Anthocyanin supplementation improves serum LDL- and HDL-cholesterol concentrations associated with the inhibition of cholesteryl ester transfer protein in dyslipidemic subjects

Background: Anthocyanins have been shown to exert benefits on the lipid profile in many animal models. Whether these molecules have similar beneficial effects in humans is currently unknown. Objective: The objective was to investigate the effects of berry-derived anthocyanin supplements on the serum lipid profile in dyslipidemic patients. Design: A total of 120 dyslipidemic subjects (age 40-65 y) were given 160 mg anthocyanins twice daily or placebo for 12 wk in a double-blind, randomized, placebo-controlled trial. Results: Anthocyanin consumption increased HDL-cholesterol concentrations (13.7% and 2.8% in the anthocyanin and placebo groups, respectively; P < 0.001) and decreased LDL-cholesterol concentrations (13.6% and -0.6% in the anthocyanin and placebo groups, respectively; P < 0.001). Cellular cholesterol efflux to serum increased more in the anthocyanin group than in the placebo group (20.0% and 0.2%, respectively; P < 0.001). Anthocyanin supplementation decreased the mass and activity of plasma cholesteryl ester transfer protein (CETP) (10.4% and 6.3%, respectively, in the anthocyanin group and -3.5% and 1.1%, respectively, in the placebo group; P < 0.001). In the anthocyanin group, the change in HDL cholesterol was negatively correlated with the change in CETP activity (r(s) = -0.330). The change in LDL cholesterol was positively correlated with the change in CETP mass (r(s) = 0.354). The change in cellular cholesterol efflux to serum was positively correlated with the change in HDL cholesterol (r(s) = 0.485). In vitro, cyanidin 3-O-beta-glucosides dose-dependently lowered CETP activity in human HepG2 cells. Conclusions: Anthocyanin supplementation in humans improves LDL- and HDL-cholesterol concentrations and enhances cellular cholesterol efflux to serum. These benefits may be due to the inhibition of CETP. Am J Clin Nutr 2009;90:485-92.