Cholesterol-Lowering Activity of the Major Polyphenols in Grape Seed

• Main Authors: Sirichai Adisakwattana, Thavaree Thilawech, Kittana Mäkynen, Sathaporn Ngamukote
• Format: Article
• Language: English
• Published: MDPI AG 2011-06-01
• Series: Molecules
• Subjects: polyphenols; grape seed; mechanism pancreatic cholesterol esterase; cholesterol micelles; bile acid
• Online Access: http://www.mdpi.com/1420-3049/16/6/5054/

The major polyphenols in grape seed have been shown to have beneficial health effects in the prevention of dyslipidemia and cardiovascular diseases. In this present study, we investigated the cholesterol-lowering activity of three major polyphenolic compounds found in grape seed. The results showed that gallic acid, catechin, and epicatechin significantly inhibited pancreatic cholesterol esterase in a concentration-dependent manner. Moreover, they bound to taurocholic acid, taurodeoxycholic acid, and glycodeoxycholic acid at levels ranging from 38.6% to 28.2%. At the concentration of 0.2 mg/mL, gallic acid, catechin, and epicatechin reduced the formation of cholesterol micelles 27.26 ± 2.17%, 11.88 ± 0.75%, and 19.49 ± 3.71%, respectively. These findings clearly demonstrate that three major polyphenolic compounds present in a particular grape seed have cholesterol-lowering activity by inhibiting pancreatic cholesterol esterase, binding of bile acids, and reducing solubility of cholesterol in micelles which may result in delayed cholesterol absorption.