摘要
利用固相多肽合成中的 Boc和 Fmoc途径分别合成了胸腺素α1 (S- Tα1 )。后者的合成产率 (去保护基后粗肽量 /理论量 )为 80 % ,大于前者的 64.2 %。在 Fmoc方法合成中 ,用 Fmoc- Asn(Trt)上羟基树脂 (HMP树脂 )提高了合成产率。经 FPLC纯化后 ,Tα1 用 HPLC、毛细管电泳、等电聚焦电泳鉴定纯度均一 ;质谱和 N端序列分析证明其符合理论值。Tα1 活性测定 ,表明 S- Tα1 能提高淋巴细胞对丝裂原刺激的增殖反应 ,增强 NK细胞杀伤活性 ,具有增加淋巴细胞产生 IFN- γ的作用 ,我们的合成产物与国外对照品 Z- Tα1 呈现相仿的活性。此工作为进一步研究 Tα1
We synthesized thymosin α 1 (S Tα 1 ) with solid phase method, using Boc and derivatives respectively. The synthetic yield(cleavaged crude peptide weight/theoretical weight) of the latter was 80%, greater than that of the former, 64.2%. We used the initial material Fmoc Asn(Trt),to couple with HMP resin in order to improve the coupling efficiency. After purification with FPLC, S Tα 1 was found to be homogeneous by HPLC, cappillary electrophoresis and electrofocusing ampholine electrophoresis. The analytical results of mass spectrum and N terminal sequencing of S Tα 1 were in accordance with the theoretical value. We assayed the biological activity of S Tα 1 . The results showed that S Tα 1 could increase the proliferative response of the mitogen stimulated lymphocytes, enhance the activity of natural killer(NK) cells,and stimulate lymphocytes to produce IFN γ. It showed that our synthetic product S Tα 1 had the same dosage effect as that of the Z Tα 1 . This work provided a good basis for further studies on the immunoregulation mechanism and clinical significance of Tα 1 .
出处
《药物生物技术》
CAS
CSCD
1998年第2期103-108,共6页
Pharmaceutical Biotechnology
关键词
胸腺素Α1
多肽合成
生物活性
Thymosin α 1 , Peptide synthesis, Biological activity
