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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
6
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pubmed:dateCreated |
1997-3-13
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pubmed:abstractText |
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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pubmed:keyword |
http://linkedlifedata.com/resource/pubmed/keyword/Clinical Research,
http://linkedlifedata.com/resource/pubmed/keyword/Contraception,
http://linkedlifedata.com/resource/pubmed/keyword/Contraceptive Agents,
http://linkedlifedata.com/resource/pubmed/keyword/Diseases,
http://linkedlifedata.com/resource/pubmed/keyword/Family Planning,
http://linkedlifedata.com/resource/pubmed/keyword/In Vitro,
http://linkedlifedata.com/resource/pubmed/keyword/Infections,
http://linkedlifedata.com/resource/pubmed/keyword/Nonoxynol-9,
http://linkedlifedata.com/resource/pubmed/keyword/Reproductive Tract Infections,
http://linkedlifedata.com/resource/pubmed/keyword/Research Methodology,
http://linkedlifedata.com/resource/pubmed/keyword/Research Report,
http://linkedlifedata.com/resource/pubmed/keyword/Sexually Transmitted...,
http://linkedlifedata.com/resource/pubmed/keyword/Sperm Immobilizing Agents,
http://linkedlifedata.com/resource/pubmed/keyword/Spermicidal Contraceptive Agents
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Dec
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pubmed:issn |
0010-7824
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
54
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
367-72
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pubmed:dateRevised |
2006-11-15
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pubmed:otherAbstract |
PIP: The possibility of enhancing the anti-fertility potential of gramicidin with low doses of ethylenediaminetetraacetic acid (EDTA) was investigated in an in vitro study. The inhibition of sperm functions was evaluated by computer-assisted semen analysis for sperm motility, cervical mucus penetration assay, and colorimetric tetrazolium salt and lactate dehydrogenase release assays. Gramicidin, nonoxynol-9, and EDTA all were found to immobilize sperm, although their effective doses diverged by orders of magnitude. Gramicidin abolished sperm motility within 2 minutes at 4 mcg/ml, but a 50 times higher dose of nonoxynol-9 and 1250 times more EDTA were required to achieve a comparable effect. The combination of 10 ng/ml of gramicidin with 0.1% of EDTA resulted in activity that was four orders of magnitude higher than the optimal combination of nonoxynol-9 with EDTA; sperm penetration into mucus was completely prevented. Moreover, gramicidin inhibited sperm motility without affecting mitochondrial respiratory function or disrupting cell membrane integrity. Quantitative toxicity tests confirmed that gramicidin is a potent spermostatic agent rather than a spermicidal agent. Further development of a gramicidin-EDTA formulation is urged given its potential as a non-toxic topical contraceptive with activity against viral and microbial sexually transmitted diseases.
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pubmed:meshHeading |
pubmed-meshheading:8968665-Cervix Mucus,
pubmed-meshheading:8968665-Drug Synergism,
pubmed-meshheading:8968665-Edetic Acid,
pubmed-meshheading:8968665-Female,
pubmed-meshheading:8968665-Gramicidin,
pubmed-meshheading:8968665-Humans,
pubmed-meshheading:8968665-L-Lactate Dehydrogenase,
pubmed-meshheading:8968665-Male,
pubmed-meshheading:8968665-Nitroblue Tetrazolium,
pubmed-meshheading:8968665-Oxidation-Reduction,
pubmed-meshheading:8968665-Sperm Motility,
pubmed-meshheading:8968665-Sperm-Ovum Interactions,
pubmed-meshheading:8968665-Spermatozoa
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pubmed:year |
1996
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pubmed:articleTitle |
Synergistic effect of gramicidin and EDTA in inhibiting sperm motility and cervical mucus penetration in vitro.
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pubmed:affiliation |
Metatron, Inc, New York, NY 10003 USA. emballon@usa.pipeline.com
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.
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