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HPLC-based activity profiling approach for the discovery of GABAA receptor ligands using a functional assay with Xenopus oocytes

Kim, H. J. and Baburin, S. and Khom, S. and Hering, S. and Hamburger, M.. (2008) HPLC-based activity profiling approach for the discovery of GABAA receptor ligands using a functional assay with Xenopus oocytes. Planta medica, Vol. 74, H. 5. pp. 521-526.

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Official URL: http://edoc.unibas.ch/dok/A5251065

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Abstract

An approach for rapid HPLC-based profiling for new GABAA ligands of natural origin has been developed. Active extracts are separated by a single injection of 3 - 10 mg of extract onto a semi-preparative (150 × 10 mm i. d.) HPLC column with gradient elution and time-based fractionation. The microfractions are tested in an automated two-microelectrode voltage-clamp assay on Xenopus oocytes expressing recombinant GABAA channels composed of α1, β2 and γ2S subunits. The protocol has been validated by spiking experiments with inactive extract and the GABAA receptor ligand magnolol, and by profiling of active extracts such as valerian extract containing the known GABAA receptor ligand valerenic acid. For dereplication of GABA containing extracts, we established a rapid and simple procedure by which GABA is analyzed as OPA derivative by reversed-phase HPLC. This dereplication protocol was validated with plant and fungal extracts which had been previously tested active or inactive in the oocyte assay and with spiking experiments.
Faculties and Departments:05 Faculty of Science > Departement Pharmazeutische Wissenschaften > Pharmazie > Pharmazeutische Biologie (Hamburger)
UniBasel Contributors:Hamburger, Matthias
Item Type:Article, refereed
Article Subtype:Research Article
Bibsysno:Link to catalogue
Publisher:Hippokrates-Verl.
ISSN:0032-0943
Note:Publication type according to Uni Basel Research Database: Journal article
Last Modified:22 Mar 2012 14:22
Deposited On:22 Mar 2012 13:30

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