Polyphenolic composition of alcohol-free red wine concentrates (AFRWC) was determined by LC-MS/MS. The concentration of salicylic acid in non-flavonoid class and malvidin in flavonoid class was the highest among all the polyphenols determined in AFRWC. In the in vitro model using HepG2 cells, AFRWC was found to be more effective for the reduction of total cholesterol than lovastatin. For the in vivo model, animals were provided with AFRWC at similar to 750 mg of total polyphenols/kg body weight per day by oral administration. The amount of AFRWC was established by extrapolation to be equivalent to 375 ml/day wine consumption, which is similar to 2-3 glasses of wine per day for a 60 kg human. Despite a high cholesterol diet, a significant reduction in both total cholesterol and LDL-cholesterol was observed when supplemented with AFRWC, but the increase of HDL-cholesterol was not observed. The expression level of mRNA of some hepatic genes participating in cholesterol biosynthesis, cholesterol esterification was found to be influenced by AFRWC supplementation, whereas reverse cholesterol transport involved with HDL-cholesterol was seldom affected showing discrepancy in the expression of associated genes. (C) 2013 Published by Elsevier Ltd.