Investigation of The Effects of Blocking of Potassium Channels with 4-
Aminopyridine on Paclitaxel Activity in Breast Cancer Cell Lines
Abstract
Paclitaxel (PTX) has been used as a chemotherapeutic agent for several
malignancies including breast cancer and efforts to increase the
efficiency of PTX are continuing. In this study, FDA-approved
4-aminopyridine (4-AP), a voltage-gated potassium channel blocker, was
used in combination with PTX in MCF-7 and MDA MB 231 cell lines it has
been confirmed that K+ (potassium) channels are involved in the cell
cycle. Viability was determined with trypan blue, a clonogenic assay was
performed, and the cell cycle was determined with a flow cytometer and
immunochemistry. To gain an insight into the mechanism, intracellular K+
concentration, intracellular Ca2+ (calcium) concentration, and
transmembrane potential measurements were made with corresponding
fluorescent dyes. Apoptotic cell number was determined using Annexin /PI
method by flow cytometer. Viability decreased with combination therapy
and the clonogenic assay proved decreased colony formation. Apoptotic
cell number was increased after treatment with the combination in both
cell lines. Cell cycle measurements showed G1 arrest for both MCF-7 and
MDA MB 231 cell lines upon 4-AP treatment. PTX caused G1 arrest in MCF-7
cells and S phase arrest in MDA MB 231 cells. Combination treatment
caused S phase arrest in MCF-7 cells and S phase and G2/M phase arrest
in MDA MB 231 cells. Intracellular K+ concentration was increased after
all treatments in both cell lines. Ca2+ concentration was increased
significantly after combination treatment. Depolarization in the
transmembrane potential was observed after all treatments in both cell
lines. Biophysical parameters like the transmembrane potential and ion
fluxes have been defined in cancer progression which can provide new
aspects for cancer treatments. This study shows that the combination of
4-AP with PTX is a promising alternative the mechanism of which needs
further investigation considering the results obtained for Ca2+, K+, and
membrane potential.