Du, Kun and De Mieri, Maria and Saxena, Priyanka and Phungula, K. V. and Zietsman, P. C. and Hering, S. and van der Westhuizen, J. H. and Hamburger, Matthias. (2015) HPLC-Based Activity Profiling for hERG Channel Inhibitors in the South African Medicinal Plant Galenia africana. Planta Medica, 81 (12/13). pp. 1154-1162.
Full text not available from this repository.
Official URL: http://edoc.unibas.ch/39407/
Downloads: Statistics Overview
Abstract
The human ether-a-go-go-related gene channel is a voltage-activated K(+) channel involved in cardiac action potential. Its inhibition can lead to QT prolongation, and eventually to potentially fatal arrhythmia. Therefore, it is considered a primary antitarget in safety pharmacology. To assess the risk of human ether-a-go-go-related gene channel inhibition by medicinal plants, 700 extracts from different parts of 142 medicinal plants collected in Southern Africa were screened on Xenopus laevis oocytes. A CH2Cl2 extract from the stems and leaves of Galenia africana (Aizoaceae) reduced the peak tail human ether-a-go-go-related gene current by 50.4 ± 5.5 % (n = 3) at a concentration of 100 µg/mL. By means of high-performance liquid chromatography-based activity profiling, nine flavonoids were identified in the active time windows. However, the human ether-a-go-go-related gene channel inhibition of isolated compounds was less pronounced than that of extract and active microfractions (human ether-a-go-go-related gene inhibition between 10.1 ± 5 and 14.1 ± 1.6 at 100 µM). The two major constituents, 7,8-methylenedioxyflavone (1) and 7,8-dimethoxyflavone (13), were quantified (4.3 % and 9.4 %, respectively, in the extract). Further human ether-a-go-go-related gene inhibition tests for compounds 1 and 13 at 300 µM showed a concentration-dependent inhibitory activity (33.2 ± 12.4 and 30.0 ± 7.4, respectively). In a detailed phytochemical profiling of the active extract, a total of 20 phenolic compounds, including six new natural products, were isolated and identified.
Faculties and Departments: | 05 Faculty of Science > Departement Pharmazeutische Wissenschaften > Ehemalige Einheiten Pharmazie > Pharmazeutische Biologie (Hamburger) |
---|---|
UniBasel Contributors: | Hamburger, Matthias and de Mieri, Maria |
Item Type: | Article, refereed |
Article Subtype: | Research Article |
Publisher: | Georg Thieme Verlag |
ISSN: | 0032-0943 |
e-ISSN: | 1439-0221 |
Note: | Publication type according to Uni Basel Research Database: Journal article |
Identification Number: | |
Last Modified: | 28 Nov 2017 08:42 |
Deposited On: | 04 May 2016 07:13 |
Repository Staff Only: item control page