Anthocyanin supplementation improves HDL-associated paraoxonase 1 activity and enhances cholesterol efflux capacity in subjects with hypercholesterolemia

J Clin Endocrinol Metab. 2014 Feb;99(2):561-9. doi: 10.1210/jc.2013-2845. Epub 2013 Nov 27.


Context and objective: Paraoxonase 1 (PON1), an enzyme associated with high-density lipoprotein (HDL-PON1), is reported to have antioxidant and cardioprotective properties. The aim of the present study was to investigate the effects of anthocyanins on the HDL-PON1 activity and cholesterol efflux capacity in hypercholesterolemic subjects.

Design and participants: A total of 122 hypercholesterolemic subjects were given 160 mg of anthocyanins twice daily or placebo (n = 61 of each group) for 24 weeks in a double-blind, randomized, placebo-controlled trial. Participants and investigators were masked to treatment allocation.

Results: Anthocyanin consumption significantly increased HDL cholesterol and decreased low -density lipoprotein cholesterol concentrations compared with placebo (P < .018 and P < .001, respectively). Anthocyanin supplementation also increased the activity of HDL-PON1 compared with placebo (P < .001). Furthermore, cholesterol efflux capacity was increased more in the anthocyanin group (20.0% increase) than in the placebo group (0.2% increase) (P < .001). The negative correlations established between HDL-PON1 activity and the levels of lipid hydroperoxides associated with HDL confirm the relationship between PON1 activity and lipid peroxidation of lipoproteins. Furthermore, a strong positive correlation was noted between increased HDL-PON1 activity and improved cholesterol efflux capacity both before and after adjustment for HDL cholesterol and apolipoprotein AI in anthocyanin-treated subjects (both P < .001). Inhibition of HDL-PON1 activity strongly prevented the antioxidant ability of HDL and attenuated the cholesterol efflux capacity of subjects from anthocyanin group.

Conclusions: Our observations suggest that the alterations of PON1 activity by anthocyanin observed in hypercholesterolemic HDL reflect a shift to an improvement of cholesterol efflux capacity of HDL and may provide a link between anthocyanin and cardioprotective effects.

Publication types

  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anthocyanins / therapeutic use*
  • Aryldialkylphosphatase / metabolism*
  • Cholesterol / blood*
  • Cholesterol, HDL / blood
  • Dietary Supplements*
  • Double-Blind Method
  • Female
  • Humans
  • Hypercholesterolemia / blood
  • Hypercholesterolemia / drug therapy*
  • Hypercholesterolemia / enzymology
  • Male
  • Middle Aged


  • Anthocyanins
  • Cholesterol, HDL
  • Cholesterol
  • Aryldialkylphosphatase