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[Effect of new peptide bioregulators livagen and epitalon on enkephalin-degrading enzymes in human serum]

Study · human · Izvestiia Akademii nauk. Seriia biologicheskaia · 2003 · PMID 12942748

Plain-language summary

Paraphrased from the published abstract below — not a verdict on whether anything works.

This in vitro study examined the peptides Livagen (Lys-Glu-Asp-Ala) and Epitalon (Ala-Glu-Asp-Gly) for their action on enkephalin-degrading enzymes in human serum and on opioid receptors from rat brain membranes. Enkephalinase activity was assayed by the rate of 3H-Leu-enkephalin hydrolysis. The authors report that both peptides inhibited the human-serum enzymes, that Livagen showed greater inhibition than the comparison peptidase inhibitors puromycin, leupeptin, and D-PAM, and that the IC50 values were 20 and 500 microM for Livagen and Epitalon respectively. Using a radioreceptor method, they observed no interaction between the peptides and mu- or delta-opioid receptors of the rat brain membrane fraction.

Abstract

The effect of new peptide bioregulators--Livagen (Lys-Glu-Asp-Ala) and Epitalon (Ala-Glu-Asp-Gly)--on endogenous opioid system was studied, particularly, their ability to change the activity of enkephalin-degrading enzymes from serum and interact with opioid receptors of the brain membrane fraction. Enkephalinase activity was assayed in vitro by the rate of 3H-Leu-enkephalin hydrolysis in the presence of the tested peptides. Livagen and Epitalon inhibited enkephalin-degrading enzymes from human serum. Livagen proved to be more efficient also as compared to well-known peptidase inhibitors such as puromycin, leupeptin, and D-PAM. The dose-inhibitory effect curves for Livagen and Epitalon were plotted; their IC50 equaled 20 and 500 microM, respectively. The interaction between the peptides and opioid receptors was estimated using a radioreceptor method with [3H][D-Ala2, D-Leu5]-enkephalin. No interaction was observed between the tested peptides and mu- or delta-opioid receptors of the membrane fraction from the rat brain.

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