Acrosin inhibitor, 4'-acetamidophenyl 4-guanidinobenzoate, an experimental vaginal contraceptive with anti-HIV activity.

Abstract

Serine proteases are involved in a wide variety of seemingly unrelated physiological functions including capacitation of the spermatozoa and potentiation of human immunodeficiency virus (HIV) infection. The experimental vaginal contraceptives derived from 4-guanidinobenzoic acid act through inhibition of acrosin--a serine protease from the sperm. The serial ten-fold dilutions of 4'-acetamidophenyl 4-guanidinobenzoate (AGB) were tested in vitro for the effect against HIV infection by assaying the suppression of de novo p24 synthesis in virus-inoculated MT-4 T lymphocytes. The results reveal that complete inhibition of HIV occurred at 100 micrograms/ml--a dose corresponding to previously reported concentrations responsible for preventing fertilization in rabbits. These findings suggest that serine protease inhibitors and in particular the guanidinobenzoates, reported to be up to 100-fold more potent and less irritating than nonoxynol-9, can be potentially operative against sexual transmission of HIV.

• Authors: A S Bourinbaiar, S Lee-Huang
• Journal: Contraception (Contraception) Vol. 51 Issue 5 Pg. 319-22 (May 1995) ISSN: 0010-7824 [Print] United States
• PMID: 7628208 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Research Support, U.S. Gov't, P.H.S.)

Chemical References

• Antiviral Agents
• Benzoates
• Guanidines
• Spermatocidal Agents
• 4'-acetamidophenyl 4-guanidinobenzoate
• Acrosin

Topics

• Acrosin (antagonists & inhibitors)
• Antiviral Agents (pharmacology)
• Benzoates (administration & dosage, pharmacology)
• CD4-Positive T-Lymphocytes (virology)
• Cell Line
• Female
• Guanidines (administration & dosage, pharmacology)
• HIV (drug effects)
• Humans
• Spermatocidal Agents (administration & dosage, pharmacology)
• Vagina