Inhibitors on an elastase-like enzyme activity catalyzing Suc-Ala-Ala-Pro-Leu-pNA amidolysis in human seminal plasma.
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.
Matsuda
Y
Y
Department of Functional Bioanalysis, Meiji Pharmaceutical University, Tokyo, Japan.
Katayama
M
M
Hara
I
I
Sato
H
H
Tomomasa
H
H
Iizumi
T
T
Umeda
T
T
Ishikawa
H
H
D000581:Amidohydrolases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D000900:Anti-Bacterial Agents / Q000494:pharmacology; D002850:Chromatography, Gel; D004305:Dose-Response Relationship, Drug; D006801:Humans; D006877:Hydroxamic Acids / Q000494:pharmacology; D008297:Male; D009842:Oligopeptides / Q000378:metabolism*; D010196:Pancreatic Elastase / Q000037:antagonists & inhibitors / Q000378:metabolism; D010455:Peptides; D011480:Protease Inhibitors / Q000494:pharmacology*; D012661:Semen / Q000201:enzymology*
D000900:Anti-Bacterial Agents; D006877:Hydroxamic Acids; D009842:Oligopeptides; D010455:Peptides; D011480:Protease Inhibitors; C016977:amastatin; D010196:Pancreatic Elastase; D000581:Amidohydrolases; C010531:actinonin