FOY对人血浆中激肽酶II的抑制作用。

Inhibition by FOY of kininase II in human plasma.

作者信息

Bönner G, Frericks A, Büchsler U, Kaufmann W

出版信息

Biol Chem Hoppe Seyler. 1986 Sep;367(9):963-8. doi: 10.1515/bchm3.1986.367.2.963.

DOI:10.1515/bchm3.1986.367.2.963

Abstract

In this investigation we studied the inhibitory effect of FOY S 983 (gabexate mesilate) and FOY S 980 (camostate mesilate) on the kininase II activity in human plasma in vitro. Both compounds were able to inhibit kinase II, however, compared to captopril or EDTA only very weakly. The inhibitory effect of FOY S 983 or FOY S 980 could be diminished neither by NaOH-induced hydrolysis of the inhibitor nor by dialysis or ultrafiltration, but could be clearly reduced by dialysis against ZnCl2 solution. The inhibition of kininase II activity in human plasma by FOY S 983 was due to its 6-guanidinocaproate component probably acting as Zn2+-complexing agent. The ethyl 4-hydroxybenzoate component of FOY S 983 had no inhibitory effect.

摘要

在本研究中，我们在体外研究了FOY S 983（甲磺酸加贝酯）和FOY S 980（甲磺酸卡莫司他）对人血浆中激肽酶II活性的抑制作用。两种化合物均能抑制激肽酶II，但与卡托普利或乙二胺四乙酸相比，抑制作用非常微弱。FOY S 983或FOY S 980的抑制作用既不会因抑制剂经氢氧化钠诱导水解而减弱，也不会因透析或超滤而减弱，但通过用氯化锌溶液透析可明显降低。FOY S 983对人血浆中激肽酶II活性的抑制作用可能归因于其6-胍基己酸盐成分，该成分可能作为锌离子络合剂。FOY S 983的4-羟基苯甲酸乙酯成分没有抑制作用。