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

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 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.

• Authors: J A Hasrat, L Pieters, M Claeys, A Vlietinck, J P De Backer, G Vauquelin
• Journal: Journal of natural products (J Nat Prod) Vol. 60 Issue 6 Pg. 638-41 (Jun 1997) ISSN: 0163-3864 [Print] United States
• PMID: 9214739 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Flavones
• Flavonoids
• Glycosides
• Ligands
• Plant Extracts
• Purinergic P1 Receptor Antagonists
• Receptors, Purinergic P1
• Xanthines
• cirsimarin
• 1,3-dipropyl-8-cyclopentylxanthine

Topics

• Animals
• Flavones
• Flavonoids (chemistry, isolation & purification, pharmacology)
• Glycosides (chemistry, isolation & purification, pharmacology)
• In Vitro Techniques
• Ligands
• Magnetic Resonance Spectroscopy
• Mass Spectrometry
• Membranes (drug effects, metabolism)
• Plant Extracts (chemistry)
• Prosencephalon (drug effects, metabolism)
• Purinergic P1 Receptor Antagonists
• Radioligand Assay
• Rats
• Receptors, Purinergic P1 (drug effects)
• Spectrophotometry, Ultraviolet
• Suriname
• Xanthines