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Mechanism of Antitumor Activity of Gold Glyconanoparticles Against Human Colon Adenocarcinoma Cells

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A possible mechanism of the antitumor activity of gold nanoparticles (GNPs) with a surface modified by carbohydrate residues tropic for tumor cell membrane lectins was studied using human colon adenocarcinoma (Caco-2) cells. Caco-2 cells were incubated for 2 and 8 h with GNP solutions. GNPs reduced the level of SH groups during a 2-hour incubation with the cells by an average of 20 times (p < 0.05); during an 8-hour incubation, by an average of 10 times (p < 0.05). The transmembrane potential of mitochondria was observed to decrease on average up to 58% (p < 0.05) after incubation for 8 h with GNP with a surface modified by fucose and lactose. GNPs modified with fucose residues increased the malondialdehyde (MDA) level by 1.5 times (p < 0.05) and the amount of proapoptotic transcription factor p53, by >2.5 times (p < 0.05) after incubation for 8 h. Thus, GNPs with surfaces modified by fucose, lactose, and galactose residues had a cytotoxic effect on Caco-2 cells, activating lipid peroxidation (Au-Fuc) and possibly initiating one of the apoptosis pathways through stimulation of the transcription factor p53 and decreasing the transmembrane potential of mitochondria.

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Correspondence to I. V. Chernykh.

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Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 57, No. 9, pp. 16 – 20, September, 2023.

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Chernykh, I.V., Kopanitsa, M.A., Shchulkin, A.V. et al. Mechanism of Antitumor Activity of Gold Glyconanoparticles Against Human Colon Adenocarcinoma Cells. Pharm Chem J 57, 1362–1366 (2023). https://doi.org/10.1007/s11094-023-02998-8

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