Laura Roncuzzi1, Francesca Perut2, Nicola Baldini2,3
1Biomedical Science and Technology and Nanobiotechnology Laboratory, IRCCS Istituto Ortopedico Rizzoli, Bologna, Italy; laura.roncuzzi@ior.it.
Background/Aim:
Osteosarcoma is an aggressive malignant bone tumor, with unfavorable outcomes in patients with metastatic and recurrent disease. To improve patient survival new treatment options are needed. By using the drug repurposing approach, which takes advantage of already approved drugs with non-oncology primary use, we investigated the activity of loperamide, a peripheral opiate receptor agonist, a drug widely used in clinical practice to treat acute non-specific and chronic diarrhea, on human osteosarcoma.
Materials And Methods:
Human osteosarcoma cell lines (143B, Saos-2, HOS and MG-63) and multidrug-resistant MG-63DXR30 cells were treated with loperamide. Proliferation and cell viability were determined by viable cell count and acid phosphatase assay. Loperamide activity on cell cycle and apoptosis induction were evaluated by flow cytometry and a luminescence assay testing caspase 3/7 activity, respectively.
Results:
Loperamide significantly inhibited cell proliferation, through alteration of cell cycle profile at G0/G1 phase and apoptotic death in human osteosarcoma cells. Furthermore, loperamide significantly inhibited the growth of multidrug-resistant osteosarcoma cells.
Conclusion:
Our findings provide new perspectives for loperamide and its therapeutic repositioning for the treatment of osteosarcoma.
Insights
Loperamide, commonly used for diarrhea, shows promise in treating osteosarcoma. This drug effectively inhibited osteosarcoma cell growth and induced cell death, offering new therapeutic possibilities for this aggressive bone cancer.
Area of Science:
- Oncology
- Pharmacology
- Drug Repurposing
Background:
- Osteosarcoma is an aggressive bone cancer with poor outcomes, especially in metastatic or recurrent cases.
- New therapeutic strategies are crucial to improve patient survival rates.
- Drug repurposing offers a viable approach by investigating existing drugs for novel applications.
Purpose of the Study:
- To evaluate the anti-cancer activity of loperamide, an anti-diarrheal drug, against human osteosarcoma.
- To explore the potential of loperamide as a repositioned therapeutic agent for osteosarcoma treatment.
Main Methods:
- Human osteosarcoma cell lines and multidrug-resistant cells were treated with loperamide.
- Cell proliferation, viability, cell cycle, and apoptosis were assessed using cell counting, acid phosphatase assay, flow cytometry, and caspase activity assays.
Main Results:
- Loperamide significantly inhibited osteosarcoma cell proliferation and viability.
- The drug induced cell cycle arrest at the G0/G1 phase and promoted apoptosis.
- Loperamide demonstrated efficacy against multidrug-resistant osteosarcoma cells.
Conclusions:
- Loperamide exhibits significant anti-osteosarcoma activity.
- These findings support the therapeutic repositioning of loperamide for osteosarcoma treatment.
- Loperamide presents a promising new avenue for osteosarcoma therapy.
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