化学
光动力疗法
钌
量子产额
光敏剂
光化学
部分
选择性
荧光素
组合化学
有机化学
荧光
立体化学
催化作用
物理
量子力学
作者
Martin Gillard,Ludovic Troian‐Gautier,Anabelle Decottignies,Benjamin Elias
标识
DOI:10.1021/acs.jmedchem.3c01678
摘要
Ruthenium(II) polypyridyl complexes exhibit a lack of selectivity toward cancer tissues despite extensive studies as photosensitizers for photodynamic therapy (PDT). Here, we report pH-activatable RuII photosensitizers for molecularly targeted PDT by exploiting the higher acidity of tumoral tissue. The fluorescein moiety, well known for its high pH sensitivity, was connected to a RuII center to yield novel photosensitizers for pH-sensitive 1O2 photogeneration. Their ability to photosensitize molecular dioxygen was studied at various pHs and revealed a drastic enhancement from 0.07 to 0.66 of the 1O2 quantum yield under acidic conditions (pH 7.5 to pH 5.5). Their photocytotoxicity against U2OS osteosarcoma cells was also investigated at pH 5.5 and 7.5 through IC50 determination. A strong enhancement of the photocytotoxicity reaching 930 nM was observed at pH 5.5, which showed the potential of such photosensitizers for pH-activatable PDT.
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