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Beta-blockers as potential adjuvants in chemotherapy against melanoma: an in vitro study
1 , 2 , 2 , 3 , * 2
1  Department of Biology, University of Aveiro, 3810-193, Aveiro, Portugal
2  Centre for Environmental and Marine Studies (CESAM), Department of Biology, University of Aveiro, 3810-193 Aveiro, Portugal
3  Department of Medical Sciences, CICECO—Aveiro Institute of Materials, University of Aveiro, 3810-193 Aveiro, Portugal
Academic Editor: Alfredo Berzal-Herranz

Published: 01 November 2023 by MDPI in 9th International Electronic Conference on Medicinal Chemistry session General (registering DOI)

Melanoma is an aggressive type of skin cancer, with the number of cases expected to increase in the future. The available treatments show low efficiency highlighting the need to develop new therapies to increase the survival of the patients. Beta-blockers, drugs already known and used for heart conditions; have shown anti-cancer properties and potential to be valuable in conjugation with chemotherapy. This study aimed to evaluate, in vitro, their potential for cancer treatment. A375 cells (melanoma cell line) were exposed to non-selective blockers (carvedilol and propranolol), β1 selective blockers (atenolol and metoprolol), and antineoplastics drugs (cisplatin and 5- fluorouracil), and viability assessed at 3 timepoints. Selective beta-1 blockers had no significant effects on cell viability. However, the other tested pharmaceuticals affected cell viability allowing the determination of median lethal concentrations (LC50) at 72h and a toxicity ranking: cisplatin (2.46 (1.87 – 3.38), 5-fluorouracil (4.77 (4.48 – 5.07)), carvedilol (16.91 (15.47 - 18.99)) and propranolol (58.03 (57.08 - 59.11)). Carvedilol and cisplatin were, respectively, the most toxic beta-blocker and antineoplastic. Following these results, a combined exposure of beta-blockers and antineoplastics was performed: cisplatin with metoprolol, propranolol, and carvedilol and also paired both non-selective beta-blockers. The results so far support the potential use of non-selective β-blockers as adjuvants of chemotherapy as a melanoma treatment.

Keywords: melanoma; cancer cell lines; beta-blockers; drug repurposing; combined exposure