胸腺素α1的C端活性片段环肽类似物的合成与生物活性评价

Synthesis and Biological Activities of Cyclic Analogues of Thymosin α1 Active Fragment

用硫酯法合成了一系列Tα1的C端活性片段的环肽类似物,以提高其活性与稳定性.用促淋巴细胞增殖法测定了环肽类似物的生物活性,结果表明,环肽类似物较好地保留或提高了促淋巴细胞增殖活性.

Thymosin α1（ Tα1 ） is an immunomodulating peptide isolated from thymic extracts containing 28 amino acid residues. It has been demonstrated that the C-terminal fragment of Tα1 is responsible for its activity. In order to increase bioactivity and improve stability to proteolytic enzymes of this fragment, a series of cyclic peptides based on the active fragment were designed, and synthesized through formation of thioesters with various amount of residues or a flexible linker. The HPLC. The bioactivity was assayed in vitro that most of the cyclic analogs retained th through resulting cyclic peptides were determined via ESI-MS and T-lymphocyte proliferation testing. Data from this test show e immunoactivity, and some of them better than the original fragment. It can be concluded that cyclizations of this active fragment lead to the increasing of the bioactivity