Mechanism of cytotoxic activity of chalcone derivatives against K562 leukemia cell lines
Abstract: Chalcone, a
precursor of flavonoids that are abundantly found in plants, has been
investigated and found to possess anticancer activity. This study aimed to
evaluate the effect of chalcone derivatives on the PI3K/AKT signaling pathway
in the K562 cell line. A K562 cell line was treated with two chalcone
derivatives: (E)-1-(4-aminophenyl)-3-(2,3dimethoxyphenyl)-prop-2-en-1-one
(Compound 4), and (E)-1-(4-aminophenyl)-3-phenylprop-2-en-1-one) (Compound 7),
and compared to the anticancer drugs imatinib and accutane. Measurement of AKT
caspase-3, STAT3, and cyclin D1 were performed with ELISA, whilst cell cycle
and apoptosis analysis were performed using flow cytometry. Both Compound 4 and
Compound 7 at all concentrations showed the most significantly decreased AKT
levels in K562. Compound 4 at 5 and 10 µg/mL, and Compound 7 at 10 µg/mL,
significantly increased caspase-3 on K562, although this was lower than when
using imatinib. Compound 4 and Compound 7 in all concentrations showed
decreasing STAT3 on K562, which were comparable to imatinib. Compound 4 and
Compound 7 showed the highest decrease of cyclin D1 among treatments, and also
arrested G0/G1 and G2/M phase in K562
cells, with the results being comparable to imatinib and Isotretinoin. Compound
4 and Compound 7 are promising anticancer agents that function via inhibition
of the PI3K/AKT signaling pathway, induction of apoptosis through up-regulation
of apoptotic markers, and blockade of cell cycle progression by regulating cell
cycle-related factors.
Author: Arina Novilla
Journal Code: jpkedokterangg170293
