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Licensed Unlicensed Requires Authentication Published by De Gruyter September 5, 2020

Anticancer effects of novel NSAIDs derivatives on cultured human glioblastoma cells

Özlem Özdemir , Lisa Marinelli , Ivana Cacciatore , Michele Ciulla , Bugrahan Emsen ORCID logo EMAIL logo , Antonio Di Stefano , Adil Mardinoglu and Hasan Turkez

Abstract

Several epidemiologic, clinical and experimental reports indicate that nonsteroidal anti-inflammatory drugs (NSAIDs) could have a potential as anticancer agents. The aim of this study was the evaluation of cytotoxic potential in human glioblastoma cells of novel synthesized NSAID derivatives, obtained by linking, through a spacer, α-lipoic acid (ALA) to anti-inflammatory drugs, such as naproxen (AL-3, 11 and 17), flurbiprofen (AL-6, 13 and 19) and ibuprofen (AL-9, 15 and 21). The effects on the level of gene expression were also determined using quantitative real-time polymerase chain reaction (qRT-PCR) analysis. According to our results, NSAID derivatives exhibited concentration dependent cytotoxic effects on U87-MG cell line when compared with the control group. Moreover, treatment of the most active compounds (AL-3, AL-6 and AL-9) caused upregulation of tumor suppressor gene PTEN and downregulation of some oncogenes such as AKT1, RAF1 and EGFR. In conclusion, our results revealed that AL-3, AL-6 and AL-9 could be suitable candidates for further investigation to develop new pharmacological strategies for the prevention of cancer.


Corresponding author: Bugrahan Emsen, Department of Biology, Kamil Özdağ Faculty of Science, Karamanoğlu Mehmetbey University, Karaman, Turkey, E-mail:

Funding source: Erzurum Technical University

Award Identifier / Grant number: 2015-12

Acknowledgment

This study was supported by Erzurum Technical University with the grant 2015-12.

  1. Author contribution: All the authors have accepted responsibility for the entire content of this submitted manuscript and approved submission.

  2. Research funding: This study was supported by Erzurum Technical University with the grant 2015-12.

  3. Conflict of interest statement: The authors declare no conflicts of interest regarding this article.

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Received: 2020-04-27
Accepted: 2020-08-22
Published Online: 2020-09-05
Published in Print: 2021-07-27

© 2020 Walter de Gruyter GmbH, Berlin/Boston

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