Abstract

The influence of Tat-derived peptide (Tat-LK15) on the uptake of membrane p- glycoproteins substrate (Calcein AM)

Highlights

  • Cell penetrating peptides (CPPs) have been used in many areas of drug delivery for mediating the delivery of peptides, protein, DNA, siRNA and liposomes

  • MRP3) 4 (Riganti et al 2005), and K562dx sublines were assessed by flow cytometry: Calcein AM (Ca AM) uptake was quantified in HT29 and K562 cell lines and in their doxorubicin resistant sublines (HT29dx and K562dx)

  • A statistically significant lower uptake of Ca AM in the doxorubicin resistant K562dx and HT29dx sublines (p < 0.05) was observed i.e. the uptake was reduced by approximately 70% in comparison to the uptake in the wild type cell lines (K562 and HT29)

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Summary

Introduction

Cell penetrating peptides (CPPs) have been used in many areas of drug delivery for mediating the delivery of peptides, protein, DNA, siRNA and liposomes. They have shown an ability to overcome drug resistance in cells and enhancing chemotherapeutic activity. Objective: The aim of this work is to study the influence of Tat-LK15 peptide on the uptake of p-glycoproteins substrate (Calcein AM). This could explain the effect of peptide on membrane. Tat-LK15 peptide exhibited an inhibitory effect on the calcein fluorescence in both K562 and HT29 cell lines and their doxorubicin resistance sublines (HT29dx and K562dx). The supposed mechanism assumed that Tat-LK15 peptide may change phospholipid architecture/packing in the cell membrane leading to a reduction in the cell

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