[Action of proteolytic enzymes from the cytosol of human erythrocytes on tuftsin, the peptide activator of phagocytosis].
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The results presented in this paper revealed high or moderate activity of ten out of nineteen amino acids tested. Strong activity stimulating phagocytosis was noted in the presence of leucine, isoleucine, proline, arginine and histidine; moderate in the presence of serine, cysteine, hydroxyproline, aspartic acid and glutamic acid. Alanine, glycine, valine, threonine, phenylalanine, tyrosine, tryptophan, methionine and lysine did not stimulate phagocytic activity of PMN.
The effect of the tetrapeptide tuftcin (Thr-Lys-Pro-Arg) on the humoral immune response in CBA mice exposed to sublethal irradiation in a dose of 450 sGy was studied. The drug was injected intraperitoneally for 5 days before (series I) or after (series II) radiation exposure. It has been shown that taftcin has no protective action but decreases considerably the immune response lowering due to radiation.
The cytochemical technique was used to measure the activity of succinate dehydrogenase (SDH), lactate dehydrogenase (LDH) and glucose-6-phosphate dehydrogenase (G-6-PDH) of peripheral blood lymphocytes of mice and rats given intraperitoneal injections of an endogenous immunostimulant tuftcin (Tre-Lys-Pro-Arg) in a dose of 0.3 mg/kg. A significant decrease of SDH activity was observed both in mice and rats 4 and 6 hours following injection, respectively. In mice, that activity returned to normal in 12, while in rats in 24 hours. An opposite action was produced by tuftcin on G-6-PDH, causing the maximum elevation of the enzyme activity in rat lymphocytes 6 hours after peptide administration. The decrease to the initial level was observed in 24 hours. Tuftcin did not affect the activity of LDH. The data obtained indicate that the immunological effect of tuftcin is coupled with the changes in the activity of Krebs cycle enzymes (SDH) and pentose phosphate cycle enzymes (G-6-PDH).
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The pharmacokinetics of a new heptapeptide with psychotropic activity was studied in rats in experiments in vitro and in vivo by means of high-performance liquid chromatography. The heptapeptide was detected in its natural form in rat blood plasma for 7-10 min; its T1/2 exceeded that of other oligopeptides of similar structure. The structure of the main pharmacologically active heptapeptide metabolite was identified by high performance liquid chromatography; it proved to be tetrapeptide Thr-Lys-Pro-Arg (taphtsin). The heptapeptide was distributed in well vascularized organs of rats: liver > kidneys > heart.
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