Study of Anti-Aggregate and Antithrombotic Effects of 11-Amino Acid Derivatives of Erythropoetin Obtained Using Blast Screening

Корокин, М. В.; Antsiferov, O.V.; Gureeva, Anastasia V.; Солдатов, Владислав О.; Корокина, Л. В.; Krupenkina, L.A.; Авдеева, Е В

doi:10.17513/spno.30454

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“…The possibility to give them additional properties by modifying the polypeptide chain, in particular, the antiplatelet activity with the cytoprotective activity remaining at the same level, is of major importance (Golubev et al 2020b;Gureev et al 2020;Korokin et al 2020b;Puchenkova et al 2020). For the study, we selected a polypeptide EP-11-1 (UEHLERALNSS), which has antiplatelet and cytoprotective activities (Antsiferov et al 2020;Korokin et al 2020c;Korokin et al 2021).…”

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confidence: 99%

A new EPOR/CD131 heteroreceptor agonist EP-11-1: a neuroprotective effect in experimental traumatic brain injury

Antsiferov¹,

Cherevatenko²,

Корокин³

et al. 2021

RRP

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Introduction: EP-11-1 (UEHLERALNSS) is a short-chain erythropoietin derivative without have erythropoietic activity. It was created by modifying a peptide mimicking the spatial structure of the erythropoietin a-helix B pHBSP. One of the promising directions of its administration is the correction of morphofunctional disorders that occur in traumatic brain injury (TBI). Materials and methods: The study was performed in 160 male Wistar rats, weighing 180–200 g.TBI was simulated using the drop-weight method. To assess the emerging morphofunctional disorders and a degree of their correction, we used the severity of neurological deficit, indicators of locomotor activity and exploration, a marker of brain injury S100B and morphological examination. Results and discussion: The combined administration of a new EPOR/CD131 heteroreceptor agonist EP-11-1 with citicoline and trimetazidine led to a more pronounced correction of the neurological deficit when compared not only to the group of the ”untreated” animals, but also to the groups of animals to which these drugs had been administered as monotherapy (p < 0.05). The same tendency was also observed in the study of locomotor activity and exploration. A biochemical study showed that the administration of all three combinations led to a statistically significant (p < 0.05) decrease in the S-100B concentration compared not only to the group of “untreated” animals, but also to the groups of animals to which these drugs had been administered as a monotherapy. Conclusion: The results of the conducted experiments prove the most pronounced positive dynamics in the combined administration of the new EPOR/CD131 heteroreceptor agonist EP-11-1with citicoline and trimetazidine.

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