Current colorectal cancer (CRC) treatments exhibit unwanted cytotoxicity
against healthy proliferating cells. Hence, these therapeutics demand higher
specificity upon drug delivery, a task that may be facilitated by the discovery
of anticancer agents bearing critical mechanisms of action. Baicalein is a
flavonoid with promising anticancer activity, among other pharmacological
benefits, and has therefore been of high clinical interest. We tested baicaleinin vitrofor its effect on several CRC hallmarks, including
the suppression of metastasis (the spread of cancer cells from their initial
site), the ability to induce apoptosis (cell death), and the inhibition of
proliferation (the growth of cells). The suppression of the metastasis of CRC
cells was recorded via two studies: the cell migration assay and the in
silicodocking
of baicalein with toll-like receptor 4 (TLR4) and matrix metalloproteinase-9
(MMP-9). Results from the cell migration assay showed that baicalein inhibited
metastasis by up to 25.76% (p< 0.01) in a
concentration-dependent manner. We then reinforced these results by docking
baicalein with TLR4 (binding affinity: -8.4 kcal/mol)
and docking baicalein with MMP-9 (binding affinity: -7.9
kcal/mol), classifying
strong binding affinities as those less than -6.0 kcal/mol. The induction of cell death was measured using a caspase
activity assay. Again, a docking study was done to reinforce the findings from
the primaryin vitro experiment, though this time between baicalein and caspase-3 (binding affinity: -7.1 kcal/mol). Despite mixed observations in
concentration dependence, caspase activity, relative to control, reached a
maximal increase of 88.6% (p<
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