含有大豆Bowman-Birk抑制剂胰凝乳蛋白酶反应位点的合成双环片段的抗胰凝乳蛋白酶和抗弹性蛋白酶活性

Anti-chymotrypsin and anti-elastase activities of a synthetic bicyclic fragment containing a chymotrypsin-reactive site of soybean Bowman-Birk inhibitor.

作者信息

Ando S, Yasutake A, Waki M, Nishino N, Kato T, Izumiya N

机构信息

Laboratory of Biochemistry, Faculty of Science, Kyushu University, Fukuoka, Japan.

出版信息

Biochim Biophys Acta. 1987 Dec 18;916(3):527-31. doi: 10.1016/0167-4838(87)90200-7.

DOI:10.1016/0167-4838(87)90200-7

PMID:3689809

Abstract

A bicyclic hexadecapeptide, which corresponds to the sequence 36-51 and contains the chymotrypsin-reactive Leu-43-Ser-44 bond of soybean Bowman-Birk inhibitor, has been synthesized. This peptide consists of two loops formed by disulfide bridges between Cys-36 and Cys-51 and between Cys-41 and Cys-49. The bicyclic peptide showed a strong anti-chymotryptic activity with a Ki of 7.1.10(-7) M. Comparison of inhibitory activity and digestive stability against chymotrypsin with other hexadecapeptides having the same sequence but lacking one or both disulfide bridges suggested that the compact bicyclic structure increases the activity and protects the Leu-Ser bond from chymotryptic digestion. Interestingly, the bicyclic peptide was found to inhibit porcine pancreatic elastase with a Ki of 4.3.10(-5) M, indicating the broad specificity of this ring system.

摘要

已合成一种双环十六肽，其对应于36 - 51序列，且含有大豆Bowman - Birk抑制剂的胰凝乳蛋白酶反应性Leu - 43 - Ser - 44键。该肽由两个环组成，这两个环通过Cys - 36与Cys - 51之间以及Cys - 41与Cys - 49之间的二硫键形成。该双环肽表现出很强的抗胰凝乳蛋白酶活性，其抑制常数Ki为7.1×10⁻⁷ M。将其与其他具有相同序列但缺少一个或两个二硫键的十六肽对胰凝乳蛋白酶的抑制活性和消化稳定性进行比较，结果表明紧密双环结构增加了活性，并保护Leu - Ser键免受胰凝乳蛋白酶消化。有趣的是，发现该双环肽对猪胰弹性蛋白酶也有抑制作用，其抑制常数Ki为4.3×10⁻⁵ M，表明该环系统具有广泛的特异性。