A moderate consumption of red wine may reduce the risk of cardiovascular diseases via wine-derived phenolic compounds. A variety of biological mechanisms have been proposed for wine-derived phenolic compounds including nitric oxide-mediated vasorelaxation. This study examined whether the vasodilating effect of wine-derived phenolic compounds was associated with the inhibition of phosphodiesterases (PDEs) and, in particular, PDE5. For this purpose, human recombinant PDE5A1 isoform was prepared by expression of the full-length cDNA of PDE5A1 into COS-7 cells. Red wine and the extracts from grape skin inhibited PDE5A1 activity, whereas the seed extracts had a negligible effect. The mixture of anthocyanins inhibited the enzyme activity (IC50 = 11.6 μM), with malvidin-3-O-β-glucoside (IC50 = 35.4 μM) and malvidin (IC50 = 24.9 μM) the most potent among the monoglucosides and aglycons, respectively. trans-Resveratrol and trans-piceid exhibited negligible effects, whereas hydroxycinnamates were completely inactive. These results indicate that polyphenols-induced vasorelaxation may also be sustained by smooth muscle PDE inhibition by anthocyanins present in red wines and grapes

Dell'Agli, M.; Galli, G.V.; Vrhovsek, U.; Mattivi, F.; Bosisio, E. (2005). In vitro inhibition of human cGMP-specific phosphodiesterase-5 by polyphenols from red grapes. JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY, 53 (6): 1960-1965. doi: 10.1021/jf048497+ handle: http://hdl.handle.net/10449/16274

In vitro inhibition of human cGMP-specific phosphodiesterase-5 by polyphenols from red grapes

Vrhovsek, Urska;Mattivi, Fulvio;
2005-01-01

Abstract

A moderate consumption of red wine may reduce the risk of cardiovascular diseases via wine-derived phenolic compounds. A variety of biological mechanisms have been proposed for wine-derived phenolic compounds including nitric oxide-mediated vasorelaxation. This study examined whether the vasodilating effect of wine-derived phenolic compounds was associated with the inhibition of phosphodiesterases (PDEs) and, in particular, PDE5. For this purpose, human recombinant PDE5A1 isoform was prepared by expression of the full-length cDNA of PDE5A1 into COS-7 cells. Red wine and the extracts from grape skin inhibited PDE5A1 activity, whereas the seed extracts had a negligible effect. The mixture of anthocyanins inhibited the enzyme activity (IC50 = 11.6 μM), with malvidin-3-O-β-glucoside (IC50 = 35.4 μM) and malvidin (IC50 = 24.9 μM) the most potent among the monoglucosides and aglycons, respectively. trans-Resveratrol and trans-piceid exhibited negligible effects, whereas hydroxycinnamates were completely inactive. These results indicate that polyphenols-induced vasorelaxation may also be sustained by smooth muscle PDE inhibition by anthocyanins present in red wines and grapes
Settore CHIM/10 - CHIMICA DEGLI ALIMENTI
2005
Dell'Agli, M.; Galli, G.V.; Vrhovsek, U.; Mattivi, F.; Bosisio, E. (2005). In vitro inhibition of human cGMP-specific phosphodiesterase-5 by polyphenols from red grapes. JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY, 53 (6): 1960-1965. doi: 10.1021/jf048497+ handle: http://hdl.handle.net/10449/16274
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