Porpholactam-cinnamaldehyde conjugates for promoting ROS generation in photodynamic therapy

摘要

Photodynamic therapy (PDT) is a non-invasive method for cancer treatment that relies on the generation of excess reactive oxygen species (ROS), upon excitation of photosensitizer (PS), to eradicate tumor cells. However, the overexpress of endogenous antioxidants in tumor cells will eliminate the ROS and restrict the therapeutic efficacy of PDT. Herein, a novel type of PS was developed by conjugating cinnamaldehyde (CA), a kind of oxidative stress amplified agent, with porpholactam through a hydrazone bond. The new PS retains the photophysical properties of porpholactam, which displays high singlet oxygen quantum yield for the PDT function. The results of in vitro experiments performed including ROS assay and the cytotoxicity in cancer cells suggest that the rational design of the novel porpholactam-CA derivatives result in enhanced ROS generation upon irradiation, providing a possible approach to achieve enhanced therapeutic effects in PDT. @@@ A novel type of photosensitizer was developed by conjugating cinnamaldehyde (CA), a kind of oxidative stress amplified agent, with porpholactam (PL) through a hydrazone bond, which result in enhanced ROS generation upon irradiation, providing a feasible approach to achieve enhanced therapeutic effects in PDT.

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