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合成 α7 nAChR 拮抗剂 APS7-2 和 APS8-2 对 A549 肺癌细胞中尼古丁作用的衰减。

Attenuation of Nicotine Effects on A549 Lung Cancer Cells by Synthetic α7 nAChR Antagonists APS7-2 and APS8-2.

机构信息

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Ljubljana, 1000 Ljubljana, Slovenia.

Department of Biology, Biotechnical Faculty, University of Ljubljana, 1000 Ljubljana, Slovenia.

出版信息

Mar Drugs. 2024 Mar 26;22(4):147. doi: 10.3390/md22040147.

DOI:10.3390/md22040147
PMID:38667764
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11051029/
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.

摘要

尼古丁与在不同癌细胞中过度表达的烟碱型乙酰胆碱受体（nAChRs）结合，促进肿瘤生长和对化疗的耐药性。在这项研究中，我们旨在研究 APS7-2 和 APS8-2（一种海洋海绵毒素的合成类似物）抑制尼古丁对 A549 人肺癌细胞的影响的潜力。我们的电生理测量证实 APS7-2 和 APS8-2 作为 α7 nAChR 拮抗剂发挥作用。APS8-2 在 A549 细胞中没有细胞毒性，而 APS7-2 在 A549 细胞中表现出浓度依赖性细胞毒性。APS7-2 和 APS8-2 的不同细胞毒性反应强调了化学结构在确定其对癌细胞的细胞毒性方面的重要性。尼古丁介导的作用包括增加细胞活力和增殖、提高细胞内钙水平以及降低 A549 细胞中顺铂诱导的细胞毒性和活性氧物质（ROS）产生。APS8-2 有效地减弱了这些尼古丁的作用，而 APS7-2 的效果较差。我们的结果表明，APS8-2 是肺癌化疗中有前途的新治疗剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5435/11051029/287c091d1b2f/marinedrugs-22-00147-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5435/11051029/41cb27e62ebc/marinedrugs-22-00147-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5435/11051029/82163b4c46be/marinedrugs-22-00147-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5435/11051029/847ddf3d3267/marinedrugs-22-00147-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5435/11051029/6cf6e71bd1f4/marinedrugs-22-00147-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5435/11051029/1305436b3074/marinedrugs-22-00147-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5435/11051029/d1db728c046e/marinedrugs-22-00147-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5435/11051029/287c091d1b2f/marinedrugs-22-00147-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5435/11051029/41cb27e62ebc/marinedrugs-22-00147-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5435/11051029/82163b4c46be/marinedrugs-22-00147-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5435/11051029/847ddf3d3267/marinedrugs-22-00147-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5435/11051029/6cf6e71bd1f4/marinedrugs-22-00147-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5435/11051029/1305436b3074/marinedrugs-22-00147-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5435/11051029/d1db728c046e/marinedrugs-22-00147-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5435/11051029/287c091d1b2f/marinedrugs-22-00147-g007.jpg

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