TY - JOUR T1 - Bis(4-hydroxy-2H-chromen-2-one) Coumarin Induces Apoptosis in MCF-7 Human Breast Cancer Cells Through Aromatase Inhibition JF - Anticancer Research JO - Anticancer Res SP - 6107 LP - 6114 DO - 10.21873/anticanres.13818 VL - 39 IS - 11 AU - LAMIA HAMDAN RAMDANI AU - OUALID TALHI AU - CAROLINE DECOMBAT AU - MARION VERMERIE AU - ALEXANDRE BERRY AU - ARTUR SILVA AU - KHALDOUN BACHARI AU - MARIE-PAULE VASSON AU - LAETITIA DELORT AU - FLORENCE CALDEFIE-CHÉZET Y1 - 2019/11/01 UR - http://ar.iiarjournals.org/content/39/11/6107.abstract N2 - Aim: The present investigation aimed to examine the therapeutic potential of the new coumarin derivative bis(4-hydroxy-2H-chromen-2-one) coumarin (4HC) against breast cancer. Materials and Methods: For this purpose, the effects of 4HC treatment on the proliferation of MCF-7 breast cancer cells and on MCF-10a non-cancerous cells were evaluated using a fluorescent assay. Cell cycle distribution and apoptosis were measured by image cytometry. The expression level of aromatase (CYP19A1) and apoptosis-related genes were determined by real-time PCR. Results: MCF-7 mammary cancer cell proliferation was significantly decreased within 24 h after treatment with 4HC at 50 μM, while no effect was observed on the viability of MCF-10a non-cancerous mammary cells. 4HC also increased the percentage of the cells in the G2/M phase, inducing apoptosis. Real-time PCR revealed that 4HC induced MCF-7 mortality through an up-regulation of Bax and a down-regulation of Bcl-2, resulting in an increase in caspase-3 gene expression. The increased expression of apoptosis-related genes was accompanied by a decrease in CYP19A1 gene expression. Conclusion: 4HC selectively inhibits proliferation of MCF-7cells in vitro. Moreover, 4HC has inhibitory effects on aromatase gene expression and promoting effects on apoptosis, in MCF-7 cells. ER -