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在先后以α-胰凝乳蛋白酶和木瓜酶作催化剂的作用下,从C端的LeuNH_2的氨基开始,逐个与N保护的氨基酸或其衍生物缩合,合成了亮-脑啡肽色氨酸类似物—TyrGlyGly Trp LeuNH_2~(**)。对酶的专一性、有机溶剂的选择和合成条件等进行了研究,在Z-TyrOMe和GlyGlyTrp LeuNH_2的缩合反应中,比较了相转移法和均相法。上述两种酶的酶促接肽的供体以N-酰基氨基酸酯为好,比相应的游离酸反应速度快,副反应少。如用嗜热菌蛋白酶,则以N-酰基氨基酸为好。酶促合成与从有机合成所得的产物相同。初步的体外实验表明合成的TyrGlyGlyTrpLeuNH_2和天然的亮-脑啡肽对豚鼠回肠的收缩显示相同程度的鸦片样的抑制作用。
After successively using α-chymotrypsin and papain as catalysts, starting from the amino group of LeuNH_2 at the C-terminal, N-protected amino acids or their derivatives are condensed one by one to synthesize a bright-enkephalin tryptophane analogue -TyrGlyGly Trp LeuNH_2 ~ (**). The specificity of the enzyme, the choice of organic solvents and the synthesis conditions were studied. In the condensation reaction of Z-TyrOMe and GlyGlyTrp LeuNH_2, phase transfer method and homogeneous method were compared. The above two enzymatic enzyme-linked peptide donors to N-acyl amino acid ester is better than the corresponding free acid reaction speed, less side effects. As with thermolysin, N-acyl amino acids are preferred. Enzymatic synthesis and the resulting product from the same organic synthesis. Preliminary in vitro experiments showed that the contractile effect of the synthetic TyrGlyGlyTrpLeuNH_2 and native enkephalin on guinea pig ileum showed the same degree of opioid inhibition.