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Anthocyanin supplementation improves serum LDL- and HDL-cholesterol concentrations associated with the inhibition of cholesteryl ester transfer protein in dyslipidemic subjects^1,2,3,4

¹ From the Departments of Nutrition (YQ, MX, JM, JL, HYM, LC, and WHL) and Statistics (YTH), School of Public Health, Sun Yat-Sen University (Northern Campus), Guangzhou, China.

² YQ and MX contributed equally to this work.

³ Supported by research grants from the National Natural Science Foundation of China (30730079) and the China Medical Board of New York Inc (CMB 98-677). The treated capsules, including the anthocyanin (Medox) and the placebo, were gifts from Polyphenols AS (Sandnes, Norway).

⁴ Address correspondence to WH Ling, Department of Nutrition, School of Public Health, Sun Yat-Sen University (Northern Campus), 74 Zhongshan Road 2, Guangzhou, Guangdong Province 510080, Peoples Republic of China. E-mail: lingwh{at}mail.sysu.edu.cn.

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-β-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.