Chalcone Scaffold in Anticancer Armamentarium: A Molecular Insight

Figure 3

Chalcones against leukemia cell lines. (1) CC₅₀ of 30 μM, (2) CC₅₀ of 40 μM, and (3) CC₅₀ of 40 μM: increases proapoptotic proteins Bax, Bid, and Bak (only chalcone 2) and decreases antiapoptotic Bcl-2 expression. Caspase-9 and caspase-12 activation increases CHOP expression resulting in induction of ER stress. (4) IC₅₀ values (4 to 8 μM) and (5) IC₅₀ values (4 to 8 μM): induction of apoptosis through the reduction of the mitochondrial membrane potential, reduction in Bcl-2 expression, increase in Bax expression, and increase in active caspase-3. ((6a) to (6c)) between 12 and 85 μM for HDAC isoenzymes, inhibiting total HDAC activity by 20–50% at 100 μM: histone deacetylases (HDACs) inhibitor. (7) IC₅₀ of 13.7 ± 0.8 μM: caspase-3 and caspase-7 activation.