HPLC-based activity profiling for GABAA receptor modulators from Murraya exotica

Syafni, Nova and Moradi-Afrapoli, Fahimeh and Danton, Ombeline and Wilhelm, Anke and Stadler, Marco and Hering, Steffen and Potterat, Olivier and Hamburger, Matthias. (2019) HPLC-based activity profiling for GABAA receptor modulators from Murraya exotica. Natural Product Communications, 14 (1). pp. 41-45.

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Official URL: https://edoc.unibas.ch/70142/

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A dichloromethane extract from twigs and leaves of Murraya exotica produced allosteric potentiation of gamma aminobutyric acid (GABA) induced chloride currents in a microelectrode assay in Xenopus laevis oocytes expressing GABA receptors of α1, β2, γ2s subunit composition. The activity was tracked by HPLC-based activity profiling utilizing a zebrafish locomotor activity assay. Osthol (9) was identified as the main active compound. In addition, five other coumarins and four flavonols were identified. Osthol (9) and structurally related coumurrayin (10) were tested in the Xenopus oocyte assay. Compound 9 potentiated GABAA-induced chloride currents by 487 ± 42%, with an EC50 of 46 ± 10 μM, while 10 showed negligible effects on chloride currents. In silico evaluation of physicochemical properties showed that 9 and 10 had properties that are favorable for oral bioavailability and BBB permeability.
Faculties and Departments:05 Faculty of Science > Departement Pharmazeutische Wissenschaften > Ehemalige Einheiten Pharmazie > Pharmazeutische Biologie (Hamburger)
UniBasel Contributors:Hamburger, Matthias and Syafni, Nova and Danton, Ombeline Réjane and Potterat, Olivier and Moradiafrapoli, Fahimeh
Item Type:Article, refereed
Article Subtype:Research Article
Publisher:Natural Product
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:07 Aug 2020 14:30
Deposited On:07 Aug 2020 14:30

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