title: Inhibition of Kv1.3 Channels in Human Jurkat T Cells by Xanthohumol and Isoxanthohumol.
abstract: Using whole-cell patch-clamp technique, we investigated influence of selected compounds from groups of prenylated chalcones and flavonoids: xanthohumol and isoxanthohumol on the activity of Kv1.3 channels in human leukemic Jurkat T cells. Obtained results provide evidence that both examined compounds were inhibitors of Kv1.3 channels in these cells. The inhibitory effects occurred in a concentration-dependent manner. The estimated value of the half-blocking concentration (EC50) was about 3 μM for xanthohumol and about 7.8 μM for isoxanthohumol. The inhibition of Kv1.3 channels by examined compounds was not complete. Upon an application of the compounds at the maximal concentrations equal to 30 μM, the activity of Kv1.3 channels was inhibited to about 0.13 of the control value. The inhibitory effect was reversible. The application of xanthohumol and isoxanthohumol did not change the currents' activation and inactivation rate. These results may confirm our earlier hypothesis that the presence of a prenyl group in a molecule is a factor that facilitates the inhibition of Kv1.3 channels by compounds from the groups of flavonoids and chalcones. The inhibition of Kv1.3 channels might be involved in antiproliferative and proapoptotic effects of the compounds observed in cancer cell lines expressing these channels.
authors: Department of Biophysics, Wroclaw Medical University, ul. Chałubińskiego 10, 50-368, Wrocław, Poland.
authors: Justyna
authors: J
authors: Gąsiorowska
authors: Andrzej
authors: A
authors: Teisseyre
authors: Anna
authors: A
authors: Uryga
authors: Krystyna
authors: K
authors: Michalak
mesh_terms: D049109:Cell Proliferation / Q000187:drug effects*; D004305:Dose-Response Relationship, Drug; D005419:Flavonoids / Q000494:pharmacology*; D006801:Humans; D019169:Jurkat Cells; D051664:Kv1.3 Potassium Channel / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011427:Propiophenones / Q000494:pharmacology*; D044004:Xanthones / Q000494:pharmacology*
chemical_list: D005419:Flavonoids; D051664:Kv1.3 Potassium Channel; D011427:Propiophenones; D044004:Xanthones; C512910:isoxanthohumol; C104536:xanthohumol