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The present investigation aim 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:
Importantly for this purpose, the effects of 4HC treatment on the proliferation of MCF-7 breast cancer cells and on MCF-10a non-cancerous cells are evaluate using a fluorescent assay. Cell cycle distribution and apoptosis are measure by image cytometry. The expression level of aromatase (CYP19A1) and apoptosis-relate genes were determine by real-time PCR.
Subsequently 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. Buy 2-mcf online
Lastly 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.
Bis(4-hydroxy-2H-chromen-2-one); Coumarin derivative; MCF-7 breast cancer cells; apoptosis; aromatase inhibition; breast cancer; cell cycle; cell proliferation.
Furthermore in connection with our continue research to generate new aza-fused heteroaromatic chemical scaffolds. Also we developed a highly atom-economical three-component route to novel 3,4-dihydropyrrolo[1,2-a]pyrazine ring skeleton multi-functionalize
on the pyrazine unit. This [4+1+1] annulation approach led us to gain access to a new N-fused bicyclic chemical space having two distinctive functional groups (heteroaryl and aroyl) in a trans manner. And Investigation of anticancer activity of the synthesized compounds. Moreso their derivatives reveal that (3R*,4S*)-3-(4-bromophenyl)-4-(4-fluorobenzoyl)-2-(2-oxo-2-phenylethyl)-3,4-dihydropyrrolo[1,2-a]pyrazin-2-ium bromide (3h) also has potent anticancer activity. 3h significantly inhibited cell viability in prostate cancer cells (PC-3) and breast cancer cells (MCF-7) with IC50 value of 1.18 ± 0.05 μM and 1.95 ± 0.04 μM, respectively. In addition 3h strongly reduced cell migration in a dose dependent manner certainly induced apoptosis via caspase-3 activation and cleavage of PARP in PC-3 and MCF-7 cells.
In the same vein our results in this study imply that 3h can be a potential anticancer agent against prostate cancer and breast cancer.