Journal
SMALL METHODS
Volume 5, Issue 11, Pages -Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/smtd.202100770
Keywords
aromatic rings; helicene; kidney cancer; selectivity; water-soluble helicenes
Funding
- National Natural Science Foundation of China [81771968, 82073295, 82003166, 92056110, 22075180]
- Shanghai Municipal Commission of Health and Family Planning [201840020]
- Shanghai Jiao Tong University [ZH2018ZDA05]
- Science and Technology Commission of Shanghai Municipality [18JC1415500, 195271040, 20JC1415000]
- Shanghai Municipal Education Commission-Gaofeng Clinical Grant Support [20181705]
- Innovative Research Team of High-level Local Universities in Shanghai [SSMU-ZDCX20180200]
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Helicenes exhibit anticancer capability by changing molecular structure, with nonplanar helicenes showing increased cytotoxicity and cancer inhibition against RCC cells. Benzo[4]helicenium selectively damages RCC cancer cells' mitochondria and DNA, indicating potential as a targeted drug for RCC treatment.
Immune and targeted therapy are becoming the first-line treatment for renal cell carcinoma (RCC). However, therapeutic outcomes are limited due to the low efficiency and side effect. Here, it is found that helicenes are able to exhibit an anticancer capability through changing the molecular structure from planar to nonplanar. Furthermore, the cytotoxicity in vitro and cancer inhibition ability of nonplanar helicenes increase with its aromatic rings' number. It is further demonstrated that benzo[4]helicenium shows the specific killing efficiency against the RCC cancer as compared to normal kidney cells. This is majorly originated from a more selective damage of benzo[4]helicenium for mitochondria and DNA in RCC cancer cells, not the normal kidney. The selective killing ability of benzo[4]helicenium makes it have potential to be used as a targeted drug for the precise treatment of RCC.
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