title: Myricetin inhibits Kv1.5 channels in HEK293 cells.
abstract: Myricetin (Myr) is a flavonoid that exerts anti-arrhythmic effects. However, its potential effects on ion channels have remained elusive. The aim of the present study was to investigate the effects of Myr on Kv1.5 channels in HEK293 cells. The current of Kv1.5 channels (Ikur) in HEK293 cells was recorded using the whole-cell patch-clamp technique and the expression of the Kv1.5 protein was measured using western blot analysis 24 h after treatment with Myr. The results showed that 5 µM Myr significantly reduced Ikur from 215.04 ± 40.59 to 77.72 ± 17.94 pA/pF (P<0.05; n=5). Myr increased the current suppression from 0 to 0.31 ± 0.12 and 0.55 ± 0.11 over 5 or 20 min, respectively. In addition, Ikur decreased from 376.23 ± 1.30 to 270.19 ± 4.28 pA/pF when the frequency was increased from 0.5 to 4 Hz in HEK293 cells treated with 10 µM Myr for 5 min. Furthermore, Myr reduced hKv1.5 protein expression in a dose-dependent manner. These results demonstrated that Myr inhibited Ikur and the expression of hKv1.5 in HEK293 cells in a dose-, time- and frequency-dependent manner. These observations partly explained the mechanisms by which Myr exerts anti-arrhythmic effect.
authors.affiliation: The Key Laboratory of Medical Electrophysiology, Ministry of Education of China, Luzhou Medical College, Luzhou, Sichuan 646000, P.R. China.
authors.forename: Xianhong
authors.initials: X
authors.lastname: Ou
authors.affiliation: The Key Laboratory of Medical Electrophysiology, Ministry of Education of China, Luzhou Medical College, Luzhou, Sichuan 646000, P.R. China.
authors.forename: Xiaohong
authors.initials: X
authors.lastname: Bin
authors.affiliation: The Key Laboratory of Medical Electrophysiology, Ministry of Education of China, Luzhou Medical College, Luzhou, Sichuan 646000, P.R. China.
authors.forename: Luzhen
authors.initials: L
authors.lastname: Wang
authors.affiliation: The Key Laboratory of Medical Electrophysiology, Ministry of Education of China, Luzhou Medical College, Luzhou, Sichuan 646000, P.R. China.
authors.forename: Miaoling
authors.initials: M
authors.lastname: Li
authors.affiliation: The Key Laboratory of Medical Electrophysiology, Ministry of Education of China, Luzhou Medical College, Luzhou, Sichuan 646000, P.R. China.
authors.forename: Yan
authors.initials: Y
authors.lastname: Yang
authors.affiliation: The Key Laboratory of Medical Electrophysiology, Ministry of Education of China, Luzhou Medical College, Luzhou, Sichuan 646000, P.R. China.
authors.forename: Xinrong
authors.initials: X
authors.lastname: Fan
authors.affiliation: The Key Laboratory of Medical Electrophysiology, Ministry of Education of China, Luzhou Medical College, Luzhou, Sichuan 646000, P.R. China.
authors.forename: Xiaorong
authors.initials: X
authors.lastname: Zeng
mesh_terms: D004305:Dose-Response Relationship, Drug; D005419:Flavonoids / Q000737:chemistry / Q000633:toxicity*; D057809:HEK293 Cells; D006801:Humans; D015640:Ion Channel Gating / Q000187:drug effects; D051666:Kv1.5 Potassium Channel / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013997:Time Factors
chemical_list: D005419:Flavonoids; D051666:Kv1.5 Potassium Channel; C040015:myricetin