双核铂(II)-蒽配合物作为溶酶体定位光动力抗癌试剂的研究

Abstract

Dinuclear platinum (II)-anthracene complexes for photodynamic anticancer therapy. • Lysosomal disruption via ROS generation. • Apoptosis induction and caspase-3 activation. • Induction of immunogenic cell death. • Inhibition of 3D multicellular tumor spheroids growth. Photodynamic therapy (PDT) has emerged as an appealing and promising approach for cancer treatment. In this study, two dinuclear platinum (II)-anthracene complexes were synthesized and their PDT anticancer activities were investigated. Results showed that complex 2 ({[Pt (dpa)] 2 L }(NO 3 ) 4 , L  = 9,10-di (pyridin-4-yl)anthracene and dpa = bis-(2-pyridylmethyl)amine) effectively produced both type I and type II reactive oxygen species (ROS) upon 405 nm light irradiation. In vitro studies revealed that 2 selectively accumulated in lysosomes, leading to significant lysosomal damage upon light exposure. This damage subsequently arrested the cell cycle at G0/G1 phase, induced cell apoptosis and evoked immunogenic cell death (ICD) in cancer cells. Download: Download high-res image (350KB) Download: Download full-size image