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In vitro inhibition of human cGMP-specific phosphodiesterase-5 by polyphenols from red grapes.
J Agric Food Chem. 2005 Mar 23; 53(6):1960-5.JA

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 microM), with malvidin-3-O-beta-glucoside (IC50 = 35.4 microM) and malvidin (IC50 = 24.9 microM) 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.

Authors+Show Affiliations

Department of Pharmacological Sciences, Faculty of Pharmacy, University of Milan, via Balzaretti 9, 20133 Milan, Italy. mario.dellagli@unimi.itNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

15769121

Citation

Dell'Agli, Mario, et al. "In Vitro Inhibition of Human cGMP-specific Phosphodiesterase-5 By Polyphenols From Red Grapes." Journal of Agricultural and Food Chemistry, vol. 53, no. 6, 2005, pp. 1960-5.
Dell'Agli M, Galli GV, Vrhovsek U, et al. In vitro inhibition of human cGMP-specific phosphodiesterase-5 by polyphenols from red grapes. J Agric Food Chem. 2005;53(6):1960-5.
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), 1960-5.
Dell'Agli M, et al. In Vitro Inhibition of Human cGMP-specific Phosphodiesterase-5 By Polyphenols From Red Grapes. J Agric Food Chem. 2005 Mar 23;53(6):1960-5. PubMed PMID: 15769121.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - In vitro inhibition of human cGMP-specific phosphodiesterase-5 by polyphenols from red grapes. AU - Dell'Agli,Mario, AU - Galli,Germana V, AU - Vrhovsek,Urska, AU - Mattivi,Fulvio, AU - Bosisio,Enrica, PY - 2005/3/17/pubmed PY - 2005/4/29/medline PY - 2005/3/17/entrez SP - 1960 EP - 5 JF - Journal of agricultural and food chemistry JO - J Agric Food Chem VL - 53 IS - 6 N2 - 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 microM), with malvidin-3-O-beta-glucoside (IC50 = 35.4 microM) and malvidin (IC50 = 24.9 microM) 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. SN - 0021-8561 UR - https://www.unboundmedicine.com/medline/citation/15769121/In_vitro_inhibition_of_human_cGMP_specific_phosphodiesterase_5_by_polyphenols_from_red_grapes_ L2 - https://doi.org/10.1021/jf048497+ DB - PRIME DP - Unbound Medicine ER -