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用固相法合成了促δ-波睡眠肽Trp-Ala-Gly-Gly-Asp-Ala-Ser-Gly-Glu(DSIP)及其十四种类似物和三个短肽,研究了结构与功能的关系,类似物的设计,主要考虑在分子中引入D-氨基酸以抑制酶的作用和增强稳定性,以及引入疏水侧链氨基酸如Phe和Trp等,位置的修饰主要在1,3,4,5,8和9位,即:D-Trp~1,Tyr~1,Tyr~1Phe~5,D-Trp~1Phe~8,Trp~(3,4),D-Trp~(3,4),D-Trp~(1,3,4)Phe~8,D-Glu~9,D-pF-Phe~(3,4)Phe~8D-Glu~9,Phe~5,Glu~5Asp~9,Tyr~5Asp~9,Ala~7和Asp~9-DSIP以及Trp-Ala-Gly-Gly-Asp,Trp-Ala-Gly-Gly-Glu和Trp-Gly-Glu,合成肽的纯度经氨基酸组成分析、元素分析、薄层层析以及纸电泳鉴定,生物试验表明D-Trp~1,Tyr~1,Tyr~1Phe~5,A~1a~7-DSIP无促眠活性;而Phe~5-DSIP的促眠活性与DSIP相接近,其他类似物的生物试验结果将另文发表。
Trp-Ala-Gly-Gly-Asp-Ala-Ser-Gly-Glu (DSIP) and its fourteen kinds of analogues and three short peptides were synthesized by solid phase method. The structure and function The main consideration is the introduction of D-amino acids in the molecule to inhibit the enzyme activity and enhance the stability, as well as the introduction of hydrophobic side-chain amino acids such as Phe and Trp. The modification of the position is mainly at 1,3,4, Trp ~ (3,4), D-Trp ~ (3,4), D-Trp ~ 1, Tyr ~ 1, Tyr ~ 1Phe ~ , D-Trp ~ (1,3,4) Phe ~ 8, D-Glu ~ 9, D-pF ~ Phe ~ (3,4) Phe ~ 8D-Glu ~ 9, Phe ~ 5, Glu ~ 5Asp ~ 9 , Tyr ~ 5Asp ~ 9, Ala ~ 7 and Asp ~ 9-DSIP and Trp-Ala-Gly-Gly-Asp, Trp-Ala-Gly-Gly-Glu and Trp-Gly-Glu. The purity of the synthesized peptide is determined by amino acid composition Bioassay showed that D-Trp ~ 1, Tyr ~ 1, Tyr ~ 1Phe ~ 5 and A ~ 1a ~ 7-DSIP had no hypnotic activity, while Phe ~ 5- DSIP sleep activity and DSIP close to other biological test results will be published separately.