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N‐Coumaroyldopamine and N‐caffeoyldopamine increase cAMP via beta 2‐adrenoceptors in myelocytic U937 cells
Author(s) -
Park Jae B.
Publication year - 2005
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/fj.04-2782com
Subject(s) - potency , fenoterol , chemistry , u937 cell , atenolol , agonist , beta (programming language) , pharmacology , salbutamol , adrenergic receptor , b2 receptor , endocrinology , receptor , stereochemistry , medicine , biochemistry , biology , in vitro , bradykinin , asthma , computer science , blood pressure , programming language
N‐Caffeoyldopamine is a phytochemical found in various plants, including cocoa (Theobroma cacao L.). N‐caffeoyldopamine and its natural analogs (N‐cinnamoyldopamine, N‐coumaroyldopamine, N‐feruloyldopamine, and N‐sinapoyldopamine) were synthesized and investigated to determine their potency as β‐adrenoceptor agonists, because they have chemical structural moieties found in β‐adrenoceptor agonists. Among the compounds tested in this study, N‐coumaroyldopamine and N‐caffeoyldopamine were the two most potent compounds, able to increase cAMP at the concentrations < 0.05 µM in U937 cells. The decreasing order of potency was N‐coumaroyldopamine < N‐caffeoyldopamine < N‐feruloyldopamine < N‐sinapoyldopamine < N‐cinnamoyldopamine. Using β2‐specific antagonists (butoxamine and ICI 118551), N‐coumaroyldopamine and N‐caffeoyldopamine were found to increase cAMP via β2‐adrenoceptors in U937 cells. In producing cAMP in U937 cells, N‐coumaroyldopamine and N‐caffeoyldopamine were as potent as several well‐known β2‐adrenoceptor agonists (salbutamol, procaterol, and fenoterol). These results indicate that N‐coumaroyldopamine and N‐caffeoyldopamine are potent compounds able to increase cAMP via β2‐adrenoceptors in U937 cells, and may have potential effects on human health.—Park, J. B. N‐Coumaroyldopamine and N‐caffeoyldopamine increase cAMP via beta 2‐adrenoceptors in myelocytic U937 cells. FASEB J . 19, 497–502 (2005)