Abstract
We have synthesized the peptide TPLVTLFK corresponding to β-endorphin fragment 12–19 (dubbed octarphin) and its analogs (LPLVTLFK, TLLVTLFK, TPLVLLFK, TPLVTLLK, TPLVTLFL). The octarphin peptide was labeled with tritium (specific activity 28 Ci/mol), and its binding to murine peritoneal macrophages was studied. [3H]Octarphin was found to bind to macrophages with high affinity (K d = 2.3 ± 0.2 nM) and specificity. The specific binding of [3H]octarphin was inhibited by unlabeled β-endorphin and the selective agonist of nonopioid β-endorphin receptor synthetic peptide immunorphin (SLTCLVKGFY) (K i = 2.7 ± 0.2 and 2.4 ± 0.2 nM, respectively) and was not inhibited by unlabeled nalox-one, α-endorphin, γ-endorphin, or [Met5]enkephalin (K i > 10 μM). Inhibitory activity of unlabeled octarphin analogs was more than 100 times lower than that of unlabeled octarphin. Octarphin was shown to stimulate activity of murine immuno-competent cells in vitro and in vivo: at concentration of 1–10 nM it enhanced the adhesion and spreading of peritoneal macrophages as well as their ability to digest bacteria of Salmonella typhimurium virulent strain 415 in vitro; the peptide administered intraperitoneally at a dose of 20 μg/animal on day 7, 3, and 1 prior to isolation of cells increased activity of peritoneal macrophages as well as spleen T- and B-lymphocytes.
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Abbreviations
- Con A:
-
concanavalin A
- CPE:
-
cytopathic effect of bacteria
- LPS:
-
lipopolysaccharide
- PA:
-
phagocytic activity
- PN:
-
phagocytic number
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Original Russian Text © Yu. A. Kovalitskaya, Yu. N. Nekrasova, V. B. Sadovnikov, Yu. A. Zolotarev, E. V. Navolotskaya, 2011, published in Biokhimiya, 2011, Vol. 76
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Kovalitskaya, Y.A., Nekrasova, Y.N., Sadovnikov, V.B. et al. Immunostimulating effect of the synthetic peptide octarphin corresponding to β-endorphin fragment 12–19. Biochemistry Moscow 76, 596–604 (2011). https://doi.org/10.1134/S0006297911050105
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DOI: https://doi.org/10.1134/S0006297911050105