Linked Life Data

16375888

Source:http://linkedlifedata.com/resource/pubmed/id/16375888

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
1-2
pubmed:dateCreated
2006-1-9
pubmed:abstractText
Strychnos icaja Baill. (Loganiaceae) 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 [(3)H]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 >1 microM with both [(3)H]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.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jan
pubmed:issn
0014-2999
pubmed:author
pubmed:issnType
Print
pubmed:day
13
pubmed:volume
530
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
15-22
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed-meshheading:16375888-Alkaloids, pubmed-meshheading:16375888-Animals, pubmed-meshheading:16375888-Antimalarials, pubmed-meshheading:16375888-Binding, Competitive, pubmed-meshheading:16375888-Carbazoles, pubmed-meshheading:16375888-Cells, Cultured, pubmed-meshheading:16375888-Dimerization, pubmed-meshheading:16375888-GABA Antagonists, pubmed-meshheading:16375888-Medicine, African Traditional, pubmed-meshheading:16375888-Membrane Potentials, pubmed-meshheading:16375888-Molecular Structure, pubmed-meshheading:16375888-Neurons, pubmed-meshheading:16375888-Patch-Clamp Techniques, pubmed-meshheading:16375888-Plant Roots, pubmed-meshheading:16375888-Pyridazines, pubmed-meshheading:16375888-Radioligand Assay, pubmed-meshheading:16375888-Rats, pubmed-meshheading:16375888-Receptors, Glycine, pubmed-meshheading:16375888-Spinal Cord, pubmed-meshheading:16375888-Structure-Activity Relationship, pubmed-meshheading:16375888-Strychnine, pubmed-meshheading:16375888-Strychnos, pubmed-meshheading:16375888-Tritium
pubmed:year
2006
pubmed:articleTitle
Study of the interaction of antiplasmodial strychnine derivatives with the glycine receptor.
pubmed:affiliation
Natural and Synthetic Drugs Research Center, Laboratory of Pharmacognosy, University of Liège, Belgium. g.phillippe@ulg.ac.be
pubmed:publicationType
Journal Article, Comparative Study, Research Support, Non-U.S. Gov't