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

作者：Crockett Sara^*; Baur Roland; Kunert Olaf; Belaj Ferdinand; Sigel Erwin

来源：Bioorganic & Medicinal Chemistry, 2016, 24(4): 681-685.

DOI：10.1016/j.bmc.2015.12.037

• Hypericum lissophloeus
• Hypericaceae
• Section Myriandra
• Chromanone
• GABA
• GABA(A) receptor

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 alpha(1)beta(2 gamma 2) GABA(A) receptors, with a half-maximal potentiation observed at a concentration of about 4 mu M and a maximal potentiation of >4000%. Significant potentiation was already evident at a concentration as low as 0.1 mu M. Extent of potentiation strongly depends on the type of alpha subunit, the type of beta subunit and the presence of the gamma subunit.

• 出版日期2016-2-15