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肽链缩短的环脂肽A类似物的合成及生物学研究

Synthesis and biological studies on analogs of cyclolinopeptide A with a shortened peptide chain.

作者信息

Siemion I Z, Pedyczak A, Strug I, Wieczorek Z

机构信息

Institute of Chemistry, Wrocław University, Poland.

出版信息

Arch Immunol Ther Exp (Warsz). 1994;42(5-6):459-65.

PMID:8572907
Abstract

Continuing our work on the immunosuppressive activity of cyclolinopeptide A (CLA), a cyclic nonapeptide of the sequence: c-(-Leu-Ile-Ile-Leu-Val-Pro-Pro-Phe-Phe), we synthesized a series of 6 linear analogs of CLA, successively shortened at the N-terminus of the peptide chain. Immunosuppressive activity of acetates as well as trifluoroacetates of these peptides was investigated using PFC (humoral immunity) and DTH (cellular immunity) tests. It was found that the immunosuppressive potency of the peptides examined diminishes with shortening of the peptide chain. Octapeptide I with the sequence Ile-Ile-Leu-Val-Pro-Pro-Phe-Phe was found to be the most active of the whole series. The immunosuppressive activity increased again for a tripeptide fragment of CLA of the sequence Pro-Phe-Phe. The immunosuppressive activity of octapeptide probably depends on the suppression of IL-1, IL-6 and TNF production by the cells involved in immune and inflammatory response.

摘要

继续我们关于环脂肽A(CLA)免疫抑制活性的研究工作,CLA是一种环状九肽,其序列为:c-(-Leu-Ile-Ile-Leu-Val-Pro-Pro-Phe-Phe),我们合成了一系列CLA的6种线性类似物,肽链的N端依次缩短。使用PFC(体液免疫)和DTH(细胞免疫)试验研究了这些肽的乙酸盐和三氟乙酸盐的免疫抑制活性。结果发现,所检测肽的免疫抑制效力随着肽链的缩短而降低。序列为Ile-Ile-Leu-Val-Pro-Pro-Phe-Phe的八肽I被发现是整个系列中活性最高的。CLA序列为Pro-Phe-Phe的三肽片段的免疫抑制活性再次增加。八肽的免疫抑制活性可能取决于对参与免疫和炎症反应的细胞产生IL-1、IL-6和TNF的抑制作用。

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Molecules. 2021 Apr 27;26(9):2538. doi: 10.3390/molecules26092538.
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Anti-Inflammatory Activity of a Cyclic Tetrapeptide in Mouse and Human Experimental Models.一种环四肽在小鼠和人类实验模型中的抗炎活性
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