Comparative analysis of the hypocholesterolemic and antithrombotic action of small regulatory glyproline peptides (Pro-Gly-Pro, Arg-Pro-Gly-Pro and Pro-Gly-Pro-Leu) was performed on an experimental hypercholesterolemia model of rats. Repeated intranasal introduction of glyproline peptides to fat-diet-fed animals led to more active functioning of the anticoagulation system (the anticoagulant and fibrinolytic properties of the plasma increased and platelet aggregation decreased) and to normalization of the total cholesterol level as a parameter of lipid metabolism. The largest anticoagulant and hypocholesterolemic effect was detected for the Pro-Gly-Pro-Leu peptide. Hypothetical mechanisms of antithrombotic and hypocholesterolemic effects of glyproline peptides are presented.