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Novel sulfonamide porphyrin TBPoS-2OH used in photodynamic therapy for malignant melanoma

[Display omitted] •The TBPoS-2OH has photo-cytotoxicity and can effectively inhibit melanoma cell proliferation with a LD50 in the nM range.•After entering the lysosome, TBPO-2OH activated the mitochondrial apoptosis pathway under the stimulation of light.•TBPoS-2OH increases the level of reactive o...

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Bibliographic Details
Published in:Biomedicine & pharmacotherapy 2021-01, Vol.133, p.111042-111042, Article 111042
Main Authors: Pan, Zhaohai, Fan, Jiaojiao, Xie, Qi, Zhang, Xin, Zhang, Wen, Ren, Qing, Li, Minjing, Zheng, Qiusheng, Lu, Jun, Li, Defang
Format: Article
Language:English
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Summary:[Display omitted] •The TBPoS-2OH has photo-cytotoxicity and can effectively inhibit melanoma cell proliferation with a LD50 in the nM range.•After entering the lysosome, TBPO-2OH activated the mitochondrial apoptosis pathway under the stimulation of light.•TBPoS-2OH increases the level of reactive oxygen species in melanoma cells after photo-irradiation. The application of photodynamic therapy (PDT) for the treatment of skin diseases has been receiving much attention. Here, we examined the anti-tumor effect of a novel porphyrin-based photosensitizer TBPoS-2OH in the malignant melanoma A375 and B16 cells. TBPoS-2OH has obvious cell photo-cytotoxicity, but it has low cell dark-cytotoxicity. Further research showed that TBPoS-2OH is enriched in lysosomes after being taken up by cells. Subsequently, the apoptotic rates were significantly increased in TBPoS-2OH-treated A375 and B16 cells. The specific mechanism may be that after receiving light stimulation, TBPoS-2OH could effectively increase the level of intracellular reactive oxygen species (ROS), thereby activating mitochondrial apoptosis pathway-related proteins in A375 and B16 cells. We found an increase in the content of cytochrome C in the cytoplasm, and the levels of related proteins, such as cleaved caspase-3, cleaved caspase-9, and cleaved PARP1, were significantly increased in TBPoS-2OH-treated cells. These results indicated that the new compound TBPoS-2OH could be developed and become an alternative drug for the treatment of melanoma. Some reference ideas for the development of new photosensitizers are also provided.
ISSN:0753-3322
1950-6007
DOI:10.1016/j.biopha.2020.111042