ADENOSINE-1 ACTIVE LIGANDS - CIRSIMARIN, A FLAVONE GLYCOSIDE FROM MICROTEA-DEBILIS

Citation
Ja. Hasrat et al., ADENOSINE-1 ACTIVE LIGANDS - CIRSIMARIN, A FLAVONE GLYCOSIDE FROM MICROTEA-DEBILIS, Journal of natural products, 60(6), 1997, pp. 638-641
Citations number
26
Categorie Soggetti
Chemistry,"Plant Sciences","Pharmacology & Pharmacy","Chemistry Medicinal
Journal title
ISSN journal
01633864
Volume
60
Issue
6
Year of publication
1997
Pages
638 - 641
Database
ISI
SICI code
0163-3864(1997)60:6<638:AAL-CA>2.0.ZU;2-P
Abstract
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 A(1) receptors. Bioassay-guided fractionation using ligand-binding studies resulted i n the isolation of an adenosine A(1) active ligand, cirsimarin (cirsim aritin 4'-O-glucoside). GTP did not influence the radioligand inhibiti on curve of cirsimarin, indicating that this compound is acting as an antagonist at the adenosine-A(1) receptors. The use of this plant agai nst ''proteinuria'' in traditional medicine in Suriname (South America ) may be explained by the adenosine A(1) antagonistic action of cirsim arin. A series of flavonoids was tested in the same assay, but they we re less active. No structure-activity relationship could be observed.