A ferutinin analogue with enhanced potency and selectivity against ER-positive breast cancer cells in vitro - 11/07/18
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Graphical abstract |
Highlights |
• | A hemi-synthetic analogue of the natural phytoestrogen ferutinin is designed to overcome its estrogenic activity. |
• | Ferutinin analogue induces a cytotoxic effect 30 times higher than that of ferutinin towards MCF-7 cell line. |
• | Treatment with ferutinin analogue (1 μM) produced significant accumulation of cells at the pre G0/G1 cell cycle phase. |
• | Ferutinin analogue inhibit the proliferation of MCF-7 cell line and consistently target their stem cells. |
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.
Le texte complet de cet article est disponible en PDF.Abbreviations : 3D, BC, BCSCs, Ca2+, CSCs, CTL, E2, EDTA, ER, FBS, FRT, HAEC, HRT, IC50, p-ER, PI, SC, SD, SERM, SFU
Keywords : Ferutinin, Hemi-synthetic analogue, Breast cancer, Estrogen, Stem/progenitor cells
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Vol 105
P. 267-273 - septembre 2018 Retour au numéroBienvenue sur EM-consulte, la référence des professionnels de santé.
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