Polycationic Core–Shell Polyurea Dendrimers with Anticancer Activity

Professors Nuno Bernardes, Sandra Pinto and Vasco Bonifácio (DBE, iBB) published in Biomaterials Science the synthesis and study of the intrinsic anticancer activity of two polycationic core–shell biodendrimers, PUREG4-OEI48 and PUREG4-OCEI24. These biodendrimers were designed as synthetic mimics of anticancer peptides (SMACPs).
Evaluation of their activity in several cancer cell lines showed that PUREG4-OEI48 compromises cell membrane integrity, interacts with mitochondria, and induces apoptosis, as evidenced by Annexin V⁺/PI⁺ cells after incubation at the IC₅₀ concentration. In contrast, PUREG4-OCEI24, which is more hydrophobic and less cationic, exhibits cytotoxic effects and inhibits cell migration (wound-healing assay) after 24 h, suggesting a mechanism partially associated with cell necrosis. Both biodendrimers act on the mitochondrial membrane, activating distinct cell death pathways. See more.
