Recent studies report that
chalcones exhibit cytotoxicity to human
cancer cell lines. Typically, the form of cell death induced by these compounds is apoptosis. In the context of the discovery of new
anticancer agents and in light of the antitumour potential of several
chalcone derivatives, in the present study, we synthesized and tested the cytotoxicity of six
chalcone derivatives on human
colon adenocarcinoma cells. Six derivatives of 3-phenyl-1-(thiophen-2-yl) prop-2-en-1-one were prepared and characterized on the basis of their (1) H and (13) C NMR spectra. HT-29 cells were treated with synthesized
chalcones on two concentrations by three different incubation times. Cells were evaluated by cell morphology, Tetrazolium
dye (MTT) colorimetric assay, live/dead, flow cytometry (
annexin V) and gene expression analyses to determine the cytotoxic way.
Chalcones 3-(4-bromophenyl)-1-(thiophen-2-yl)prop-2-en-1-one (C06) and 3-(2-nitrophenyl)-1-(thiophen-2-yl)prop-2-en-1-one (C09) demonstrated higher cytotoxicity than other
chalcones as shown by cell morphology, live/dead and MTT assays. In addition, C06 induced apoptosis on flow cytometry
annexin V assay. These data were confirmed by a decreased expression of anti-apoptotic genes and increased pro-apoptotic genes. Our findings indicate in summary that the cytotoxic activity of
chalcone C06 on
colorectal carcinoma cells occurs by apoptosis.