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Anticancer Agents Med Chem. 2018 Feb 28. doi: 10.2174/1871520618666180228152713. [Epub ahead of print]

Riluzole Inhibits Proliferation, Migration and Cell Cycle Progression and Induces Apoptosis in Tumor Cells of Various Origins.

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Institute of Agricultural Medicine. Poland.
Department of Biochemistry and Molecular Biology, Medical University of Lublin, 20-093 Lublin. Poland.
Department of Virology and Immunology, Institute of Microbiology and Biotechnology, Maria Curie-Sklodowska University, 20-033 Lublin. Poland.
Department of Virology and Immunology, Institute of Microbiology and Biotechnology, Maria Curie-Sklodowska University, Akademicka 19, 20-033 Lublin. Poland.
Department of Neurology, University of Wisconsin, 53792 Madison, Wisconsin. United States.


Regardless of contemporary improvements in cancer treatment, the results of drug treatment are not always efficacious. Thus, the development of novel approaches that affect cancer cell-specific metabolic pathways are needed. Since much evidence has shown that tumor cell proliferation and motility are stimulated by glutamate via activation of its receptors, use of antagonists to these receptors may be the key to control cancer cell progression. Riluzole noncompetitive metabotropic glutamate receptor 1 (mGluR1) antagonist, commonly used to treat patients with amyotrophic lateral sclerosis (ALS), has shown some antineoplastic properties against melanoma, breast and prostate cancer. Yet little is known on its molecular mode of action. The current study aims at evaluating the abilities of Riluzole to inhibit proliferation of several cancer cell lines, as well as resolve the mechanism of its action. We demonstrated antiproliferative and antimigrative properties of Riluzole in rhabdomyosarcoma-medulloblastoma, neuroblastoma, astrocytoma, glioma, colon cancer, lung cancer, thyroid carcinoma, leukemia, erythroleukemia and multiple myeloma. Our studies revealed apoptosis induction and G2-Mcell cycle arrest in Riluzole treated A549, C6 and HT-29 cells. At the molecular level, we found that these cells treated with Riluzole had a decrease of Cyclin B and an increase of p21 Waf1/Cip1 and p53 expression. We also observed an enhancement of CDK1 and Chk2 phosphorylation. Reported changes may suggest involvement of these proteins in G2-M arrest, observed in flow cytometry analysis. These data indicated the potential use of Riluzole in the treatment ofdifferent types of cancers.


Migration; Riluzole; Tumor ; Various Origins

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