20.500.12556/RUL-155641 Attenuation of Nicotine Effects on A549 Lung Cancer Cells by Synthetic α7 nAChR Antagonists APS7-2 and APS8-2 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. marine toxin nicotinic acetylcholine receptor nAChR antagonist APS7-2 APS8-2 rak (medicina) toksičnost morski toksini nikotinski acetilholinski receptor antagonist nAChR APS7-2 APS8-2 true false true Angleški jezik Slovenski jezik Članek v reviji 2024-04-09 13:11:27 2024-04-09 13:11:31 2024-04-11 03:16:07 0000-00-00 00:00:00 2024 0 0 14 str. iss. 4 Vol. 22 2024 0000-00-00 Zaloznikova Objavljeno NiDoloceno 0000-00-00 0000-00-00 0000-00-00 615.9:616.24-006 1660-3397 10.3390/md22040147 190758147 marinedrugs-22-00147-v2.pdf marinedrugs-22-00147-v2.pdf 1 63E69A5A08CEF6DE779A2314CF654EC8 553afb1bcdcbf7ea5e2c5c8122100f7938338c3cb583d801bab09c5300909631 e25b384a-f662-11ee-be47-0050569b8976 https://repozitorij.uni-lj.si/Dokument.php?lang=slv&id=182644 https://www.mdpi.com/1660-3397/22/4/147 1 ec674985-f661-11ee-be47-0050569b8976 https://repozitorij.uni-lj.si/Dokument.php?lang=slv&id=182643 Fakulteta za farmacijo Biotehniška fakulteta 0 0 0