Inhibition of benzodiazepine binding in vitro by amentoflavone, a constituent of various species of Hypericum

• Published in: Pharmaceutica acta Helvetiae Vol. 72; no. 3; pp. 153 - 157
• Main Authors: H. Baureithel, Karl, Büter, Karin Berger, Engesser, Anja, Burkard, Willy, Schaffner, Willi
• Format: Journal Article
• Language: English
• Published: Switzerland Elsevier B.V 01.06.1997
• Subjects: [3H]flumazenil; Amentoflavone; Animals; Antidepressive Agents - pharmacology; Benzodiazepine receptor (BDZ-R); Biflavonoids; Binding, Competitive; Brain - drug effects; Brain - metabolism; Cells, Cultured; Flavonoids - isolation & purification; Flavonoids - pharmacology; Flumazenil - metabolism; GABA Modulators - metabolism; GABA-A Receptor Antagonists; Hypericum; Perylene - analogs & derivatives; Perylene - pharmacology; Plant Extracts - pharmacology; Plants, Medicinal; Rats; Amentoflavone; [3H]flumazenil; Hypericum; Benzodiazepine receptor (BDZ-R)

Flower extracts of Hypericum perforatum, Hypericum hirsutum, Hypericum patulum and Hypericum olympicum efficiently inhibited binding of [3H]flumazenil to rat brain benzodiazepine binding sites of the GABAA-receptor in vitro with IC50 values of 6.83, 6.97, 13.2 and 6.14 μg/ml, respectively. Single co...