PMID: 8968665Dec 1, 1996Paper

Synergistic effect of gramicidin and EDTA in inhibiting sperm motility and cervical mucus penetration in vitro

Contraception
A S Bourinbaiar, C H Lee

Abstract

Gramicidin, a linear polypeptide with antiviral and antimicrobial properties, was compared in vitro with a commonly used spermicidal detergent-nonoxynol-9 (N9). The inhibition of sperm functions was evaluated by computer-assisted semen analysis (CASA) for sperm motility, in cervical mucus penetration assay, and by colorimetric tetrazolium salt and lactate dehydrogenase release assays routinely employed for testing the toxicity of drugs. The effective 100% inhibitory concentration (IC100) of gramicidin in a 2-min sperm immobilization assay by CASA was equal to 4 micrograms/ml, whereas IC100 of N9 was equal to 200 micrograms/ml. The presence of 0.1% of chelating agent, EDTA, reduced IC100 of gramicidin to 10 ng/ml, while less than a twofold enhancement in N9 activity was observed upon combination with EDTA. Likewise, the gramicidin/EDTA combination was 100,000 times more potent than N9/EDTA in the sperm penetration assay. Quantitative toxicity tests confirmed that gramicidin is a potent spermostatic rather than spermicidal agent. Further development of a gramicidin/EDTA formulation is warranted as a nontoxic topical contraceptive with activity against viral and microbial sexually transmitted diseases (STDs).

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Citations

Jun 13, 2003·Fertility and Sterility·Nicolai WroblewskiRalf Henkel
Nov 6, 2003·Toxicology in Vitro : an International Journal Published in Association with BIBRA·D HoornstraM S Salkinoja-Salonen
Apr 29, 2015·Toxins·Abaid MalikFlorian Lang
Jun 22, 2010·Current Opinion in Biotechnology·Sheereen MajdMichael Mayer
Aug 26, 2014·Toxins·Philip A Gurnev, Ekaterina M Nestorovich
Sep 8, 1998·Archives of Andrology·Y L KuoS T Young
Nov 26, 2005·Contraception·Amira ZairiKhaled Hani

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