促睡眠肽(DSIP)的合成及其生理活性

用经典方法合成了保护的兔睡眠九肽经三氟乙酸处理,凝胶柱层析纯化,得到了纯的自由九肽。pH 3.8电泳、微晶纤维素薄板层析及高效液相色谱鉴定表明产物为不合Asp残基α→β转位副产物的纯Asp~5-α-促睡眠肽,将其经脑室(5微克/兔)或静脉(25微克/公斤)给家兔注射后引起睡眠,兔脑电图(EEG)均呈现δ及σ波明显增强作用。     

SYNTHESIS OF DELTA SLEEP-INDUCING PEPTIDE(DSIP) AND ITS PHYSIOLOGICAL ACTIVITY

Protected nonapeptide—Delta Sleep-Induclng Peptide(DSIP)(Boc·Trp·Ala·Gly·Gly·Asp·Ala·Ser·Gly·Glu-OBu~t) has been synthesized by classical method. The product has been treated with TFA and purified on DEAE-Sephadex-A25 coltunn, pure free nonapeptide obtained and a to β transposition of Asp-residue found to be absent. It has been assayed by electrophoresis at pH 3.8, microcrystallinecellulose TLC and HPLC. The physiological activities of synthetic DSIP are performed on rabbits by using intravenous administration or mesodiencephalic ventricular infusion. Its function Of intensifying δ and σ waves on rabbit's electroencephalogram(EEG) is evident. There is no concomitant increase of δ- and σ-enhancing effect following mesodiencephalic ventricular infusion of 10 or 20 times higher than 5 μg/rabbit doses. Results of 6-day consecutive intravenous administration(50μg/kg) indicate that there is no obvious sign of adaptation to DSIP. Results suggest that the physiological function of endogenous sl