A selective CuII complex with 4-fluorophenoxyacetic acid hydrazide and phenanthroline displays DNA-cleaving and pro-apoptotic properties in cancer cells
Abstract The thin line between efficacy and toxicity has challenged cancer therapy. As copper is an essential micronutrient and is important to tumor biology, Cu II complexes emerged as an alternative to chemotherapy; however, its biological properties need to be better understood. Thus, we report i...
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Published in | Scientific reports Vol. 11; no. 1; pp. 1 - 15 |
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Main Authors | , , , , , , , , , , , , , , , , |
Format | Journal Article |
Language | English |
Published |
London
Nature Publishing Group
27.12.2021
Nature Publishing Group UK Nature Portfolio |
Subjects | |
Online Access | Get full text |
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Summary: | Abstract
The thin line between efficacy and toxicity has challenged cancer therapy. As copper is an essential micronutrient and is important to tumor biology, Cu
II
complexes emerged as an alternative to chemotherapy; however, its biological properties need to be better understood. Thus, we report in vitro the antitumor effects of two Cu
II
complexes named [Cu(4-fh)(phen)(ClO
4
)
2
] (complex
1
) and [Cu(4-nh)(phen)(ClO
4
)
2
]·H
2
O (complex
2
), in which 4-fh = 4-fluorophenoxyacetic acid hydrazide; 4-nh = 4-nitrobenzoic hydrazide and phen = 1,10-phenanthroline. Both complexes presented cytotoxic activity against tumor cells, but only complex
1
showed significant selectivity. Complex
1
also induced DNA-damage, led to G0/G1 arrest and triggered apoptosis, which was initiated by an autophagy dysfunction. The significant in vitro selectivity and the action mechanism of complex
1
are noteworthy and reveal this prodrug as promising for anticancer therapy. |
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ISSN: | 2045-2322 2045-2322 |
DOI: | 10.1038/s41598-021-03909-1 |