Cytotoxic effect of the serotonergic drug 1-(1-Naphthyl)piperazine against melanoma cells

authors	Menezes, AC; Carvalheiro, M; de Oliveira, JMPF; Ascenso, A; Oliveira, H
nationality	International
journal	TOXICOLOGY IN VITRO
author keywords	Melanoma skin cancer; Antitumor agents; 1-(1-Naphthyl)piperazine; Apoptosis; Oxidative stress
keywords	CIS-UROCANIC ACID; DNA-DAMAGE; IMMUNE SUPPRESSION; CANCER-CELLS; LUNG-CANCER; APOPTOSIS; PHOTOCARCINOGENESIS; RECEPTOR; ASSAY; SKIN
abstract	1-(1-Naphthyl)piperazine (1-NPZ) is a serotonergic derivative of quipazine acting both as antagonist and agonist of different serotonin receptors, with promising results for the management of skin cancer. In this work, we studied the effect of 1-NPZ on human MNT-1 melanoma cells by evaluating its effects on cell viability, ability to form colonies, cell cycle dynamics, reactive oxygen species (ROS) production and apoptosis. Treatment of MNT-1 cells with 1-NPZ for 24 h decreased cell viability and induced apoptosis in a dose-dependent manner. Activity against melanoma was confirmed with a different melanoma cell line, SK-MEL-28. Simultaneously, 1-NPZ affected cell cycle progression by mediating a S-phase delay. Higher levels of ROS were also detected in MNT-1 cells after treatment with 1-NPZ. Furthermore, 1-NPZ significantly increased the expression of cyclooxygenase-2 in MNT-1 cells. These findings suggest that 1-NPZ pretreatment is able to induce oxidative stress, and consequently apoptotic cell death in melanoma cells. In conclusion, this study demonstrates the cytotoxic and genotoxic potential of 1-NPZ against melanoma cells.
publisher	PERGAMON-ELSEVIER SCIENCE LTD
issn	0887-2333
year published	2018
volume	47
beginning page	72
ending page	78
digital object identifier (doi)	10.1016/j.tiv.2017.11.011
web of science category	Toxicology
subject category	Toxicology
unique article identifier	WOS:000426409400008