Biotinylated curcumin as a novel chemosensitizer enhances naphthalimide-induced autophagic cell death in breast cancer cells.

Achieving selective release of chemical anticancer agents and improving therapeutic efficacy has always been a hot spot in the field of cancer research, yet how to achieve this remains a great challenge. In this work, we constructed a novel chemical anticancer agent (named MCLOP) by introducing naphthalimide into the skeleton of methylene blue (MB). Under the stimulation by cellular hypochlorous acid (HClO) and visible light, selective release of active naphthalimide can be achieved within breast cancer cell lines, the release process of which can be tracked visually using near-infrared fluorescence of MB (685 nm). More importantly, we developed biotinylated curcumin (Cur-Bio) as a new chemosensitizer, which significantly enhanced the ability of MCLOP to induce autophagic cell death of breast cancer cells. This synergistic treatment strategy exhibited an excellent anti-proliferation effect on breast cancer cells in vitro , three-dimensional (3D) cell sphere model, and mouse tumor model in vivo. This work provides a new strategy for the treatment of breast cancer and also opens new opportunities for the efficient treatment of cancer with curcumin-based chemosensitizer. [Display omitted] • New anticancer agent MCLOP was developed based on naphthalimide and methylene blue. • Stimulation with HClO and visible light release active naphthalimide in MCF-7 cells. • The biotinylated curcumin (Cur-Bio) was constructed as a new chemosensitizer. • Cur-Bio enhances the ability of MCLOP to induce autophagic cell death of MCF-7 cells. • Treatment with MCLOP and Cur-Bio exhibits a synergistic anticancer effect in vivo. [ABSTRACT FROM AUTHOR]