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Attenuation of Nicotine Effects on A549 Lung Cancer Cells by Synthetic α7 nAChR Antagonists APS7-2 and APS8-2.
- Source :
-
Marine drugs [Mar Drugs] 2024 Mar 26; Vol. 22 (4). Date of Electronic Publication: 2024 Mar 26. - Publication Year :
- 2024
-
Abstract
- Nicotine binds to nicotinic acetylcholine receptors (nAChRs) that are overexpressed in different cancer cells, promoting tumor growth and resistance to chemotherapy. In this study, we aimed to investigate the potential of APS7-2 and APS8-2, synthetic analogs of a marine sponge toxin, to inhibit nicotine-mediated effects on A549 human lung cancer cells. Our electrophysiological measurements confirmed that APS7-2 and APS8-2 act as α7 nAChR antagonists. APS8-2 showed no cytotoxicity in A549 cells, while APS7-2 showed concentration-dependent cytotoxicity in A549 cells. The different cytotoxic responses of APS7-2 and APS8-2 emphasize the importance of the chemical structure in determining their cytotoxicity on cancer cells. Nicotine-mediated effects include increased cell viability and proliferation, elevated intracellular calcium levels, and reduced cisplatin-induced cytotoxicity and reactive oxygen species production (ROS) in A549 cells. These effects of nicotine were effectively attenuated by APS8-2, whereas APS7-2 was less effective. Our results suggest that APS8-2 is a promising new therapeutic agent in the chemotherapy of lung cancer.
- Subjects :
- Humans
A549 Cells
Animals
Nicotinic Antagonists pharmacology
Cell Proliferation drug effects
Cisplatin pharmacology
Calcium metabolism
Porifera chemistry
alpha7 Nicotinic Acetylcholine Receptor metabolism
Nicotine pharmacology
Lung Neoplasms drug therapy
Lung Neoplasms pathology
Reactive Oxygen Species metabolism
Antineoplastic Agents pharmacology
Cell Survival drug effects
Subjects
Details
- Language :
- English
- ISSN :
- 1660-3397
- Volume :
- 22
- Issue :
- 4
- Database :
- MEDLINE
- Journal :
- Marine drugs
- Publication Type :
- Academic Journal
- Accession number :
- 38667764
- Full Text :
- https://doi.org/10.3390/md22040147