Cyclic Peptide Containing Hydrophobic and Positively Charged Residues as a Drug Delivery System for Curcumin.

摘要: Due to the low water solubility and hydrophobic nature of curcumin, an efficient cellular uptake is critical for its biological activity. We have previously developed a number homochiral L-cyclic peptides containing arginine tryptophan as cell-penetrating peptides. Among synthesized peptides, [WR]5 five residues was found be most one. Here, we compared application improve intracellular curcumin by using both peptide-curcumin conjugate physical mixture (peptide + curcumin) strategies. Flow cytometry results showed that (50 μM) enhanced through mixing with 5.7 folds alone in human leukemia (CCRFCEM) cells after 3 h. When conjugated 4 fold. These data suggest can work more efficiently enhancing delivery curcumin. Furthermore, antiproliferative activity 20% ∼13% conjugate, respectively, CCRF-CEM 72