Planta Med 2014; 80(12): 1045-1050
DOI: 10.1055/s-0034-1382907
Biological Screening
Original Papers
Georg Thieme Verlag KG Stuttgart · New York

Natural Products as Potential Human Ether-a-Go-Go-Related Gene Channel Inhibitors – Outcomes from a Screening of Widely Used Herbal Medicines and Edible Plants

Anja Schramm1, Evelyn A. Jähne1, Igor Baburin2, Steffen Hering2, Matthias Hamburger1
  • 1Division of Pharmaceutical Biology, University of Basel, Basel, Switzerland
  • 2Institute of Pharmacology and Toxicology, University of Vienna, Vienna, Austria
Weitere Informationen

Publikationsverlauf

received 27. Februar 2014
revised 25. Juni 2014

accepted 30. Juni 2014

Publikationsdatum:
04.August 2014 (eFirst)

Abstract

Inhibition of the human ether-a-go-go-related gene channel is the single most important risk factor leading to acquired long QT syndrome. Drug-induced QT prolongation can cause severe cardiac complications, including arrhythmia, and is thus a liability in drug development. Considering the importance of the human ether-a-go-go-related gene channel as an antitarget and the daily intake of plant-derived foods and herbal products, surprisingly few natural products have been tested for channel blocking properties. In an assessment of possible human ether-a-go-go-related gene liabilities, a selection of widely used herbal medicines and edible plants (vegetables, fruits, and spices) was screened by means of a functional two-microelectrode voltage-clamp assay with Xenopus oocytes. The human ether-a-go-go-related gene channel blocking activity of selected extracts was investigated with the aid of a high-performance liquid chromatography-based profiling approach, and attributed to tannins and alkaloids. Major European medicinal plants and frequently consumed food plants were found to have a low risk for human ether-a-go-go-related gene toxicity.

Supporting Information