Phytochemicals are ubiquitous in naturally occurring dietary elements that exhibits diverse pharmacological properties over various pathological disorders, including cancer. Voltage gated K+ (KV) channel in the plasma membrane contributes to wide range of cellular processes including cancer progression. Therefore, modulation of KV channel is being considered as a novel potential target for cancer therapy. The whole cell patch clamp technique was used to record the modulatory effect of chrysin, naringenin, caffeic acid, gallic acid, and zingerone on delayed rectifier potassium current (IK) in human prostate cancer cells LNCaP and PC-3. Among the tested compounds, zingerone blocked IK in a concentration-dependent manner in LNCaP cells and estimated the IC50 value of 141 μM and Emax was 81.3%. Further analysis of KV channel activation kinetics showed that zingerone induces a positive shift in the activation curve in LNCaP cells, whereas the inhibitory effect of gallic acid on IK was significantly less potent than the inhibition caused by zingerone. However, chrysin, naringenin, and caffeic acid did not modulate the KV channel conductance in LNCaP or PC-3 cells. Our findings confirmed that not all the tested phytochemicals to be effective modulators of IK and suggested that IK inhibitory effect of zingerone and gallic acid may be responsible for their anticancer effects in prostate cancer cells.
Keywords: Flavonoid; I K; Phenolic acids; Phenolic alkanone; Prostate cancer.