Purification and identification of components of the Aquilegia vulgaris extract fraction exhibiting anti-epileptic activity
R. Solomonia 1,2, N. Kuchiashvili 1, V. Pkhakadze1, N. Trapaidze 1, I. Abesadze 1,
H. Kojima 2 and N. Dalakishvili1
Institute of Physiology, Georgian Academy of Sciences, 14 Gotua St, 0160 Tbilisi, Georgia
Laboratory of Biologically Active Compounds, Department of Biochemistry, I. Javakhishvili State University, 2 University St, Tbilisi, Georgia
National Institute of Advanced Industrial Science & Technology, Higashi, Tsukuba, Ibaraki 305-8565, Japan
The extract of the plant Aquilegia vulgaris is used in folk medicine as an antiepileptic andsoporific medicament. Our previous results demonstrated that the extractcontains compounds selectively acting on the GABAA-receptorsystem in vitro. The present workaimed to identify and characterize these compounds. High performance liquidchromatography with subsequent gas chromatography coupled with massspectrometry have identified two main active compounds of this extract: (1) myo-inositol and (2) an oleamide sleep-inducing lipid.The effects of oleamide on GABAA receptors are well documented, whereas the influence of myo-inositol on neuroreceptors has not been prevouslydescribed. We have also observed that myo-inositol inhibits 3H-muscimol (a specific ligand ofthe GABA binding site at the GABAA receptor)binding and stimulates 3H-MK801 (a specific ligand of activated NMDA-typeglutamate receptors) binding. These results, combined with our previousfindings on the effects of myo-inositolon epileptic convulsions, clearly indicate that oleamide and myo-inositol are the main compounds determining theantiepileptic and soporific attributes of Aquilegia vulgaris extract.
Keywords: epilepsy, GABAA-receptor, HPLC,mass spectrometry, myo-inositol,oleamide