Title: | APS8, a polymeric alkylpyridinium salt blocks [alpha]7 nAChR and induces apoptosis in non-small cell lung carcinoma |
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Authors: | ID Zovko, Ana (Author) ID Viktorsson, Kristina (Author) ID Lewensohn, Rolf (Author) ID Kološa, Katja (Author) ID Filipič, Metka (Author) ID Xing, Hong (Author) ID Kem, William R. (Author) ID Paleari, Laura (Author) ID Turk, Tom (Author) |
Files: | URL - Source URL, visit http://www.mdpi.com/1660-3397/11/7/2574
PDF - Presentation file, download (973,49 KB) MD5: 1933F4A3AE898A003AAF96BFBE7EF34B
URL - Source URL, visit https://doi.org/10.3390/md11072574
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Language: | English |
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Typology: | 1.01 - Original Scientific Article |
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Organization: | NIB - National Institute of Biology
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Abstract: | Naturally occurring 3-alkylpyridinium polymers (poly-APS) from the marine sponge Reniera sarai, consisting of monomers containing polar pyridinium and nonpolar alkyl chain moieties, have been demonstrated to exert a wide range of biological activities, including a selective cytotoxicity against non-small cell lung cancer (NSCLC) cells. APS8, an analog of poly-APS with defined alkyl chain length and molecular size, non-competitively inhibits α7 nicotinic acetylcholine receptors (nAChRs) at nanomolar concentrations that are too low to be acetylcholinesterase (AChE) inhibitory or generally cytotoxic. In the present study we show that APS8 inhibits NSCLC tumor cell growth and activates apoptotic pathways. APS8 was not toxic for normal lung fibroblasts. Furthermore, in NSCLC cells, APS8 reduced the adverse anti-apoptotic, proliferative effects of nicotine. Our results suggest that APS8 or similar compounds might be considered as lead compounds to develop antitumor therapeutic agents for at least certain types of lung cancer. |
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Keywords: | 3-alkylpyridinium polymers, apoptosis, nicotine, nicotinic acetylcholine receptor, non-small cell lung carcinoma |
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Publication status: | Published |
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Publication version: | Version of Record |
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Publication date: | 16.07.2013 |
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Year of publishing: | 2013 |
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Number of pages: | str. 2574-2594 |
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Numbering: | Vol. 11, no. 7 |
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PID: | 20.500.12556/DiRROS-20018 |
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UDC: | 577.1 |
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ISSN on article: | 1660-3397 |
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DOI: | 10.3390/md11072574 |
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COBISS.SI-ID: | 2854223 |
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Note: | Nasl. z nasl. zaslona;
Opis vira z dne 20. 8. 2013;
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Publication date in DiRROS: | 02.08.2024 |
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Views: | 311 |
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Downloads: | 243 |
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