[SUBUNIT SPECIFIC MODULATION OF GLYCINE RECEPTORS BY GINKGOLIC ACID.]

Abstract

Ginkgo biloba extract is a multicomponent pharmacological agent widely used in neurological disorders therapy. It was shown that ginkgolic acid, a constituent of lipophylic Ginkgo biloba extract, has numerous biological activities. In the present study we have focused on the features of ginkgolic acid action on αl and α2 glycine receptors that make part of the inhibitory system of the brain. Using whole-cell configuration of patch-clamp recording we analysed effects of ginkgolic acid on different subunits of glycine receptors. Experiments were performed on cultured Chinese hamster ovary cells (CHO cells), transfected with αl and α2 glycine receptor subunits. Ionic currents were induced by the fast application of different glycine concentrations. After 20-40 sec of pre-treatment with ginkgolic acid (25μM) currents mediated by al glycine receptors reversibly increased from 364±49 pA, (n=34) to 846±134 pA, (n=34). EC(50) for glycine has changed from 36±6 μM (control) to 17±2 μM. In contrast, the application of ginkgolic acid on glycine receptors formed by α2 subunits did not provoke potentiation. Our results demonstrate that ginkgolic acid is a subunit specific modulator of glycine receptors. The mechanisms of the ginkgolic acid action on glycine receptors require further investigation.