Peptide Amphiphiles (PAs) have been known as promising tools in drug and gene delivery systems due to their biocompatibility and bioactivity. A series of four PAs containing arginine and lysine residues linked to one or two hydrophobic tails with different chain lengths (i.e., (NH(Ac)-Lys(Palm)-Arg-Lys(Palm)-COOH), (NH(Ac)-Lys(My)-Arg-Lys(My)-COOH), (NH(Ac)-Arg-Lys(Palm)-Arg-COOH), and (NH(Ac)-Arg-Lys(My)-Arg-COOH), where My and Palm are myristoyl and palmitoyl, respectively) were synthesized using solid-phase Fmoc chemistry. All synthesized PAs did not show significant toxicity in human ovarian cancer (SK-OV-3), human leukemia cancer (CCRF-CEM), and human colorectal (HCT-116) cells. The cellular uptake of fluorescent-labeled phosphopeptide F-GpYEEI was evaluated in the presence or absence of all synthesized PAs in human ovarian cancer cells (SK-OV-3) after 1 h incubation using flow cytometry (FACS). (NH(Ac)-Lys(Palm)-Arg-Lys(Palm)-COOH) was found to be more efficient transporter compared to the other synthesized PAs. The cellular uptake of F-GpYEEI was improved (3 folds) in the presence of this PA.

Peptide amphiphiles as new transporters for the delivery of phosphopeptides

245th National Meeting (2013)

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