三阴性乳腺癌(TNBC)是最具恶性的乳腺肿瘤之一，因其预后差和高复发率而闻名。开发新的策略或有效药剂以克服耐药和提高治疗效果是非常紧迫的。基于硼二吡咯烷(BODIPY) 的光敏剂具有令人兴奋的光物理特性，可用于治疗刻划应用，即光动力疗法(PDT)。我们设计了一种带有BODIPY衍生物的发光单官能团铂(II)络合物，即 I2BC-Pt，作为三阴性乳腺癌(TNBC)崭新的高PDT剂处理。二碘化BODIPY络合物I2BC-Pt在绿光(520nm)下对MDA-MB-231和MDA-MB-468细胞展现出了出色的PDT效果，给予的IC50值介于0.11-0.13μM之间。I2BC-Pt主要在MDA-MB-231细胞线粒体中聚集并发出绿色荧光。此外，抗癌机制研究表明，I2BC-Pt通过减弱RAD51、FoxM1和BRCA1/2来帮助DNA修复，诱导p53介导的TNBC细胞凋亡。总之，I2BC-Pt有望成为一种基于BODIPY的光敏剂，用于TNBC治疗。Copyright © 2023. Elsevier Inc. 发布。

Triple-negative breast cancer (TNBC) is one of the most malignant breast tumors for its poor prognosis and high tumor recurrence. It is urgent to develop new strategy or effective agents to overcome resistance and improve therapeutic effectiveness. Boron-dipyrromethene (BODIPY) based photosensitizers possess exciting photophysical features suitable for theranostic applications, namely, photodynamic therapy (PDT). We have designed a luminescent monofunctional platinum(II) complex with BODIPY derivative, namely I2BC-Pt, as novel high PDT agent against triple negative breast cancer (TNBC). The di-iodinated BODIPY complex I2BC-Pt showed excellent PDT effect against TNBC cells in green light (520 nm) giving IC50 values of 0.11-0.13 μM in MDA-MB-231 and MDA-MB-468 cells. I2BC-Pt predominately aggregated in the mitochondria of MDA-MB-231 cells and emitted green fluorescence. Besides, the anticancer mechanism studies demonstrated that I2BC-Pt could help DNA repair through attenuating RAD51, FoxM1 and BRCA1/2, and induce p53-mediated apoptosis of TNBC cells. Taken together, I2BC-Pt could be potentially developed as a BODIPY-based photosensitizers for TNBC therapy.Copyright © 2023. Published by Elsevier Inc.