Crockett, Sara; Baur, Roland; Kunert, Olaf; Belaj, Ferdinand; Sigel, Erwin (2016). A new chromanone derivative isolated from Hypericum lissophloeus (Hypericaceae) potentiates GABAA receptor currents in a subunit specific fashion. Bioorganic & medicinal chemistry, 24(4), pp. 681-685. Elsevier 10.1016/j.bmc.2015.12.037
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A phytochemical investigation of the lipophilic extract of Hypericum lissophloeus (smoothbark St. John's wort, Hypericaceae) was conducted, resulting in the isolation and identification of a new chromanone derivative: 5,7-dihydroxy-2,3-dimethyl-6-(3-methyl-but-2-enyl)-chroman-4-one (1). This compound was demonstrated to act as a potent stimulator of currents elicited by GABA in recombinant α1β2γ2 GABAA receptors, with a half-maximal potentiation observed at a concentration of about 4μM and a maximal potentiation of >4000%. Significant potentiation was already evident at a concentration as low as 0.1μM. Extent of potentiation strongly depends on the type of α subunit, the type of β subunit and the presence of the γ subunit.
Item Type: |
Journal Article (Original Article) |
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Division/Institute: |
04 Faculty of Medicine > Pre-clinic Human Medicine > Institute of Biochemistry and Molecular Medicine |
UniBE Contributor: |
Baur, Roland, Sigel, Erwin |
Subjects: |
500 Science > 570 Life sciences; biology 600 Technology > 610 Medicine & health |
ISSN: |
0968-0896 |
Publisher: |
Elsevier |
Language: |
English |
Submitter: |
Barbara Franziska Järmann-Bangerter |
Date Deposited: |
04 Mar 2016 11:09 |
Last Modified: |
05 Dec 2022 14:52 |
Publisher DOI: |
10.1016/j.bmc.2015.12.037 |
PubMed ID: |
26791864 |
Uncontrolled Keywords: |
Chromanone; GABA; GABA(A) receptor; Hypericaceae; Hypericum lissophloeus; Section Myriandra |
BORIS DOI: |
10.7892/boris.76361 |
URI: |
https://boris.unibe.ch/id/eprint/76361 |