作者: Jae B. Park
DOI: 10.1002/PTR.5391
关键词: Cyclic adenosine monophosphate 、 Platelet activation 、 Chemistry 、 Cyclooxygenase 、 Platelet 、 IC50 、 Houttuynia cordata 、 P-selectin 、 Thromboxane B2 、 Immunology 、 Pharmacology
摘要: Atherosclerosis is a well-known inflammatory cardiovascular disease. Recent studies suggested potential anti-atherosclerosis effects of becatamide found in Houttuynia cordata. Therefore, this study, we investigated effect (1) and its analogues (enferamide (2), veskamide (3), oretamide (4) amkamide (5)) on cyclooxygenase (COX)-1 -2 the production cyclic adenosine monophosphate (cAMP), which are critically involved platelet activation. Among them, was most potent compound able to inhibit COX-1 (IC50 = 0.27 µm) = 0.78 µm) (p veskamide > enferamide > oretamide > amkamide. As result inhibition, thromboxane B2 P-selectin expression were suppressed by 35% (p < 0.05) 28% (p < 0.05), respectively, mouse blood treated with (0.25 µm). However, did not increase intracellular cAMP platelets. suppression blocked beta 2-adrenoceptor antagonists, suggesting that COX inhibition likely an underlying mechanism for suppression. In summary, may be activation inhibiting enzymes, increasing cAMP. Published 2015. This article U.S. Government work public domain USA.