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 [(þ)-catechin, ()-epicatechin, (þ)-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 ¼ 8, IC50 ¼ 0.1 mg/L) present lower IC50 than the intermediate
ones (DPn ¼ 5, IC50 ¼ 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.
Inhibition of the angiotensin I converting enzyme (ACE) is an important therapeutic approach in thetreatment of several cardiovascular disorders. In this study the inhibitory potential of procyanidin-richfractions of grape seed (Vitis vinifera L.) was evaluated. The inhibitory capacity was assayed by fluorometricdetermination of the amount of histidyl-leucine released from the substrate utilized in thepresence of ACE from rabbit lung. Four purified monomers [(þ)-catechin, ()-epicatechin, (þ)-catechin-O-gallate, and ()-epigallocatechin] were also tested for comparison. Results showed that the naturalphenolic extracts exhibit higher inhibitory potential than the monomers, and that fractions with higheraverage degrees of polymerization (DPn ¼ 8, IC50 ¼ 0.1 mg/L) present lower IC50 than the intermediateones (DPn ¼ 5, IC50 ¼ 3.5 mg/L). Such findings strengthen the idea that the inhibitor extension, and thenumber of heterocyclic oxygen and hydroxyl groups in their structures, could define their in vitro action.
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