Abstract: 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.

Keywords: polyphenols; grape seed; mechanism pancreatic cholesterol esterase; cholesterol micelles; bile acid

Molecules 2011, 16(6), 5054-5061; doi:10.3390/molecules16065054

Sathaporn Ngamukote 1,2,3, Kittana Mäkynen 1,2,3, Thavaree Thilawech 1,2,3 and Sirichai Adisakwattana 1,2,3,* 

- Authors' affiliations 1 The Medical Food Research and Development Center, Department of Transfusion Medicine, Faculty of Allied Health Sciences, Chulalongkorn University, Bangkok, Thailand2 Program in Nutrition and Dietetics, Faculty of Allied Health Sciences, Chulalongkorn University, Bangkok, Thailand3 The Research Group of Herbal Medicine for Prevention and Therapeutic of Metabolic Diseases, Chulalongkorn University, Bangkok, Thailand

* Author to whom correspondence should be addressed.

Received: 8 April 2011; in revised form: 13 June 2011 / Accepted: 16 June 2011 / Published: 17 June 2011 (This article belongs to the Section Natural Products)

Originally published on http://www.mdpi.com/1420-3049/16/6/5054