SUBUNIT SPECIFIC MODULATION OF GLYCINE RECEPTORS BY GINKGOLIC ACID
G. Maleeva1,2, S. Buldakova1, P. Bregestovski1
- Institute of System Neurosciences, University of Aix-Marseille, France;
- O. O. Bogomoletz Institute of Physiology, National Academy of Science, Ukraine, Kyiv
DOI: https://doi.org/10.15407/fz62.04.040
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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 α1 and α2 glycine receptors that make part of the inhibitory
system of the brain. Using whole-cell configuration of patchclamp
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 α1 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 α1 glycine receptors reversibly
increased from 364±49 pA, (n=34) to 846±134 pA, (n=34). EC50
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 а subunit specific modulator of
glycine receptors. The mechanisms of the ginkgolic acid action
on glycine receptors require further investigation.
Keywords:
glycine receptor; ginkgolic acid; ionic currents; patch-clamp.
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