In Vitro Photodynamic Studies of a BODIPY-Based Photosensitizer

Abstract

A new halogenated 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene (BODIPY) derivative was designed as a singlet-oxygen photosensitizer (PS) for use as a photodynamic therapy (PDT) agent, and its photophysical properties were characterized. The PS, having two iodine atom substituents, exhibited a low fluorescence quantum yield (ΦFL) of 0.02 and high singlet-oxygen-generation quantum yield (ΦΔ) of 0.93. Furthermore, in vitro photodynamic activities were evaluated to assess the potential of using the PS for PDT. A propidium iodide (PI) fluorescence assay and live-cell imaging of Lewis lung carcinoma (LLC) cells demonstrated that the cellular damage is induced by the photosensitization of the BODIPY dye, which subsequently leads to cell death by necrosis.q.