Hierarchical Self-Assembly of BODIPY Dyes as a Tool to Improve the Antitumor Activity of Capsaicin in Prostate Cancer.

Hierarchical Self-Assembly of BODIPY Dyes as a Tool to Improve the Antitumor Activity of Capsaicin in Prostate Cancer. Angew Chem Int Ed Engl. 2018 Oct 16;: Authors: Sampedro A, Ramos-Torres A, Schwöppe C, Mück-Lichtenfeld C, Helmers I, Bort A, Diaz-Laviada Marturet I, Fernandez G Abstract Capsaicin (CAP) has been long known for its analgesic properties and more recently for its antitumor activity in various cell types. However, its pungency and the high doses needed to achieve a significant activity have precluded its application in cancer therapy. Herein, we propose a straightforward novel strategy to improve the antitumor effect of CAP based on the enhancement of its aggregation propensity in aqueous media by covalent attachment of a BODIPY (BDP) dye. The target CAP-BDP 1 self-assembles in aqueous solutions into weakly fluorescent globular assemblies that become highly emissive upon cell uptake-induced disassembly. Remarkably, due to the improved delivery of material upon aggregation, we have succeeded in reducing the doses of CAP-based drugs in vivo in prostate cancer two orders of magnitude while maintaining a substantial antitumor activity. PMID: 30324638 [PubMed - as supplied by publisher]
Source: Angewandte Chemie - Category: Chemistry Authors: Tags: Angew Chem Int Ed Engl Source Type: research