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Caffedymine from cocoa has COX inhibitory and cAMP producing activities suppressing the expression of a platelet activation marker, P‐selectin.
Author(s) -
Park Jae
Publication year - 2007
Publication title -
the faseb journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.709
H-Index - 277
eISSN - 1530-6860
pISSN - 0892-6638
DOI - 10.1096/fasebj.21.5.a360-c
Subject(s) - enzyme , platelet , chemistry , inhibitory postsynaptic potential , thromboxane , thromboxane a2 , pharmacology , biochemistry , endocrinology , biology , receptor , immunology
Caffedymine (N‐caffeoyldopamine) is a clovamide‐type phenylpropenoic acid amide found in cocoa plant. Previous studies indicate that caffedymine inhibits P‐selectin expression via increasing cAMP through beta‐2 adrenoceptors, but the inhibition is only partially repressed by beta‐2 adrenoceptor antagonists, suggesting additional mechanism underlying the inhibitory effect. Therefore, in this study, the effect of caffedymine and its analogues (N‐caffeoyltyramine, N‐feruloyltyramine, N‐coumaroyltyramine, N‐cinnamoyltyramine) on COX enzymes (I and II) was investigated, because COX enzymes are deeply involved in regulating P‐selectin expression on human platelets. The decreasing order of COX‐I inhibitory activity was caffedymine > N‐caffeoyltyramine > N‐feruloyltyramine > N‐coumaroyltyramine > N‐cinnamoyltyramine. Caffedymine was the most potent compound able to inhibit COX‐I enzyme by 43 % (P < 0.013), at the concentration (0.01 microM). At the same concentration, caffedymine was also able to inhibit COX‐II enzyme by 36 % (P < 0.015), and the decreasing order of COX‐II inhibitory activity was similar as that of COX‐I. As a result of the COX inhibition, the production of thromboxane B2, (thromboxane A2 derivative) also decreased significantly in mouse blood treated with caffedymine and its analogues (0.05 microM). Caffedymine and N‐caffeoyltyramine with potent COX inhibitory activity are also able to inhibit P‐selectin expression and platelet‐leukocyte interactions. These data indicate that COX inhibition is likely to be another mechanism for caffedymine to inhibit P‐selectin expression on platelets. Also, potential beneficial effects of caffedymine on the reported adversary effects of COX inhibitors are discussed in this study.