Two flavonoids from Artemisia herba-alba Asso with in vitro GABAA-benzodiazepine receptor activity.
An ethyl acetate extract of Artemisia herba-alba was partitioned by HPLC in 10 fractions that were tested in the [(3)H]-flumazenil radioligand assay, for affinity to the GABA(A)-benzodiazepine receptor. Two fractions showed activity from which hispidulin and cirsilineol were isolated. The structures were confirmed by (1)H NMR. The IC(50) values were 8 microM for hispidulin and 100 microM for cirsilineol.
Salah
Sam Medhat
SM
Department of Medicinal Chemistry, The Danish University of Pharmaceutical Sciences, 2 Universitetsparken, 2100 Copenhagen O, Denmark.
Jäger
Anna Katharina
AK
D019306:Artemisia / Q000737:chemistry*; D002851:Chromatography, High Pressure Liquid; D047309:Flavones / Q000302:isolation & purification / Q000494:pharmacology; D005419:Flavonoids / Q000494:pharmacology*; D005442:Flumazenil / Q000494:pharmacology; D018755:GABA Agonists / Q000302:isolation & purification / Q000494:pharmacology; D018756:GABA Antagonists / Q000302:isolation & purification / Q000494:pharmacology; D018757:GABA Modulators / Q000494:pharmacology; D007861:Lebanon; D009682:Magnetic Resonance Spectroscopy; D010936:Plant Extracts / Q000737:chemistry; D011869:Radioligand Assay; D011963:Receptors, GABA-A / Q000187:drug effects*
D047309:Flavones; D005419:Flavonoids; D018755:GABA Agonists; D018756:GABA Antagonists; D018757:GABA Modulators; D010936:Plant Extracts; D011963:Receptors, GABA-A; D005442:Flumazenil; C057618:cirsilineol; C055957:hispidulin