Susceptibility of glycolytic enzyme activity and motility of spermatozoa from rat, mouse, and human to inhibition by proven and putative chlorinated antifertility compounds in vitro
Identifieur interne : 00CA17 ( Main/Merge ); précédent : 00CA16; suivant : 00CA18Susceptibility of glycolytic enzyme activity and motility of spermatozoa from rat, mouse, and human to inhibition by proven and putative chlorinated antifertility compounds in vitro
Auteurs : Wilhelm Bone [Allemagne] ; Alan R. Jones [Australie] ; Christophe Morin [France] ; Eberhard Nieschlag [Allemagne] ; Trevor G. Cooper [Allemagne]Source :
- Journal of andrology [ 0196-3635 ] ; 2001.
Descripteurs français
- Pascal (Inist)
- Wicri :
- topic : Homme.
English descriptors
- KwdEn :
Abstract
Nonhormonal contraceptives that act by blocking energy metabolism within sperm have the advantage over spermatogenic inhibitors by their fast onset of infertility and their almost immediate restoration of fertility after withdrawal of the contraceptive agent. This study was done to test new chlorinated compounds for their contraceptive potency on rodent and human sperm in vitro. Cells were incubated in a medium containing glucose as the sole energy source with 1-chloro-3-hydroxypropanone (CHOP) and 1,6-dichloro-1,6-dideoxy-D-fructose (DCDF), chlorinated analogues of glycolytic substrates, as well as racemic (R,S)-α-chlorohydrin (ACH). After incubation, enzymatic activity and kinematic parameters were estimated. A dose-dependent inhibition of the glycolytic enzyme, glyceraldehyde 3-phosphate dehydrogenase (GAPDH), of rat and mouse distal cauda epididymidal and human ejaculated sperm by ACH, CHOP, and DCDF was demonstrated. Triosephosphate isomerase (TPI) was inhibited by ACH, but not by CHOP and DCDF, irrespective of species. All compounds inhibited sperm motility and kinematic parameters with increasing concentration. The results confirm that inhibition of glycolytic enzymes of sperm, including those of human, can be effectively brought about by a variety of chloro-compounds that can be converted to (s)-3-chlorolactaldehyde, the stereospecific chloro-derivative of the enzyme's natural substrate, (R)-glyceraldehyde 3-phosphate, and could be developed into contraceptive agents for men.
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Pascal:01-0354166Le document en format XML
<record><TEI><teiHeader><fileDesc><titleStmt><title xml:lang="en" level="a">Susceptibility of glycolytic enzyme activity and motility of spermatozoa from rat, mouse, and human to inhibition by proven and putative chlorinated antifertility compounds in vitro</title>
<author><name sortKey="Bone, Wilhelm" sort="Bone, Wilhelm" uniqKey="Bone W" first="Wilhelm" last="Bone">Wilhelm Bone</name>
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<s2>Münster</s2>
<s3>DEU</s3>
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<sZ>4 aut.</sZ>
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<country>Allemagne</country>
<placeName><region type="land" nuts="1">Rhénanie-du-Nord-Westphalie</region>
<region type="district" nuts="2">District de Münster</region>
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<author><name sortKey="Jones, Alan R" sort="Jones, Alan R" uniqKey="Jones A" first="Alan R." last="Jones">Alan R. Jones</name>
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<region type="état">Nouvelle-Galles du Sud</region>
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</placeName>
<orgName type="university">Université de Sydney</orgName>
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<author><name sortKey="Morin, Christophe" sort="Morin, Christophe" uniqKey="Morin C" first="Christophe" last="Morin">Christophe Morin</name>
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<sourceDesc><biblStruct><analytic><title xml:lang="en" level="a">Susceptibility of glycolytic enzyme activity and motility of spermatozoa from rat, mouse, and human to inhibition by proven and putative chlorinated antifertility compounds in vitro</title>
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<author><name sortKey="Jones, Alan R" sort="Jones, Alan R" uniqKey="Jones A" first="Alan R." last="Jones">Alan R. Jones</name>
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<country>Australie</country>
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<settlement type="city">Sydney</settlement>
</placeName>
<orgName type="university">Université de Sydney</orgName>
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<author><name sortKey="Morin, Christophe" sort="Morin, Christophe" uniqKey="Morin C" first="Christophe" last="Morin">Christophe Morin</name>
<affiliation wicri:level="3"><inist:fA14 i1="03"><s1>Laboratoire d'études dynamiques et structurales de la sélectivité de la Université de Grenoble</s1>
<s2>Grenoble</s2>
<s3>FRA</s3>
<sZ>3 aut.</sZ>
</inist:fA14>
<country>France</country>
<placeName><region type="region">Auvergne-Rhône-Alpes</region>
<region type="old region">Rhône-Alpes</region>
<settlement type="city">Grenoble</settlement>
</placeName>
</affiliation>
</author>
<author><name sortKey="Nieschlag, Eberhard" sort="Nieschlag, Eberhard" uniqKey="Nieschlag E" first="Eberhard" last="Nieschlag">Eberhard Nieschlag</name>
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<country>Allemagne</country>
<placeName><region type="land" nuts="1">Rhénanie-du-Nord-Westphalie</region>
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</placeName>
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<author><name sortKey="Cooper, Trevor G" sort="Cooper, Trevor G" uniqKey="Cooper T" first="Trevor G." last="Cooper">Trevor G. Cooper</name>
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<series><title level="j" type="main">Journal of andrology</title>
<title level="j" type="abbreviated">J. androl.</title>
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<seriesStmt><title level="j" type="main">Journal of andrology</title>
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</fileDesc>
<profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Animal</term>
<term>Chlorohydrin</term>
<term>Contraceptive</term>
<term>Enzymatic activity</term>
<term>Glycolysis</term>
<term>Human</term>
<term>In vitro</term>
<term>Mouse</term>
<term>Rat</term>
<term>Sensitivity</term>
<term>Spermatozoa</term>
</keywords>
<keywords scheme="Pascal" xml:lang="fr"><term>Activité enzymatique</term>
<term>Spermatozoïde</term>
<term>Sensibilité</term>
<term>Glycolyse</term>
<term>Homme</term>
<term>Animal</term>
<term>Chlorhydrine</term>
<term>Rat</term>
<term>Contraceptif</term>
<term>In vitro</term>
<term>Souris</term>
</keywords>
<keywords scheme="Wicri" type="topic" xml:lang="fr"><term>Homme</term>
</keywords>
</textClass>
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</teiHeader>
<front><div type="abstract" xml:lang="en">Nonhormonal contraceptives that act by blocking energy metabolism within sperm have the advantage over spermatogenic inhibitors by their fast onset of infertility and their almost immediate restoration of fertility after withdrawal of the contraceptive agent. This study was done to test new chlorinated compounds for their contraceptive potency on rodent and human sperm in vitro. Cells were incubated in a medium containing glucose as the sole energy source with 1-chloro-3-hydroxypropanone (CHOP) and 1,6-dichloro-1,6-dideoxy-D-fructose (DCDF), chlorinated analogues of glycolytic substrates, as well as racemic (R,S)-α-chlorohydrin (ACH). After incubation, enzymatic activity and kinematic parameters were estimated. A dose-dependent inhibition of the glycolytic enzyme, glyceraldehyde 3-phosphate dehydrogenase (GAPDH), of rat and mouse distal cauda epididymidal and human ejaculated sperm by ACH, CHOP, and DCDF was demonstrated. Triosephosphate isomerase (TPI) was inhibited by ACH, but not by CHOP and DCDF, irrespective of species. All compounds inhibited sperm motility and kinematic parameters with increasing concentration. The results confirm that inhibition of glycolytic enzymes of sperm, including those of human, can be effectively brought about by a variety of chloro-compounds that can be converted to (s)-3-chlorolactaldehyde, the stereospecific chloro-derivative of the enzyme's natural substrate, (R)-glyceraldehyde 3-phosphate, and could be developed into contraceptive agents for men.</div>
</front>
</TEI>
<affiliations><list><country><li>Allemagne</li>
<li>Australie</li>
<li>France</li>
</country>
<region><li>Auvergne-Rhône-Alpes</li>
<li>District de Münster</li>
<li>Nouvelle-Galles du Sud</li>
<li>Rhénanie-du-Nord-Westphalie</li>
<li>Rhône-Alpes</li>
</region>
<settlement><li>Grenoble</li>
<li>Münster</li>
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<tree><country name="Allemagne"><region name="Rhénanie-du-Nord-Westphalie"><name sortKey="Bone, Wilhelm" sort="Bone, Wilhelm" uniqKey="Bone W" first="Wilhelm" last="Bone">Wilhelm Bone</name>
</region>
<name sortKey="Cooper, Trevor G" sort="Cooper, Trevor G" uniqKey="Cooper T" first="Trevor G." last="Cooper">Trevor G. Cooper</name>
<name sortKey="Nieschlag, Eberhard" sort="Nieschlag, Eberhard" uniqKey="Nieschlag E" first="Eberhard" last="Nieschlag">Eberhard Nieschlag</name>
</country>
<country name="Australie"><region name="Nouvelle-Galles du Sud"><name sortKey="Jones, Alan R" sort="Jones, Alan R" uniqKey="Jones A" first="Alan R." last="Jones">Alan R. Jones</name>
</region>
</country>
<country name="France"><region name="Auvergne-Rhône-Alpes"><name sortKey="Morin, Christophe" sort="Morin, Christophe" uniqKey="Morin C" first="Christophe" last="Morin">Christophe Morin</name>
</region>
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</tree>
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</record>
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