Phenolics from grapefruit peels inhibit HMG-CoA reductase and angiotensin-I converting enzyme and show antioxidative properties in endothelial EA.Hy 926 cells

Abstract

This study sought to investigate the possible mechanisms for the use of phenolic extracts from grapefruit peels in the management/prevention of cardiovascular complications. The effects of the phenolic extracts on key enzymes relevant to cardiovascular diseases [3-hydroxy-methyl-3-glutaryl coenzyme A reductase (HMG-CoA reductase) and angiotensin-I converting enzyme (ACE)], cellular antioxidant activity in human endothelial cells (EA.Hy 926) and radicals [1,1-diphenyl-2 picrylhydrazyl (DPPH) and 2,2′-azino-bis(3-ethylbenzthiazoline-6-sulphonic acid) (ABTS)] scavenging abilities were investigated. The phenolic contents of the extracts were investigated using HPLC–DAD. There was no significant (P>0.05) difference in the HMG-CoA reductase inhibitory ability of the two extracts, while the bound phenolic extracts had a stronger ACE inhibitory ability than the soluble free phenolics. The extracts also showed intracellular antioxidant activity in human endothelial (EA.Hy 926) cells. Furthermore, the bound phenolics had significantly higher radicals (DPPH* and ABTS*) scavenging abilities than the free phenolics. The HPLC analysis revealed the presence of flavonoids (quercetin and kaempferol), phenolics acids (resveratrol, gallic acid, ellagic acid and caffeic acid) and tannin (catechin). The cellular antioxidative properties and inhibition of enzymes relevant to the management of cardiovascular complications showed that grapefruit peels could be used as nutraceuticals for the management of such conditions.