Inhibition of platelet-activating factor receptor binding by aporphine and phenanthrenoid alkaloids from Aromadendron elegans

I Jantan; I A Rafi; J Jalil

doi:10.1055/s-2001-15819

Inhibition of platelet-activating factor receptor binding by aporphine and phenanthrenoid alkaloids from Aromadendron elegans

Planta Med. 2001 Jul;67(5):466-7. doi: 10.1055/s-2001-15819.

Authors

I Jantan¹, I A Rafi, J Jalil

Affiliation

¹ receptor binding, with IC50 values of 52.4, 38.6, and 29.8 microM, respectively. The flexibility of the biphenyl system of the aporphine and the presence of methoxy groups at C-9 and C-10 were all preferable in binding to the receptor.

PMID: 11488464
DOI: 10.1055/s-2001-15819

Abstract

Six aporphine and one phenanthrenoid alkaloids isolated from Aromadendron elegans Blume were investigated for their inhibitory effect on platelet-activating factor (PAF) binding to rabbit platelets using 3H-PAF as a ligand. Of the compounds tested, (-)-N-acetylanonaine, 1-(N-acetyl-N-methylamino)ethyl-3,4,6-trimethoxy-7-hydroxy-phenanthrene, and predicentrine showed strong inhibition of

Publication types

Letter

MeSH terms

Alkaloids / isolation & purification
Alkaloids / pharmacology*
Animals
Aporphines / isolation & purification
Aporphines / pharmacology*
In Vitro Techniques
Lipoxygenase Inhibitors / isolation & purification
Lipoxygenase Inhibitors / pharmacology*
Magnoliopsida / chemistry*
Molecular Structure
Phenanthrenes / isolation & purification
Phenanthrenes / pharmacology*
Plant Extracts
Platelet Membrane Glycoproteins / antagonists & inhibitors*
Platelet Membrane Glycoproteins / metabolism
Rabbits
Receptors, Cell Surface*
Receptors, G-Protein-Coupled*
Structure-Activity Relationship

Substances

Alkaloids
Aporphines
Lipoxygenase Inhibitors
Phenanthrenes
Plant Extracts
Platelet Membrane Glycoproteins
Receptors, Cell Surface
Receptors, G-Protein-Coupled
platelet activating factor receptor
aporphine