In:
Natural Product Communications, SAGE Publications, Vol. 14, No. 1 ( 2019-01), p. 1934578X1901400-
Abstract:
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 α 1 , β 2 , γ 2s 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 GABA A -induced chloride currents by 487 ± 42%, with an EC 5 0 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.
Type of Medium:
Online Resource
ISSN:
1934-578X
,
1555-9475
DOI:
10.1177/1934578X1901400112
Language:
English
Publisher:
SAGE Publications
Publication Date:
2019
detail.hit.zdb_id:
2430442-6
SSG:
15,3
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