Inhibition of the hERG potassium channel by phenanthrene: a polycyclic aromatic hydrocarbon pollutant.

ABSTRACT: The lipophilic polycyclic aromatic hydrocarbon (PAH) phenanthrene is relatively abundant in polluted air and water and can access and accumulate in human tissue. Phenanthrene has been reported to interact with cardiac ion channels in several fish species. This study was undertaken to investigate the ability of phenanthrene to interact with hERG (human Ether-à-go-go-Related Gene) encoded Kv11.1 K⁺ channels, which play a central role in human ventricular repolarization. Pharmacological inhibition of hERG can be proarrhythmic. Whole-cell patch clamp recordings of hERG current (I_hERG) were made from HEK293 cells expressing wild-type (WT) and mutant hERG channels. WT I_hERG1a was inhibited by phenanthrene with an IC₅₀ of 17.6 ± 1.7 µM, whilst I_hER

SUBMITTER: Al-Moubarak E 

PROVIDER: S-EPMC8629796 | biostudies-literature | 2021 Dec

REPOSITORIES: biostudies-literature