首页|Synthesis and evaluation of new fluorinated pyropheophorbide-a derivatives for photodynamic therapy
Synthesis and evaluation of new fluorinated pyropheophorbide-a derivatives for photodynamic therapy
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NSTL
The discovery of new photosensitizers with excellent photodynamic anti-tumor effects remains a challenge for photodynamic therapy and diagnosis. Here a series of chlorophyll derivatives containing fluorine-substituted alkyl side chain were designed and synthesized. These compounds exhibited strong absorption at 660-665 nm with excellent molar extinction coefficients. Their singlet oxygen generation ability was also proved to be excellent. Upon excitation with a 411 nm laser, strong fluorescence emission around 660-670 nm was observed. They also showed obvious photodynamic antitumor activity to A549 cell in vitro and to tumor-bearing mice in vivo. Their photodynamic anti-proliferative abilities were confirmed in vivo with histotomy. Flow cytometry test showed that new compounds could induce late period cell apoptosis or necrosis. Sub-organelle localization test indicated that they primarily localized in the endoplasmic reticulum. Among them, compound F-C4-Ppa possesses the most outstanding anti-tumor effect and therefore, it is a promising anti-tumor drug candidate in photodynamic therapy and photo-imaging diagnosis.
NSTL
