Aggregate Formation of BODIPY-Tethered Oligonucleotides That Led to Efficient Intracellular Penetration and Gene Regulation

摘要： Exogenous nucleic acids showed low e?ciency regarding cellular uptake and low stability in biological conditions; therefore, a number of techniques have been developed to improve their basic properties. One of the best solutions is the application of nanosized particles consisting of oligonucleotides that penetrate the cell membrane without any additives and exhibit high stability in cells. In this report, we employed a simple approach to address the basic properties of nanoparticles of oligonucleotides in biological systems. We prepared BODIPY-labeled oligonucleotides that carried an exclusive modi?cation at the strand end. BODIPY shows high hydrophobicity and ?uorescent emission; therefore, the oligonucleotides formed nanosized aggregates in aqueous solution and their behaviors in cells or tissues were easily revealed that aggregate formation was tracked. Detailed experiments indispensable for the oligonucleotides via scavenger-receptor-mediated endocytosis. In addition, the aggregates provided an e?cient gene regulation in living cells and tumor tissues transplanted into mice.