[Semax and selank inhibit the enkephalin-degrading enzymes from human serum]].
Kost. N V NV; Sokolov. O Iu OIu; Gabaeva. M V MV; Grivennikov. I A IA; Andreeva. L A LA; Miasoedov. N F NF; Zozulia. A A AA
Key Findings
- Semax inhibits enkephalinâdegrading enzymes with an IC50 of ~10âŻÂ”M; Selank does so with an IC50 of ~20âŻÂ”M
- Both peptides are more potent inhibitors than common peptidase blockers like puromycin (IC50âŻââŻ10âŻmM)
- Pentapeptide fragments of semax and selank also inhibit the enzymes, while shorter or longer fragments do not
Practical Outcomes
- The main takeaway is that semax and selank may boost levels of natural regulatory peptides by slowing their breakdown, which could contribute to their reported moodâenhancing or stressâreducing effects. However, because the data are from isolated serum enzymes, you canât directly translate this into dosing guidelines or guaranteed benefits without further inâvivo research.
Summary
The study shows that the brainâactive peptides semax and selank can block enzymes in human blood that break down natural opioidâlike compounds, doing so at fairly low concentrations. This suggests a possible way these peptides work, but the work was done in a testâtube, not in people, so it doesnât tell you how to dose or what effects to expect in real life.
Abstract
A dose-dependent effect of synthetic heptapeptides Semax (Met-Glu-His-Phe-Pro-Gly-Pro) and Selank (Thr-Lys-Pro-Arg-Pro-Gly-Pro) on the enkephalin-degrading enzymes of human serum was demonstrated. The inhibitory effects of Semax (IC50 10 microM) and Selank (IC50 20 microM) are more pronounced than those of puromycin (IC50 10 mM), bacitracin, and some other inhibitors of peptidases. Beside the heptapeptides, their pentapeptide fragments also possessed an inhibitory effect; tri-, tetra-, and hexapeptide fragments did not display such an effect. As the above enzymes take part in degradation of not only enkephalins but also other regulatory peptides, it can be assumed that one of the mechanisms of biological activity of Semax and Selank is related to this inhibitory activity of theirs.
Study Information
pubmed
2001
10.1023/a:1011373002885