Study On Antitumor Activity Of Nucleoside N And Mechanism

ObjectiveTo investigate the inhibitory effect of nucleoside N on human cancer cell line in vitro. The antitumor activities of N were examined in order to find effective anticancer agents with low toxicity and provide leading compounds for new drug research and development.Methods1. The cultured JEG-3、HepG2、HL-60cells were treated with different concentrations of N and the cell proliferation was tested by MTT assay.2. The characteristic morphological changes of apoptosis in N (0.1μM、0.2μM) treated HL-60and JEG-3cells for24hours were observed by microscope.3. Western blot was used to detect the expression of several apoptosis related proteins (caspase-3, AKT), after treatment of HL-60cells by N (0.1μM、0.2μM) for24hours.Results1. After JEG-3and HL-60cells were treated with different concentrations of N, dose and time dependent growth inhibition was demonstrated, IC50for48hours were0.3μM、0.15μM respectively.2. N (0.1μM,0.2μM) brought out markedly apoptotic morphological changes on HL-60and JEG-3cell lines.3. The results also showed that apoptosis on HL-60cells induced by N (0.1μM,0.2μM) might correlate with down regulation of AKT expression and activation of caspases-3.ConclusionN can inhibit human cancer cells (JEG-3, HL-60)in vitro in a dose-dependent manner. N can activate caspases-3and downregulate expression of AKT. Our findings may provide new insights for development of antitumor compounds.