A new chromanone derivative isolated from Hypericum lissophloeus (Hypericaceae) potentiates GABAA receptor currents in a subunit specific fashion. Issue 4 (15th February 2016)

• Record Type: Journal Article
• Authors: Crockett, Sara; Baur, Roland; Kunert, Olaf; Belaj, Ferdinand; Sigel, Erwin
• Is Part Of: Bioorganic & medicinal chemistry. Volume 24:Issue 4(2016)
• Page Start: 681
• Page End: 685
• Publication Date: 2016-02-15
• Subjects: Hypericum lissophloeus -- Hypericaceae -- Section Myriandra -- Chromanone -- GABA -- GABAA receptor; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; Biochemistry -- Periodicals; Chemistry, Clinical -- Periodicals; Chemistry, Organic -- Periodicals; Chimie bio-organique -- Périodiques; Chimie pharmaceutique -- Périodiques; 615.19
• DOI: 10.1016/j.bmc.2015.12.037
• Languages: English
• ISSNs: 0968-0896

Abstract

Graphical abstract: Abstract: 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 α1 β2 γ2 GABAA receptors, with a half-maximal potentiation observed at a concentration of about 4 μM and a maximal potentiation of >4000%. Significant potentiation was already evident at a concentration as low as 0.1 μM. Extent of potentiation strongly depends on the type of α subunit, the type of β subunit and the presence of the γ subunit.