Evaluación de la posible actividad sobre el receptor GABAA de compuestos fenólicos de origen natural: Carvacrol y Eugenol

CORVALAN NATALIA,; ZYGADLO JA,; GARCIA DA

Huerta Grande, Córdoba

Congreso; 1º Reunión Conjunta de Sociedades de Biología de la República Argentina; 2007

Sociedades de Biología de la República Argentina

GABAA receptor has different recognition sites to specific ligands (GABA) and other allosteric modulators as benzodiazepines, barbiturates, neurosteroids, etc. Many natural products have been assayed by our group as possible modulators of this receptor. One of them, thymol, demonstrated an important activity as positive modulator and GABA agonist. In the present work, it was evaluated the activity of two natural products on GABAA receptor through the evaluation of the 3H-flunitrazepam binding in sinaptosomal membranes from chicks forebrain. The assayed compounds, carvacrol and eugenol, share in their structure the presence of a phenolic ring. The results showed a positive effect on ligand binding induced by both compounds, with EC50 values of 157Carv y 171Eug and maximal stimulation of 160Carv y 143Eug %. Since these phenolic compounds are highly lipophilic, we analyzed the non-specific ligand binding, which showed non-significative changes respect to control. Concluding, the results indicate a agonist/positive modulatory like activity for both compounds. Additional studies tending to confirm this activity (evaluation of their effects on 3H-flunitrazepam binding in the presence of known GABA antagonist and determination of chloride uptake) are being investigated by our laboratory.