Next Article in Journal
Next Article in Special Issue
Previous Article in Journal
Previous Article in Special Issue
Mar. Drugs 2013, 11(7), 2574-2594; doi:10.3390/md11072574
Article

APS8, a Polymeric Alkylpyridinium Salt Blocks α7 nAChR and Induces Apoptosis in Non-Small Cell Lung Carcinoma

1,2
, 2
, 2
, 3
, 3
, 4
, 4
, 5
 and 1,*
Received: 9 April 2013; in revised form: 17 June 2013 / Accepted: 25 June 2013 / Published: 16 July 2013
(This article belongs to the Special Issue Marine Compounds and Cancer)
View Full-Text   |   Download PDF [979 KB, uploaded 16 July 2013]
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.
Keywords: 3-alkylpyridinium polymers; apoptosis; nicotine; nicotinic acetylcholine receptor; non-small cell lung carcinoma 3-alkylpyridinium polymers; apoptosis; nicotine; nicotinic acetylcholine receptor; non-small cell lung carcinoma
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Export to BibTeX |
EndNote


MDPI and ACS Style

Zovko, A.; Viktorsson, K.; Lewensohn, R.; Kološa, K.; Filipič, M.; Xing, H.; Kem, W.R.; Paleari, L.; Turk, T. APS8, a Polymeric Alkylpyridinium Salt Blocks α7 nAChR and Induces Apoptosis in Non-Small Cell Lung Carcinoma. Mar. Drugs 2013, 11, 2574-2594.

AMA Style

Zovko A, Viktorsson K, Lewensohn R, Kološa K, Filipič M, Xing H, Kem WR, Paleari L, Turk T. APS8, a Polymeric Alkylpyridinium Salt Blocks α7 nAChR and Induces Apoptosis in Non-Small Cell Lung Carcinoma. Marine Drugs. 2013; 11(7):2574-2594.

Chicago/Turabian Style

Zovko, Ana; Viktorsson, Kristina; Lewensohn, Rolf; Kološa, Katja; Filipič, Metka; Xing, Hong; Kem, William R.; Paleari, Laura; Turk, Tom. 2013. "APS8, a Polymeric Alkylpyridinium Salt Blocks α7 nAChR and Induces Apoptosis in Non-Small Cell Lung Carcinoma." Mar. Drugs 11, no. 7: 2574-2594.



Mar. Drugs EISSN 1660-3397 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert