Using the whole-cell patch-clamp technique, we investigated the influence of
8-prenylnaringenin on the activity of the voltage-gated Kv1.3
potassium channels in the human leukemic T lymphocyte cell line Jurkat.
8-prenylnaringenin is a potent plant-derived
phytoestrogen that has been found to inhibit
cancer cell proliferation. The results show that it inhibited the Kv1.3 channels in a concentration-dependent manner. Complete inhibition occurred at concentrations higher than 10 μM. The inhibitory effect of
8-prenylnaringenin was reversible. It was accompanied by a significant acceleration of channel inactivation without any pronounced change in the activation rate. Of the
naringenin derivatives tested to date,
8-prenylnaringenin is the most potent inhibitor of the Kv1.3 channels. The potency of the inhibition may be due to the presence of a
prenyl group in the molecule of this
flavonoid. The inhibition of the Kv1.3 channels might be involved in the antiproliferative and pro-apoptotic effects of
8-prenylnaringenin that have been observed in
cancer cell lines expressing these channels.