BODIPY photosensitizers as novel PDT agents against lung cancer cell lines A548 and H1299.

Abstract

Lung cancer is one of the most commonly diagnosed and lethal cancers, affecting both men and women. While conventional treatments such as surgery, chemotherapy, and radiotherapy offer therapeutic benefits in some cases, their efficacy is often limited by side effects and the development of drug resistance. Consequently, the urgent development of novel, more effective, and less toxic therapeutic agents is needed. Photodynamic therapy (PDT) presents a promising alternative, using a photosensitizer activated by visible light of a specific wavelength. This activation generates reactive oxygen species (ROS), inducing cytotoxic effects and ultimately leading to cell death. Despite this potential, the clinical translation of PDT has been affected by the limited number of FDA-approved drugs and clinical trials. This study investigated the potential of a series of BODIPY derivatives as photosensitizers for use in PDT. Eight BODIPYs, belonging to the boron-dipyrromethenes family and representing an alternative to porphyrin-based photosensitizers, were synthesized and evaluated in vitro against two human lung cancer cell lines, A549 and H1299. Notably, the synthesized compounds exhibited significant antitumour activity, warranting further investigation. The photodynamic response was found to be dependent on both photosensitizer concentration and incubation time. Post-treatment, a marked reduction in viability was observed. Among the synthesized photosensitizers, BDPs 3 and 5 (presenting phenyl and anthracenyl groups in meso position, respectively) emerged as the most promising candidates for in vivo PDT studies.