A new chromanone derivative isolated from Hypericum lissophloeus (Hypericaceae) potentiates GABAA receptor currents in a subunit specific fashion.

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)

Division/Institute:

04 Faculty of Medicine > Pre-clinic Human Medicine > Institute of Biochemistry and Molecular Medicine

UniBE Contributor:

Baur, Roland and Sigel, Erwin

Subjects:

500 Science > 570 Life sciences; biology
600 Technology > 610 Medicine & health

ISSN:

0968-0896

Publisher:

Elsevier

Language:

English

Submitter:

Barbara Järmann-Bangerter

Date Deposited:

04 Mar 2016 11:09

Last Modified:

04 Mar 2016 11:09

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

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