Selenium nanoparticles loaded with an anticancer molecule offer a new strategy for cancer treatment. In the current study, anisomycin-loaded functionalized selenium nanoparticles (SeNPs@Am) have been made by conjugating anisomycin to the surface of selenium nanoparticles to improve anticancer efficacy. The prepared nanoparticles were fully characterized by transmission electronic microscopy, energy dispersive X-ray spectroscopy, Fourier-transformed infrared spectroscopy, and X-ray photoelectron

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... spectroscopy. The results showed that anisomycin was successfully conjugated with selenium nanoparticles. The size of particles could be effectively regulated through altering the reaction concentrations of sodium selenite and anisomycin. The SeNPs@Am particles (56 nm) exhibited the greatest capacity for cellular uptake. The further study showed that SeNPs@Am entered human hepatocellular carcinoma HepG2 cells in a dose or time-dependent manner via macropinocytosis and clathrin-mediated endocytosis pathways. SeNPs@Am significantly inhibited HepG2 cell proliferation with the low cytotoxicity against normal cells, and dramatically precluded the aggression and migration of HepG2 cells. It also arrested the cell cycle progression at the G0/G1 phase through the activation of the cyclin-dependent kinase inhibitors with inhibition of CDK-2 and ICBP90, and induced the cell apoptosis through activating the caspase cascade signaling in HepG2 cells, markedly superior to anisomycin alone. The findings indicate that SeNPs@Am may be a promising drug for hepatocellular carcinoma.