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