摘要
Singlet oxygen(^(1)O_(2)) is a strong oxidant which plays important roles in photodynamic therapy(PDT). The exploitation of photosensitizers with high ^(1)O_(2) production is crucial to improve PDT efficiency. In this study, a radical labeled quartet photosensitizer Cy-DENT is reported with high singlet oxygen quantum yield(Φ_(Δ)=32.3%) due to a radical enhanced inter-system crossing(ISC) process. After the introduction of 2,2,6,6-tetramethylpiperidinyloxy(TEMPO) radical, quartet state ^(4)[R,T] of CyDENT could be formed to give an over 20-fold enhancement of singlet oxygen quantum yield compared to Cy-DEN(without TEMPO radical) under irradiation of near infrared(NIR) light. In addition, the ^(1)O_(2 )production is well controlled by varying the electron-donating ability of the terminal substituent group. Cy-DENT possesses good cell permeability and is localized in mitochondria. Under the irradiation of 700 nm light, Cy-DENT can produce high levels of ROS to destroy the mitochondria membrane potential and induce cell apoptosis. Through the encapsulation of PEG-SS-PCL micelle, Cy-DENT can be effectively delivered to tumors and suppresses the tumor growth after PDT treatment.
基金
supported by the National Natural Science Foundation of China(21421005,21576037,U1608222)。
