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Cytotoxic effect of the serotonergic drug 1-(1-Naphthyl)piperazine against melanoma cells.
- Source :
-
Toxicology in vitro : an international journal published in association with BIBRA [Toxicol In Vitro] 2018 Mar; Vol. 47, pp. 72-78. Date of Electronic Publication: 2017 Nov 16. - Publication Year :
- 2018
-
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 24h 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.<br /> (Copyright © 2017 Elsevier Ltd. All rights reserved.)
- Subjects :
- Cell Line, Tumor
Cell Survival drug effects
Cyclooxygenase 2 chemistry
Cyclooxygenase 2 genetics
Cyclooxygenase 2 metabolism
Drug Resistance, Neoplasm
Enzyme Induction drug effects
Humans
Immunosuppression Therapy
Interleukin-12 Subunit p35 agonists
Interleukin-12 Subunit p35 genetics
Interleukin-12 Subunit p35 metabolism
Melanoma immunology
Melanoma metabolism
Melanoma pathology
Neoplasm Proteins agonists
Neoplasm Proteins antagonists & inhibitors
Neoplasm Proteins genetics
Neoplasm Proteins metabolism
Reactive Oxygen Species agonists
Reactive Oxygen Species metabolism
S Phase drug effects
Serotonin Antagonists pharmacology
p21-Activated Kinases antagonists & inhibitors
p21-Activated Kinases genetics
p21-Activated Kinases metabolism
Antineoplastic Agents pharmacology
Apoptosis drug effects
Gene Expression Regulation, Neoplastic drug effects
Melanoma drug therapy
Oxidative Stress drug effects
Piperazines pharmacology
Serotonin Receptor Agonists pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1879-3177
- Volume :
- 47
- Database :
- MEDLINE
- Journal :
- Toxicology in vitro : an international journal published in association with BIBRA
- Publication Type :
- Academic Journal
- Accession number :
- 29155207
- Full Text :
- https://doi.org/10.1016/j.tiv.2017.11.011