Antineoplastic mechanisms of niclosamide-loaded nanoparticles in human colorectal cancer cells

Zhirnik A.S.1 , Semochkina Y.P.1, Moskaleva E.Yu.1, Krylov N.I.1, Tubasheva I.A.1, Kuznetsov S.L.1, Vorontsov E.A.1

1. National Research Centre “Kurchatov Institute”, NBICS Centre, Moscow, Russia
Section: Experimental Study
DOI: 10.18097/PBMC20176302132      PubMed Id: 28414284
Year: 2017  Volume: 63  Issue: 2  Pages: 132-138
Using poly(lactic-co-glycolic) acid we developed a polymeric form of niclosamide (PFN) and investigated molecular mechanisms underlying its antitumor activity against human colorectal cancer cell lines (SW837, Caco-2, COLO 320 HSR). PFN was shown to be more cytotoxic against cancer cells and less cytotoxic against normal cells (human embryonic lung fibroblasts) as compared to niclosamide. Both niclosamide and its polymeric form caused mitochondrial damage (evaluated as a decrease in rhodamine 123 accumulation) and increased the levels of reactive oxygen species, particularly mitochondrial superoxide, resulting in the oxidative damage to biomolecules. Furthermore, niclosamide and PFN induced G0/G1 cell cycle arrest.
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Keywords: niclosamide, polymeric form of niclosamide, poly(lactic-co-glycolic) acid, reactive oxygen species, cell cycle, colorectal cancer

Zhirnik, A. S., Semochkina, Y. P., Moskaleva, E. Yu., Krylov, N. I., Tubasheva, I. A., Kuznetsov, S. L., Vorontsov, E. A. (2017). Antineoplastic mechanisms of niclosamide-loaded nanoparticles in human colorectal cancer cells. Biomeditsinskaya Khimiya, 63(2), 132-138.
This paper is also available as the English translation: 10.1134/S1990750817030131
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