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具有造血活性的新型拟肽环-{E(I)-E(W)}Na(CP-88)在侵入性给药和口服给药中的活性维持:实验和临床前评估

Novel Peptidomimetic Cyclo-{E(I)-E(W)}Na (CP-88) with Hematopoietic Activity Sustained in Invasive and Oral Administration: Experimental and Preclinical Evaluation.

作者信息

Deigin Vladislav, Vinogradova Yulia, Vinogradov Dmitriy, Linkova Natalia, Dyatlova Anastasiia, Medvedev Dmitrii, Krasichkov Alexander, Polyakova Victoria

机构信息

Institute of Bioorganic Chemistry, Russian Academy of Sciences, Miklukho-Maklaya St., 16/10, 117997 Moscow, Russia.

The Department of Hospital Therapy No. 2, I.M. Sechenov First Moscow State Medical University, 8 Trubetskaya Str., 119048 Moscow, Russia.

出版信息

Int J Mol Sci. 2024 Dec 13;25(24):13385. doi: 10.3390/ijms252413385.

Abstract

Over the last decades, significant progress has been made in studying agonistic and antagonistic hematopoietic peptides. The main disadvantage of this class of peptides is their low stability with noninvasive administration methods, which limits the widespread use of hematopoiesis-regulated peptide drugs in medical practice. The aim of this work is to study novel peptidomimetics with hematopoietic activity sustained in invasive and oral administration. The activity of the leading compound cyclopeptide Cyclo-[Glu(Ile)-Glu(Trp)] (CP-88) was compared to that of the pharmaceutical preparation Stemokin in stimulating the population of committed colony-forming cells in intact and irradiated mice. CP-88 peptide increases the relative number of CD34+ cells in the blood and bone marrow, leading to expanded hematopoietic stem cells. CP-88 peptide, applied 48 h before bone marrow extraction, stimulates the population of committed colony-forming cells in the normal bone marrow by 33-37% above the normal level. In recipient mice injected with irradiated bone marrow, this peptide was restored practically to normal levels of colony-forming cells in a wide range of doses at intraperitoneal and oral administration. The toxicological results conclude that in humans, considering interspecies extrapolation, the CP-88 peptide can be practically safe with a single and course administration in doses of up to 100 μg/kg. The results of this investigation underscore the significant potential of CP-88 peptide as a hematopoiesis-regulated drug and instill optimism for its future application in medical practice.

摘要

在过去几十年中,在研究激动性和拮抗性造血肽方面取得了重大进展。这类肽的主要缺点是在非侵入性给药方法下稳定性较低,这限制了造血调节肽药物在医学实践中的广泛应用。这项工作的目的是研究在侵入性和口服给药后具有持续造血活性的新型肽模拟物。将先导化合物环肽Cyclo-[Glu(Ile)-Glu(Trp)](CP-88)与药物制剂Stemokin在刺激完整和受辐照小鼠中定向集落形成细胞群体方面的活性进行了比较。CP-88肽增加了血液和骨髓中CD34+细胞的相对数量,从而导致造血干细胞扩增。在骨髓提取前48小时应用CP-88肽,可使正常骨髓中定向集落形成细胞群体比正常水平高出33%-37%。在注射了辐照骨髓的受体小鼠中,该肽在腹腔内和口服给药的广泛剂量范围内,集落形成细胞水平实际上恢复到了正常水平。毒理学结果表明,在人类中,考虑到种间外推,CP-88肽在单次和疗程给药剂量高达100μg/kg时几乎是安全的。这项研究结果强调了CP-88肽作为造血调节药物的巨大潜力,并为其未来在医学实践中的应用注入了乐观情绪。

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