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Article Dans Une Revue Chemico-Biological Interactions Année : 2010

Parazoanthoxanthin A blocks Torpedo nicotinic acetylcholine receptors.

Résumé

Nicotinic acetylcholine receptors are implicated in different nervous system-related disorders, and their modulation could improve existing therapy of these diseases. Parazoanthoxanthin A (ParaA) is a fluorescent pigment of the group of zoanthoxanthins. Since it is a potent acetylcholinesterase inhibitor, it may also bind to nicotinic acetylcholine receptors (nAChRs). For this reasonits effect on Torpedo nAChR (alpha1(2)betagammadelta) transplanted to Xenopuslaevis oocytes was evaluated, using the voltage-clamp technique. ParaA dose-dependently reduced the acetylcholine-induced currents. This effect was fully reversible only at lower concentrations. ParaA also reduced the Hill coefficient and the time to peak current, indicating a channel blocking mode of action. On the other hand, the combined effect of ParaA and d-tubocurarine (d-TC) on acetylcholine-induced currents exhibited only partial additivity, assuming a competitive mode of action of ParaA on nAChR. These results indicate a dual mode of action of ParaA on the Torpedo AChR.

Dates et versions

hal-00464523 , version 1 (17-03-2010)

Identifiants

Citer

Klara Bulc Rozman, Rómulo Aráoz, Kristina Sepčić, Jordi Molgó, Dušan Suput. Parazoanthoxanthin A blocks Torpedo nicotinic acetylcholine receptors.. Chemico-Biological Interactions, 2010, 187 (1-3), pp.384-7. ⟨10.1016/j.cbi.2010.03.016⟩. ⟨hal-00464523⟩

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