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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 
 
 
 
 

Adenosine-1 active ligands: cirsimarin, a flavone glycoside from Microtea debilis.

Several plants collected through different approaches were screened on distinct receptors using ligand-binding studies as bioassay. Extracts of Microtea debilis showed high activity on adenosine A1 receptors. Bioassay-guided fractionation using ligand-binding studies resulted in the isolation of an adenosine A1 active ligand, cirsimarin (cirsimaritin 4'-O-glucoside). GTP did not influence the radioligand inhibition curve of cirsimarin, indicating that this compound is acting as an antagonist at the adenosine-A1 receptors. The use of this plant against "proteinuria" in traditional medicine in Suriname (South America) may be explained by the adenosine A1 antagonistic action of cirsimarin. A series of flavonoids was tested in the same assay, but they were less active. No structure-activity relationship could be observed.[1]

References

  1. Adenosine-1 active ligands: cirsimarin, a flavone glycoside from Microtea debilis. Hasrat, J.A., Pieters, L., Claeys, M., Vlietinck, A., De Backer, J.P., Vauquelin, G. J. Nat. Prod. (1997) [Pubmed]
 
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