光动力疗法
光敏剂
化学
细胞毒性
赫拉
质子化
猝灭(荧光)
荧光
光化学
单线态氧
生物物理学
紧身衣
溶酶体
癌细胞
组合化学
体外
氧气
生物化学
有机化学
癌症
离子
物理
量子力学
生物
酶
医学
内科学
作者
Carlotta Figliola,Halina Anton,Christophe Sutter,Camille Chériaux,Alexandra Sutter,Valérie Mazan,Mourad Elhabiri,Pascal Didier,Denis Jacquemin,Gilles Ulrich
出处
期刊:ChemBioChem
[Wiley]
日期:2023-05-16
卷期号:24 (12)
被引量:8
标识
DOI:10.1002/cbic.202300139
摘要
Photodynamic therapy (PDT) is a photochemistry-based medical treatment combining light at a specific wavelength and a photosensitizer (PS) in the presence of oxygen. Application of PDT as a conventional treatment is limited and clearly the approval in clinics of new PS is challenging. The selective accumulation of the PS in the targeted malignant cells is of paramount importance to reduce the side effects that are typical of the current worldwide approved PS. Here we report a new series of aniline- and iodine-substituted BODIPY derivatives (1-3) as promising lysosome-targeting and pH-responsive theranostic PS, which displayed a significant in vitro light-induced cytotoxicity, efficient imaging properties and low dark toxicity (for 2 and 3). These compounds were obtained in few reproducible synthetic steps and good yields. Spectroscopic and electrochemical measurements along with computational calculations confirmed the quenching of the emissive properties of the PS, while both fluorescence and 1 O2 emission were obtained only under acidic conditions inducing amine protonation. The pKa values and pH-dependent emissive properties of 1-3 being established, their cellular uptake and activation in the lysosomal vesicles (pH≈4-5) were confirmed by their co-localization with the commercial LysoTracker deep red and light-induced cytotoxicity (IC50 between 0.16 and 0.06 μM) against HeLa cancer cells.
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