Probucol in concentrations of 10-50/aM effectively inhibits CuZ+-induced free radical oxidation of native low density lipoproteins and in concentration of 100 ~tM it inhibits lipoperoxide formation. The mean plasma concentration of probucol in patients receiving 250 mg of this drug is 25 ~tM. Both 250 and 1000 mg probucol daily during 3-6 month block the oxidation of isolated low density lipoproteins. Electron paramagnetic resonance spectrometry data showed that probucol incorporated in vivo into lipoprotein particles interacts with lipid radicals yielding long-lived phenoxyradicals. Probucol can be used in complex therapy of atherosclerosis as an antioxidant drug and its dose required for lipoprotein protection against atherogenic modification can be decreased to 250 mg/day.
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