oligorutin

Oligorutin (OR) is a novel oligoflavonoid-derived delivery system synthesized enzymatically. It demonstrates preferential penetration into cancer cells through a lipid raft-mediated endocytosis pathway, with cell membrane cholesterol being crucial for its internalization. This tumor-targeting property has been confirmed by in vivo biodistribution studies. Oligorutin has been utilized to develop pH-responsive drug delivery systems, such as OR-BTZ, by conjugating it with antitumor drugs like bortezomib via a pH-sensitive borate ester bond. OR-BTZ has shown cytotoxicity, inhibition of migration and invasion in hepatoma carcinoma cells, and low systemic toxicity in murine hepatocellular carcinoma models, while exhibiting no apparent cytotoxicity to normal liver cells. This research highlights the potential of oligoflavonoids as biomaterials for targeted cancer therapy.