A ferutinin analogue with enhanced potency and selectivity against ER-positive breast cancer cells in vitro.
Biomed Pharmacother
; 105: 267-273, 2018 Sep.
Article
em En
| MEDLINE
| ID: mdl-29860218
ABSTRACT
Estrogen is considered a risk factor for breast cancer since it promotes breast-cell proliferation. The jaesckeanadiol-3-p-hydroxyphenylpropanoate, a hemi-synthetic analogue of the natural phytoestrogen ferutinin (jaesckeanadiol-p-hydroxybenzoate), is designed to be devoid of estrogenic activity. This analogue induces a cytotoxic effect 30 times higher than that of ferutinin towards MCF-7 breast cancer cell line. We compared these two compounds with respect to their effect on proliferation, cell cycle distribution and cancer stem-like cells in the MCF-7 cell line. Treatment with ferutinin (30 µM) and its analogue (1 µM) produced significant accumulation of cells at the pre G0/G1 cell cycle phase and triggered apoptosis. Importantly, this compound retains its anti-proliferative activity against breast cancer stem/progenitor cells that are naturally insensitive to ferutinin at the same dose. These results position ferutinin analogue as an effective compound inhibiting the proliferation of estrogen-dependent breast cancer cells and consistently targeting their stem-like cells.
Palavras-chave
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Sesquiterpenos
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Benzoatos
/
Neoplasias da Mama
/
Receptores de Estrogênio
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Cicloeptanos
Tipo de estudo:
Risk_factors_studies
Limite:
Female
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Humans
Idioma:
En
Revista:
Biomed Pharmacother
Ano de publicação:
2018
Tipo de documento:
Article
País de afiliação:
Líbano