ABSTRACT
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.
Subject(s)
Artemisia/chemistry , Flavonoids/pharmacology , Receptors, GABA-A/drug effects , Chromatography, High Pressure Liquid , Flavones/isolation & purification , Flavones/pharmacology , Flumazenil/pharmacology , GABA Agonists/isolation & purification , GABA Agonists/pharmacology , GABA Antagonists/isolation & purification , GABA Antagonists/pharmacology , GABA Modulators/pharmacology , Lebanon , Magnetic Resonance Spectroscopy , Plant Extracts/chemistry , Radioligand AssayABSTRACT
In the recent decades the use of traditional medicine in Lebanon has increased. Aqueous, ethanol and ethyl acetate extracts of seven Lebanese plants that are used traditionally for neurological disorders as Alzheimer's disease, epilepsy and affective disorders as depression were tested for inhibition of acetylcholinesterase and affinity to the GABA(A)-benzodiazepine site and to the serotonin transporter. Ethyl acetate extracts of Salvia triloba, Lavandula officinalis, Origanum syriacum and Artemisia herba-alba exhibited weak activity in the acetylcholinesterase assay. None of the plants were active in the serotonin transporter assay. An ethanolic extract of Artemisia herba-alba had good affinity to the GABA(A)-benzodiazepine receptor site; ethanolic extracts of Melissa officinalis and Salvia triloba had moderate activity.
