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VP-16-ARG complex in lower native drug concentration range (50-300 μM) has lower anticancer activity compared with native VP-16, due to reduced intracellular transport of the more hydrophilic complex as indicated by the cell viability assay and confirmed by cell uptake study. However, at higher drug concentrations (500 μM) the complex's higher anticancer activity is ascribed to the synergistic effect between ARG and VP-16. These data suggest that an optimal ARG concentration can have positive effects with potential benefits for chemother