胸腺肽α_1活性片段和其自旋标记衍生物的合成及免疫活性研究

Study of Synthesis and Immunofunction of Active Fragment of Thymosin α_1 and Its Spin Labelled Analog

报道了胸腺肽α_１活性片段Ｔｈｙｍｏｓｉｎα_１［Ｌｙｓ（２３）］（２３－２７）ＯＨ和其自旋标记衍生物的合成及对实验动物免疫功能的影响。其氨基酸序列分别为Ｈ_２Ｎ－Ｌｙｓ－Ｇｌｕ－Ｇｌｕ－Ａｌａ－Ｇｌｕ－ＯＨ，用Ｔｈｙα_１［Ｌｙｓ^（２３）］表示，修饰物为Ｇｌｕ－ＯＨ），用Ｔｈｙα_１［Ｌｙｓ^（２３）］·Ｒ表示。ＨＰＬＣ测得该肽的纯度在９０％以上，ＥＳＲ谱测定自旋标记衍生物给出氮氧自由基信号，氨基酸组成与预期值相符。实验小鼠腹腔连续注射剂量为０．１、１、１０、１００和１０００μｇ／ｋｇ的该肽１０天后，发现腹腔巨噬细胞吞噬功能、ＥＲＦＣ阳性率及血清溶血素含量明显升高，且最佳剂量在０．１－１０μｇ／ｋｇ范围。实验结果表明人工合成胸腺肽α_１活性片段及其自旋标记衍生物具有显著的免疫促进活性。

A fragment with bioactivity of thymosin α1 and its spin labelled analog with peptides sequences as K-E-E-A-E(Thy α_1[Lys￣(23)], ) , CO-K-E-E-A-E(Thy α1 [Lys￣(23)].R)were synthesized. These peptides were judged to be greater than 90% in purity using HPLC ,calculated values were in agreement with those obtained from AAA. The ESR spectrum of the spin labelled analog was obtained and showed nitroxide radical signal. The phagocytosis of macrophage ,E-rosette formation cells ,and content of hemolysin in mice serum were improved significantly by Thy α1[Lys23] and Thy α1 [Lys23] . R of 0. 1、1、10、100 and 1000 μg/kg . d for 10d after intraperitoneal injection. The optimal doses of these peptides might be 0.1-10 μg/kg. Results showed that the peptides have immunological competence.