article · Biomolecules
A series of cinnamaldehyde-based chalcone derivatives, designated 3a to 3k, were synthesised and evaluated for antioxidant properties and anticancer activity against human Caco-2 colon cancer cells. Among the tested molecules, compound 3e demonstrated the strongest antioxidant activity in DPPH assays. It also exhibited the most potent inhibitory effect on Caco-2 cell proliferation, achieving the lowest half-maximal inhibitory concentration, whilst causing no harmful effects on healthy human lung cells. Detailed cellular assessments revealed that compound 3e induced both early and late apoptosis and caused DNA damage evidenced by comet assay findings. Further molecular analyses demonstrated that the compound altered the expression of apoptosis-related genes and proteins, triggering Caspase-3 activation through an intrinsic apoptotic pathway. These findings indicate that compound 3e has potential as a therapeutic candidate for the treatment of human colon cancer.
Colorectal cancer remains a major global health challenge requiring treatments that selectively destroy malignant cells without damaging normal tissue. This research identifies a specific synthetic chalcone derivative that halts colon cancer cell growth and triggers cellular suicide mechanisms in vitro, all whilst sparing healthy lung cells in laboratory tests.
This research is at an early, laboratory-based discovery stage. The findings could enable oncology drug development teams to consider compound 3e as a lead molecule for colon cancer therapies. Moving towards practical application will require substantial further research, including in vivo efficacy testing, pharmacokinetic evaluations, and comprehensive safety profiling before clinical trials could be considered.
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The purpose of the current investigation was to produce cinammaldehyde-based chalcone derivatives (<b>3a</b>-<b>k</b>) to evaluate their potential effectiveness as antioxidant and inhibitory agents versus human Caco-2 cancer cells. The findings obtained using the DPPH assay showed that compound <b>3e</b> had the highest effective antioxidant activity with the best IC<sub>50</sub> value compared with the other compounds. Moreover, the cytotoxic findings revealed that compound <b>3e</b> was the best compound for inhibiting Caco-2 development in contrast to all other produced derivatives, with the lowest IC<sub>50</sub> concentration (32.19 ± 3.92 µM), and it also had no detrimental effects on healthy human lung cells (wi38 cells). Exposure of Caco-2 cells with this IC<sub>50</sub> value of compound <b>3e</b> resulted in a substantial rise in the number of early and late cells that are apoptotic with a significant comet nucleus when compared with control cells employing the annexin V/PI and comet evaluations, respectively. Furthermore, qRT-PCR and ELISA examinations indicated that compound <b>3e</b> significantly altered the expression of genes and their relative proteins related to apoptosis in the treated Caco-2 cells, thus significantly inhibiting Caco-2 growth through activating Caspase-3 via an intrinsic apoptotic pathway. As a result, compound <b>3e</b> could serve as an effective therapy for human colon cancer.
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DOI: 10.3390/biom14020216
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