Tetrapeptide Pro-Gly-Pro-Leu in vitro effectively inhibited platelet aggregation over the entire range of studied concentrations (10(-12)-10(-3) M). In concentrations of 10(-9)-10(-3) M it exhibits fibrinolytic activity and in concentrations of 10(-5)-10(-3) M has anticoagulant properties. Under in vivo conditions the analyzed tetrapeptide in a dose of 1 mg/kg increased anticoagulant, total and fibrin depolymerizating activities and increased activity of plasminogen activator. Intravenous administration produced more pronounced anticoagulant effect and leads to a greater increase in activity of plasminogen activator than intranasal administration. Tetrapeptide Pro-Gly-Pro-Leu also exerts antithrombotic effect. Preliminary repeated intranasal administration of the peptide before blood clot formation reduces the weight of fresh fibrin clots.
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Proteolysis of Pro-Gly-Pro-Leu in the hippocampus, cerebellum, and cerebral cortex in rats after intravenous injection.
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November 2014
Department of Chemistry of Physiologically Active Substances, Institute for Molecular Genetics, Russian Academy of Science, Moscow, Russia,
We studied the dependence of the levels of Pro-Gly-Pro-Leu peptide and its metabolites (Gly-Pro-Leu, Pro-Gly-Pro, Gly-Pro and Pro-Gly) from the time of administration in the hippocampus, cerebellum, and cerebral cortex of rats. After intravenous injection of Pro-Gly-Pro-Leu, the maximum concentration of metabolites in the rat brain was found in 20-min sample (0.026% from the amount of introduced labeled tetrapeptide); it was by 2.
View Article and Find Full Text PDFHypoglycemic and anticoagulant effects of tetrapeptide Pro-Gly-Pro-Leu in hypercholesterolemia.
Bull Exp Biol Med
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Laboratory of Blood Protective Systems, Biological Faculty, M. V. Lomonosov Moscow State University, Moscow, Russia,
In rats with experimental hypercholesterolemia, 7-fold intranasal administration of the peptide Pro-Gly-Pro-Leu in a dose of 200 μg/kg body weight prevented the increase in blood glucose level and produced an anticoagulant effect.
View Article and Find Full Text PDFThe experimental data on the therapeutic and prophylactic antidiabetogenic effect of di-, tri-, and tetrapeptides of the glyproline family with the additional inclusion of arginine or leucine at different positions are presented. The results are obtained using two animal models: with insulin-dependent diabetes mellitus (type 1), and persistent hyperglycemia similar to development of non-insulin-dependent diabetes mellitus (type 2) in humans. It is shown that repeated intranasal administration of Pro-Gly, Pro-Gly-Pro, Pro-Gly-Pro-Arg, Pro-Gly-Arg, Arg-Pro-Gly, Arg-Pro-Gly-Pro, Gly-Pro-Arg, Pro-Arg-Gly, Pro-Gly-Pro-Leu, Leu-Pro-Gly-Pro peptides to rats with hyperglycemia of different etiology led to the combined normoglycemic and anticoagulant effects in the blood plasma.
View Article and Find Full Text PDFIn the present paper anticoagulant-fibrinolytic effects of the peptide Pro-Gly-Pro-Leu in rats (370-500 g body weight) who consumed fatty foods with excess of saturated fatty acids (wheat flour and bread--35%, sugar--10%, margarine hydrogenated fats, mayonnaise, cheese--35% and offals--10%, cholesterol--1%, dry food--9%) has been established. The duration of the animals on the diet was 15 days. The experimental animals intranasally obtained peptide (200 microg/kg body weight per volume of 0.
View Article and Find Full Text PDFEffects of peptide Pro-Gly-Pro-Leu under conditions of normal hemostasis and thrombus formation in rats.
Bull Exp Biol Med
December 2011
Department of Human and Animal Physiology, Biological Faculty, M. V. Lomonosov Moscow State University, Russia.
Tetrapeptide Pro-Gly-Pro-Leu in vitro effectively inhibited platelet aggregation over the entire range of studied concentrations (10(-12)-10(-3) M). In concentrations of 10(-9)-10(-3) M it exhibits fibrinolytic activity and in concentrations of 10(-5)-10(-3) M has anticoagulant properties. Under in vivo conditions the analyzed tetrapeptide in a dose of 1 mg/kg increased anticoagulant, total and fibrin depolymerizating activities and increased activity of plasminogen activator.
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