Photodynamic therapy(PDT)has emerged as a significant cancer therapy option.Currently,cation-based organic small molecule aggregation-induced emission(AIE)photosensitizers(PSs)attract the wide atten-tion of many scien...Photodynamic therapy(PDT)has emerged as a significant cancer therapy option.Currently,cation-based organic small molecule aggregation-induced emission(AIE)photosensitizers(PSs)attract the wide atten-tion of many scientists,due to improved reactive oxygen species(ROS)production after cationization.However,such PSs tend to localize only the mitochondria,limiting the death way of tumor cells(usu-ally apoptosis)during PDT process,which may affect the therapeutic effect under some circumstances.Herein,we designed a novel water-soluble three positive charge PS,TPAN-18F,which could be distributed uniformly in cell cytoplasm and had distribution in different sub-organelles(mitochondria,endoplasmic reticulum,lysosome).The experimental results showed that TPAN-18F-based PDT process can not only disrupt mitochondrial functions(reducing ATP production and destroying mitochondrial membrane po-tential),but also elevate the intracellular lipid peroxides(LPOs)level,which evoke the non-apoptotic death manner of tumor cells.Further,in vivo studies showed that TPAN-18F-based PDT could effectively inhibit tumor growth.Accordingly,we believe that the construction of TPAN-18F is suggestive for tumor non-apoptotic therapy.展开更多
基金supported by the National Science Foundation of China(No.21890744)the National Key R&D Program of China(No.2019YFA0210100).
文摘Photodynamic therapy(PDT)has emerged as a significant cancer therapy option.Currently,cation-based organic small molecule aggregation-induced emission(AIE)photosensitizers(PSs)attract the wide atten-tion of many scientists,due to improved reactive oxygen species(ROS)production after cationization.However,such PSs tend to localize only the mitochondria,limiting the death way of tumor cells(usu-ally apoptosis)during PDT process,which may affect the therapeutic effect under some circumstances.Herein,we designed a novel water-soluble three positive charge PS,TPAN-18F,which could be distributed uniformly in cell cytoplasm and had distribution in different sub-organelles(mitochondria,endoplasmic reticulum,lysosome).The experimental results showed that TPAN-18F-based PDT process can not only disrupt mitochondrial functions(reducing ATP production and destroying mitochondrial membrane po-tential),but also elevate the intracellular lipid peroxides(LPOs)level,which evoke the non-apoptotic death manner of tumor cells.Further,in vivo studies showed that TPAN-18F-based PDT could effectively inhibit tumor growth.Accordingly,we believe that the construction of TPAN-18F is suggestive for tumor non-apoptotic therapy.
