Becatamide Found in Houttuynia cordata Suppresses P-selectin Expression Via Inhibiting COX Enzyme, Not Increasing cAMP in Platelets.

作者: Jae B. Park

DOI: 10.1002/PTR.5391

关键词: Cyclic adenosine monophosphatePlatelet activationChemistryCyclooxygenasePlateletIC50Houttuynia cordataP-selectinThromboxane B2ImmunologyPharmacology

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.

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