Inhibitory effect of phenolic compounds from grape seeds (Vitis vinifera L.) on the activity of angiotensin I converting enzyme

Inhibition of the angiotensin I converting enzyme (ACE) is an important therapeutic approach in the treatment of several cardiovascular disorders. In this study the inhibitory potential of procyanidin-rich fractions of grape seed (Vitis vinifera L.) was evaluated. The inhibitory capacity was assayed by fluorometric determination of the amount of histidyl-leucine released from the substrate utilized in the presence of ACE from rabbit lung. Four purified monomers [(+)-catechin, (−)-epicatechin, (+)-catechin-O-gallate, and (−)-epigallocatechin] were also tested for comparison. Results showed that the natural phenolic extracts exhibit higher inhibitory potential than the monomers, and that fractions with higher average degrees of polymerization (DPn = 8, IC50 = 0.1 mg/L) present lower IC50 than the intermediate ones (DPn = 5, IC50 = 3.5 mg/L). Such findings strengthen the idea that the inhibitor extension, and the number of heterocyclic oxygen and hydroxyl groups in their structures, could define their in vitro action.