title: In vitro inhibitory activities of Lauraceae aporphine alkaloids.
abstract: The in vitro anti-inflammatory effect of eight aporphine alkaloids isolated from the leaves of two Lauraceae plants (Pleurothyrium cinereum and Ocotea macrophylla) was evaluated through inhibition of two isozymes of cyclooxygenase (COX-1 and COX-2), 5-lipoxygenase (5-LOX), and platelet aggregation induced by PAF, AA and ADP. All alkaloids exhibited inhibitory activities against COX-2 (IC50 25.9-116 microM range) and PAF- and AA-induced platelet aggregation, while only four and three of them were good COX-1 and 5-LOX inhibitors, respectively. (+)-N-acetyl-nornantenine 6 was the most potent COX-2, 5-LOX, AA and PAF inhibitor.
authors.affiliation: Laboratorio de Investigación en Productos Naturales Vegetales, Departamento de Química, Facultad de Ciencias, Universidad Nacional de Colombia, Bogotá D.C., Colombia.
authors.forename: Ericsson David
authors.initials: ED
authors.lastname: Coy Barrera
authors.forename: Luis Enrique
authors.initials: LE
authors.lastname: Cuca Suárez
mesh_terms: D000244:Adenosine Diphosphate / Q000494:pharmacology; D000470:Alkaloids / Q000737:chemistry* / Q000494:pharmacology; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry* / Q000494:pharmacology; D001060:Aporphines / Q000737:chemistry* / Q000494:pharmacology; D016718:Arachidonic Acid / Q000494:pharmacology; D002942:Circular Dichroism; D051545:Cyclooxygenase 1 / Q000378:metabolism; D052246:Cyclooxygenase 2 Inhibitors / Q000737:chemistry / Q000494:pharmacology; D016861:Cyclooxygenase Inhibitors / Q000737:chemistry / Q000494:pharmacology; D005260:Female; D066298:In Vitro Techniques; D019770:Lauraceae / Q000737:chemistry*; D016859:Lipoxygenase Inhibitors; D009682:Magnetic Resonance Spectroscopy; D010936:Plant Extracts / Q000737:chemistry; D018515:Plant Leaves / Q000737:chemistry; D010972:Platelet Activating Factor / Q000494:pharmacology; D010974:Platelet Aggregation / Q000187:drug effects; D011817:Rabbits
chemical_list: D000470:Alkaloids; D000894:Anti-Inflammatory Agents, Non-Steroidal; D001060:Aporphines; D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors; D016859:Lipoxygenase Inhibitors; D010936:Plant Extracts; D010972:Platelet Activating Factor; C081279:aporphine; D016718:Arachidonic Acid; D000244:Adenosine Diphosphate; D051545:Cyclooxygenase 1