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

Bioorganic & Medicinal Chemistry
Sara CrockettErwin Sigel

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 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.

References

Jan 14, 1998·Trends in Pharmacological Sciences·E Sigel, A Buhr
Feb 11, 2005·Molecular Nutrition & Food Research·Erwin Sigel, Frédéric Minier

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Citations

Sep 27, 2019·Mini Reviews in Medicinal Chemistry·Mariangela MarrelliFilomena Conforti
Mar 15, 2020·Molecular Diversity·Kavita BhagatPreet Mohinder S Bedi
Apr 4, 2021·International Journal of Molecular Sciences·Luiza Carolina França OpretzkaCristiane Flora Villarreal
Aug 29, 2018·Phytochemistry·Henrique BridiGilsane Lino von Poser

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