These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.


Pubmed for Handhelds

PUBMED FOR HANDHELDS

Search MEDLINE/PubMed

  • Title: Inhibition of human sperm acrosin by synthetic agents.
    Author: Bhattacharyya AK, Zaneveld LJ, Dragoje BM, Schumacher GF, Travis J.
    Journal: J Reprod Fertil; 1976 May; 47(1):97-100. PubMed ID: 1271380.
    Abstract:
    Twenty-two synthetic proteinase inhibitors were tested for their inhibitory properties towards human acrosin. p-Nitrophenyl-p1-guanidino benzoate (NPGB) was the most effective (K1 value of 1-5 X 10(-8) M), producing a non-competitive type of inhibition in contrast to all other inhibitors which showed a competitive type of inhibition. The Michaelis constant for human acrosin on BAEE at pH 8-1 was calculated to be 4-25 X 10(-5) M. The neutral acrosomal proteinase, acrosin, has been found in the spermatozoa from many species. The addition of naturally occurring or synthetic inhibitors of acrosin to capacitated spermatozoa prevents fertilization, and synthetic acrosin inhibitors prevent fertilization by ejaculated spermatozoa while natural inhibitors do not. It was therefore thought possible that the synthetic inhibitors might be developed as contraceptive agents. In this study 22 synthetic proteinase inhibitors were tested in relation to human acrosin. Techniques used are described. The most effective compound was p-nitrophenyl-p'-guanidino benzoate (NPGB), which produced a noncompetitive type of inhibition. Some others tested showed a competitive type of inhibition. They were at least 200-3000 times less effective than NPGB. The high affinity of human acrosin for NPGB suggests that the enzyme has a serine group at its active site. Results indicate that NPGB has a greater protential as an antifertility agent than any other inhibitor tested.
    [Abstract] [Full Text] [Related] [New Search]