The alkylphosphocholine, erucylphospho-N,N, N-trimethylpropanolamine (
erufosine), has demonstrated anticancer effects in various cell lines, including
leukemia,
multiple myeloma, bladder, breast and
oral squamous cell carcinoma cells. The purpose of the present study was to investigate its antiproliferative, antimigratory and pro-apoptotic effects in
colorectal cancer cell lines, SW480 and CC531. The antiproliferative effect was determined by (3-[4,5-dimethylthiazol-2-yl]-2, 5-diphenyltetrazolium
bromide) (MTT)
dye reduction assay following exposure to
erufosine (3.1-100 µM) for 24-72 h. The antimigratory effect of
erufosine (1.6-6 µM) was investigated by a wound healing assay for 12-48 h.
Caspase-3/-7 activity was measured to detect apoptotic cell death.
Erufosine inhibited cell proliferation in a dose- and time-dependent manner. The IC50 values following 72 h of incubation were 3.4 and 25.4 µM for SW480 and CC531 cells, respectively.
erufosine at concentrations of 50 and 100 µM induced
caspase-3/-7 activity concentration-dependently in SW480 cells, but only at 100 µM in CC531 cells. Incubation of SW480 cells with
erufosine (1.56 µM) for 48 h inhibited migration into the scratched area by 54% as compared to the untreated cells; whereas in CC531 cells, the
wound width in the
erufosine-treated (1.56-6.25 µM) cells following 48 h was closed 2-fold slower than the rate in the untreated group.
Erufosine (25 µM) attenuated
osteonectin expression and abolished COL1A1 expression in CC531 cells.
Erufosine appears to be a promising treatment agent for
colorectal cancer. Rat CC531 cells are less sensitive to
erufosine than human SW480 cells.