The invention relates to a synergistic composition of naturally occurring substances, which is particularly effective in the treatment of hypercholesterolemia. The composition of the invention comprises at least one substance having 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitory activity, a substance having cytochrome CYP7A1 expression increasing activity, a substance having inhibitory activity against the enzyme Acyl-CoA: cholesterol acyltransferase ACAT1 and ACAT2 isoforms, procyanidins, and optionally, coenzyme Q10 and phytosterols.