Synthesis of 3betaL-Lysinamide-carbamoyl Cholesterol Derivatives by Solid-Phase Method and Characteristics of Complexes with Antisense Oligodeoxynucleotides

摘要

In this report,we describe the synthesis of mono-and di-valent cationic 3betaL-Lysinamide-carbamoyl cholesterol(K-Chol)derivatives by solid-phase peptide synthesis method and the characteristics of K-Chol/ antisense oligodeoxynucleotide(ODN)complexes.K-Chol was able to interact with antisense ODNs electrostatically and constructed nanometer-sized complexes of 50-100 nm in diameter.The formation of K-Chol/antisense ODN complexes was demonstrated by non-denaturing polyacrylamide gel electrophoresis assay and atomic force microscopy.The cell-associated radioactivity was measured to monitor the cellular uptake of the complexes containing radioactive antisense ODNs using HL 60 cells.