Development of a novel,multifunctional, membrane-interactive pyridinium salt with potent anticancer activity |
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| Affiliation: | 1. School of Pharmacy and Biomedical Sciences, University of Central Lancashire, Maudland Building, Preston, Lancashire PR1 2HE, UK;2. Brain Tumour Research Centre, University of Wolverhampton, Wulfruna Street, Wolverhampton WV1 1LY, UK;1. A.E. Favorsky Irkutsk Institute of Chemistry, Siberian Branch of the Russian Academy of Sciences, 1 Favorsky Street, 664033 Irkutsk, Russia;2. East-Siberian State Academy of Education, 6 Niznyaya Nabereznaya, 664011 Irkutsk, Russia;3. L.V. Kirensky Institute of Physics, Siberian Branch of the Russian Academy of Sciences, Akademgorodok, 660036 Krasnoyarsk, Russia;1. Molecular Probe Program, Molecular Imaging Center, National Institute of Radiological Sciences, 4-9-1 Anagawa, Inage-ku, Chiba 263-8555, Japan;2. SHI Accelerator Service Co. Ltd, 5-9-11 Kitashinagawa, Shinagawa-ku, Tokyo 141-8686, Japan;1. Laboratoire Physico-chimie de l’Etat Solide, Département de Chimie, Faculté des Sciences de Sfax, B.P. 1171, 3000 Sfax, Université de Sfax, Tunisia;2. Laboratory of Plant Biotechnology, Faculty of Sciences of Sfax, 3000 Sfax, Tunisia;1. Department of Chemistry, Simon Fraser University, Burnaby, BC V5A 1S6, Canada;2. Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), S.A.S. Nagar, Punjab 160062, India;3. Department of Chemistry, University of Saskatchewan, 110 Science Place, Saskatoon, Saskatchewan S7N 5C9, Canada;1. School of Pharmacy, Xuzhou Medical College, Xuzhou 221004, People’s Republic of China;2. State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, People’s Republic of China;3. Department of Environmental Pharmacy, Tianjin Institute of Health and Environmental Medicine, Tianjin 300050, People’s Republic of China |
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| Abstract: | The synthesis and biological evaluation of a novel pyridinium salt is reported. Initial membrane interaction with isolated phospholipid monolayers was obtained with the pyridinium salt, and two neutral analogues for comparison, and the anticancer effects of the best compound established using a cytotoxicity screening assay against glioma cells using both an established cell line and three short-term cell cultures—one of which has been largely resistant to all chemotherapeutic drugs tested to date. The results indicate that the pyridinium salt exhibits potent anticancer activity (EC50s = 9.8–312.5 μM) on all cell types, including the resistant one, for a continuous treatment of 72 h. Microscopic examination of the treated cells using a trypan blue exclusion assay showed membrane lysis had occurred. Therefore, this letter highlights the potential for a new class of pyridinium salt to be developed as a much needed alternative treatment for glioma chemotherapy. |
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| Keywords: | Pyridinium salts Anticancer Glioma Amide Biocidal |
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