In vitro inhibitory activities of Lauraceae aporphine alkaloids.
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.
Coy Barrera
Ericsson David
ED
Laboratorio de Investigación en Productos Naturales Vegetales, Departamento de Química, Facultad de Ciencias, Universidad Nacional de Colombia, Bogotá D.C., Colombia.
Cuca Suárez
Luis Enrique
LE
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
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