Reference : Study of the interaction of antiplasmodial strychnine derivatives with the glycine recep...
Scientific journals : Article
Life sciences : Anatomy (cytology, histology, embryology...) & physiology
Human health sciences : Pharmacy, pharmacology & toxicology
http://hdl.handle.net/2268/4940
Study of the interaction of antiplasmodial strychnine derivatives with the glycine receptor
English
Philippe, Geneviève mailto [Université de Liège - ULg > Département de pharmacie > Pharmacognosie >]
Nguyen, Laurent mailto [Université de Liège - ULg > Département des sciences cliniques > Neurologie >]
Angenot, Luc mailto [Université de Liège - ULg > Département de pharmacie > Pharmacognosie >]
Frederich, Michel mailto [Université de Liège - ULg > Département de pharmacie > Pharmacognosie >]
Moonen, Gustave mailto [Université de Liège - ULg > Département des sciences cliniques > Neurologie - Doyen de la Faculté de Médecine]
Tits, Monique mailto [Université de Liège - ULg > Département de pharmacie > Phytochimie et phytothérapie >]
Rigo, Jean-Michel [Universiteit Hasselt - UH > > > >]
13-Jan-2006
European Journal of Pharmacology
Elsevier Science Bv
530
1-2
15-22
Yes (verified by ORBi)
International
0014-2999
Amsterdam
[en] stryehnine ; glycine receptor ; patch-clarnp ; [H-3]strychnine binding ; antimalarial drug
[en] Strychnos icaja Baill. (Loganiaccae) is a liana found in Central Africa known to be an arrow and ordeal poison but also used by traditional medicine to treat malaria. Recently, many dimeric or trimeric indolomonoterpenic alkaloids with antiplasmodial properties have been isolated from its rootbark. Since these alkaloids are derivatives of strychnine, it was important, in view of their potential use as antimalarial drugs, to assess their possible convulsant strychnine-like properties. In that regard, their interaction with the strychnine-sensitive glycine receptor was investigated by whole-cell patch-clamp recordings on glycine-gated currents in mouse spinal cord neurons in culture and by [H-3]strychnine competition assays on membranes from adult rat spinal cord. These experiments were carried out on sungucine (leading compound of the chemical class) and on the antiplasmodial strychnogucine B (dimeric) and strychnohexamine (trimeric). In comparison with strychnine, all compounds interact with a very poor efficacy and only at concentrations > I mu M with both [H-3]strychnine binding and glycine-gated currents. Furthermore, the effects of strychnine and protostrychnine, a monomeric alkaloid (without antiplasmodial activity) also isolated from S. icaja and differing from strychnine only by a cycle opening, were compared in the same way. The weak interaction of protostrychnine confirms the importance of the G cycle ring structure in strychnine for its binding to the glycine receptor and its antagonist properties. (c) 2005 Elsevier B.V. All rights reserved.
Researchers ; Professionals
http://hdl.handle.net/2268/4940
10.1016/j.ejphar.2005.11.048

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