Multifunctional Nanoaggregates Composed of Active CPUL1 and a Triphenylphosphine Derivative for Mitochondria‐Targeted Drug Delivery and Cell Imaging

We report that active substance (CPUL1) and triphenylphosphine (TPP) derivative could self-assemble into multifunctional nanoaggregates (CPUL1-TPP NAs) through electrostatic and π-π stacking interactions. CPUL1 was wrapped tightly inside the nanoparticles as well as CPUL1 and TPP derivative self-assembled into stable and compact nanoparticles in water. The positive surface charge of CPUL1-TPP NAs made them much easier to be endocytosed to enter cytoplasm, accumulate in the mitochondria and induce cell apoptosis based on their mitochondria targeting ability, fluorescence property and fast cell uptake characteristic, which showed better antitumor efficacy on HUH7 hepatoma cells in vitro than that of free CPUL1.