title: Inhibition of platelet-activating factor receptor binding by aporphine and phenanthrenoid alkaloids from Aromadendron elegans.
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
authors.affiliation: 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.
authors.forename: I
authors.initials: I
authors.lastname: Jantan
authors.forename: I A
authors.initials: IA
authors.lastname: Rafi
authors.forename: J
authors.initials: J
authors.lastname: Jalil
mesh_terms: D000470:Alkaloids / Q000302:isolation & purification / Q000494:pharmacology*; D000818:Animals; D001060:Aporphines / Q000302:isolation & purification / Q000494:pharmacology*; D066298:In Vitro Techniques; D016859:Lipoxygenase Inhibitors / Q000302:isolation & purification / Q000494:pharmacology*; D019684:Magnoliopsida / Q000737:chemistry*; D015394:Molecular Structure; D010616:Phenanthrenes / Q000302:isolation & purification / Q000494:pharmacology*; D010936:Plant Extracts; D010980:Platelet Membrane Glycoproteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011817:Rabbits; D011956:Receptors, Cell Surface; D043562:Receptors, G-Protein-Coupled; D013329:Structure-Activity Relationship
chemical_list: D000470:Alkaloids; D001060:Aporphines; D016859:Lipoxygenase Inhibitors; D010616:Phenanthrenes; D010936:Plant Extracts; D010980:Platelet Membrane Glycoproteins; D011956:Receptors, Cell Surface; D043562:Receptors, G-Protein-Coupled; C039351:platelet activating factor receptor; C081279:aporphine