Curcumin Polymers as Anticancer Prodrugs

Taking the advantage of the symmetric structure and bi-hydroxyl functionalities of the curcumin molecule, curcumin is polymerized to high molecular weight polymers (polycurcumins) by condensation polymerizations. These polycurcumins had high curcumin content and adjustable water-solubility. Especially, the hydrolysable polycurcumins show significantly higher cytotoxicity than free curcumin against human SKOV-3, MCF-7, and OVCAR cancer cell lines with IC50 of 1.2 ìg/mL, 1.4 ìg/mL and 0.4 µg/mL, respectively, based on the curcumin equivalent dose. The polymer down-regulates the cyclin D1 and CDK4, CDK6 of SKOV-3 in a dose a dose-dependent fashion and arrests SKOV-3 cell cycle at G0/G1 phase. The cell apoptosis via caspase-3-dependent pathway induced by polycurcumin 8 is observed. In vivo, the polymer demonstrates remarkable antitumor activity in SKOV-3 xenograft mice model.