Matsuda Y, Katayama M, Hara I, Sato H, Tomomasa H, Iizumi T, Umeda T, Ishikawa H
Department of Functional Bioanalysis, Meiji Pharmaceutical University, Tokyo, Japan.
Arch Androl. 2000 Jan-Feb;44(1):1-9. doi: 10.1080/014850100262353.
The behavior of some proteinase inhibitors toward the Suc-Ala-Ala-Pro-Leu-pNA amidolytic enzyme activity in human seminal plasma (HSP) was tested. [(2S, 3R)-3-Amino-2-hydroxy-5-methyl-hexanoyl]L-valyl-L-valyl-L-aspartic acid (Amastatin) and 3-[1-[(2-(hydroxymethyl)- -pyrolidinyl)-2-methylpropyl]-carbamoyl] octanohydroxamic acid (Actinonin) showed strong inhibitory effects. No inhibition of this present enzyme activity was seen with anti-human serum (whole), anti-human leukocyte elastase, phenyl-methyl sulfonyl fluoride, Elastatinal, ethyeneglycol bis(beta-aminoethyl ethyl)N,N,N:N'-tetra acetic acid, and [L-3-trans-ethoxycarbonyl-oxirane-2-carbonyl]1-L-leucine(3-methylbutyl)a mido (E-64). No relation was observed between human pancreatic elastase antigen and the Suc-Ala-Ala-Pro-Leu-pNA amidolytic enzyme enzyme activity in HSP. Two peaks of Suc-Ala-Ala-Leu-Pro-pNA amidolytic enzyme activity were separated by Cellulofine GCL-2000 gel filtration and these activities were completely abolished by addition of Amastatin. Suc-Ala-Ala-Pro-Leu-pNA amidolytic enzyme activity in HSP is not an elastase-like metalloproteinase but is rather an acyl amidase-like leucine aminopeptidase.
测试了一些蛋白酶抑制剂对人精浆（HSP）中Suc-Ala-Ala-Pro-Leu-pNA酰胺水解酶活性的作用。[(2S, 3R)-3-氨基-2-羟基-5-甲基己酰基]L-缬氨酰-L-缬氨酰-L-天冬氨酸（氨肽素）和3-[1-[(2-(羟甲基)-吡咯烷基)-2-甲基丙基]-氨基甲酰基]辛烷异羟肟酸（放线菌素）表现出强烈的抑制作用。抗人血清（全血清）、抗人白细胞弹性蛋白酶、苯甲基磺酰氟、抑肽酶、乙二醇双(β-氨基乙基醚)N,N,N:N'-四乙酸以及[L-3-反式-乙氧羰基-环氧乙烷-2-羰基]1-L-亮氨酸(3-甲基丁基)酰胺（E-64）对该酶活性均无抑制作用。未观察到人胰腺弹性蛋白酶抗原与HSP中Suc-Ala-Ala-Pro-Leu-pNA酰胺水解酶活性之间存在关联。通过Cellulofine GCL-2000凝胶过滤分离出了Suc-Ala-Ala-Leu-Pro-pNA酰胺水解酶活性的两个峰，加入氨肽素后这些活性完全被消除。HSP中的Suc-Ala-Ala-Pro-Leu-pNA酰胺水解酶活性不是一种类似弹性蛋白酶的金属蛋白酶，而是一种类似酰基酰胺酶的亮氨酸氨肽酶。
