Near‐Infrared Light‐Mediated Photoactivation of a Platinum Antitumor Prodrug and Simultaneous Cellular Apoptosis Imaging by Upconversion‐Luminescent Nanoparticles

• DOI: 10.1002/ange.201308834
• Publication Date: 2013-12-06T11:27:47Z
• Authors: Yuanzeng Min; Jinming Li; Fang Liu; Edwin K. L. Yeow; Bengang Xing
• Keywords: Luminescence; Organoplatinum Compounds; Infrared Rays; Antineoplastic Agents; Apoptosis; 02 engineering and technology; 01 natural sciences; Structure-Activity Relationship; Cell Line, Tumor; Humans; Prodrugs; DRNTU::Science::Mathematics; Cell Proliferation; Fluorescent Dyes; Dose-Response Relationship, Drug; Molecular Structure; 540; Photochemical Processes; Silicon Dioxide; 0104 chemical sciences; 3. Good health; :Science::Mathematics [DRNTU]; Nanoparticles; Drug Screening Assays, Antitumor; 0210 nano-technology

AbstractPlatinum‐based drugs are among the most active antitumor reagents in clinical practice; their application is limited by side effects and drug resistance. A novel and personalized near‐infrared (NIR) light‐activated nanoplatform is obtained by combining a photoactivatable platinum(IV) prodrug and a caspase imaging peptide conjugated with silica‐coated upconversion‐luminescent nanoparticles (UCNPs) for the remote control of antitumor platinum prodrug activation, and simultaneously for real‐time imaging of apoptosis induced by activated cytotoxicity. Upon NIR light illumination, the PtIV prodrug complex is activated at the surface of the nanoparticle and active components are selectively released which display cytotoxicity against human ovarian carcinoma A2780 cells and its cisplatin‐resistant variant A2780cis cells. More importantly, the caspases enzymes triggered by cytotoxicity would effectively cleave the probe peptide, thereby allowing the direct imaging of apoptosis in living cells.