Loading…
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...
Saved in:
Published in: | Biomedicine & pharmacotherapy 2021-01, Vol.133, p.111042-111042, Article 111042 |
---|---|
Main Authors: | , , , , , , , , , |
Format: | Article |
Language: | English |
Subjects: | |
Citations: | Items that this one cites Items that cite this one |
Online Access: | Get full text |
Tags: |
Add Tag
No Tags, Be the first to tag this record!
|
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 |