A comparative study of the in vitro antioxidant activity of statins.
BACKGROUND
Treatment of hypercholesterolemia with statins is remarkably effective in cardiovascular prevention. This has led to the hypothesis that these drugs may act on the atherosclerotic plaque by mechanism(s) independent of the reduction of serum cholesterol levels. The aim of this study was to assess the total antioxidant activity of the most prescribed statins: fluvastatin, atorvastatin, pravastatin and simvastatin.


METHODS
We measured the in vitro antioxidant activity of statins as their ability to antagonize the oxidation of alpha-keto-gamma-methiolbutyric acid by both hydroxyl and peroxyl radicals. The results are expressed as Total Oxyradical Scavenging Capacity (TOSC) units. Uric acid and Trolox were used as the reference antioxidants.


RESULTS
The scavenging capacity towards hydroxyl radicals was highest for simvastatin (3375+/-112 U/mg), a value 270.2% higher (P<0.0001) compared to uric acid (reference antioxidant vs. hydroxyl radicals, 1249+/-71 U/mg). Among the tested statins, fluvastatin exhibited the highest anti-peroxyl radical antioxidant capacity (8755+/-187 U/mg) which appeared 50% lower (P<0.0001) compared to Trolox (reference antioxidant vs. peroxyl radicals, 17460+/-379 U/mg).


CONCLUSIONS
All the statins tested have intrinsic antioxidant activity with both anti-hydroxyl and peroxyl radical activity. Simvastatin was the most effective as an anti-hydroxyl radical antioxidant and fluvastatin as an anti-peroxyl radical antioxidant.
Franzoni
Ferdinando
F
Department of Internal Medicine, University of Pisa School of Medicine, Via Roma, 67, 56100 Pisa, Italy.
Quiñones-Galvan
Alfredo
A
Regoli
Francesco
F
Ferrannini
Ele
E
Galetta
Fabio
F
D000704:Analysis of Variance; D000924:Anticholesteremic Agents / Q000494:pharmacology*; D016166:Free Radical Scavengers / Q000494:pharmacology*; D006801:Humans; D017665:Hydroxyl Radical / Q000378:metabolism*; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors / Q000494:pharmacology*; D006937:Hypercholesterolemia / Q000188:drug therapy*; D010545:Peroxides / Q000378:metabolism*
D000924:Anticholesteremic Agents; D016166:Free Radical Scavengers; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors; D010545:Peroxides; C049375:perhydroxyl radical; D017665:Hydroxyl Radical