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At least 19 recordsLinked to original sources
PubMed1977

Chemical sterilization of male langurs: synergistic action of alpha-chlorohydrin (U-5897) with methallibure (ICI, 33828) on the testes and epididymides of Presbytis entellus entellus Dufresne.

1. Synergistic action of alpha-chlorohydrin with methallibure (ICI, 33828) on the testicular function of Presbytis entellus entellus Dufresne has been studied. 2. Chronic administration of alpha-chlorohydrin alone (140 mg/day for 40 days) caused testicular lesion resulting in a massive atrophy of the spermatogenic elements. Epididymal epithelium was regressed and the lumen was devoid of spermatozoa. 3. alpha-Chlorohydrin inhibited the synthesis of RNA and sialic acid in the testes and epididymides. Total cholesterol per gram of testis and alkaline phosphatase activity were increased after alpha-chlorohydrin administration. 4. These effects could be achieved with a lower dose of alpha-chlorohydrin (1/4) when administered in combination with a gonadotrophin inhibitor, i. e. ICI, 33828 (Methallibure). Methallibure alone (200 mg/kg: total dose) has no damaging effects on the testes and epididymides. But it altered testicular cholesterol and enzyme activity. 5. In conclusion, an effective inhibition of spermatogenesis could be achieved by synergistic action of the two different drugs i. e. alpha-chlorohydrin and ICI, 33828 (Methallibure).

Alkaline Phosphatase↗
PubMed1979

The interaction of alpha-chlorohydrin with glycerol kinase.

alpha-Chlorohydrin has been examined both for its ability to act as a substrate for glycerol kinase and as an inhibitor of the reaction of glycerol with glycerol kinase. Using a purified enzyme from Candida mycoderma, it was established that alpha-chlorohydrin does not act as a substrate for glycerol kinase, but does act as a competitive inhibitor (Ki of 30 mM) of purified glycerol kinase and the enzyme present in a sonicated preparation of ram spermatozoa. Neither alpha-chlorohydrin nor alpha-chlorohydrin phosphate acted as inhibitors of NAD- or flavin-linked glycerolphosphate dehydrogenase. It is concluded that alpha-chlorohydrin does not cause the impairment of sperm metabolism as a result of phosphorylation catalysed by glycerol kinase.

Animals↗
PubMed1975

Effect of low doses of alpha-chlorohydrin on fertility and semen characteristics and binding of the drug of spermatozoa in swine.

Daily feeding of 1 mg of alpha-chlorohydrin per kg body weight to boars prevented fertility completely when the ejaculate was used for insemination. The semen charactreated than in untreated boars, but the sperm morphology was otherwise normal. In vitro addition of 5 mg/epididymal contents from the treated boars revealed normal Na+, K+ and glycerylphosphorylcholine concentrations. The movement of sperm cytoplasmic droplets was completed on all spermatozoa more distally in treated than in untreated boars, but the sperm morphology was otherwise normal. In vitro addition of 5 mg/100 ml of alpha-chlorohydrin to ejaculate boar semen completely inhibited and 2.5 mg/100 ml decreased fertility. Removal of the alpha-chlorohydrin prior to insemination partially restored fertility. 14C-alpha-chlorohydrin was shown to be more firmly bound to boar spermatozoa than 14C-carboxyinulin and could not be removed from the spermatozoa with 3 washings. The contraceptive mechanism of the drug is suggested to be alkylation of the sperm membrane by free alpha-chlorohydrin in the epididymis.

Animals↗
PubMed1979

The antifertility activity and toxicity of alpha-chlorohydrin derivatives in male rats.

The antifertility activity and toxicity of alpha-chlorohydrin, six derivatives and glycidol were investigated in male rats. At a dose of 5 mg/kg injected intraperitoneally each day for 14 days, only alpha-chlorohydrin produced complete infertility. When rats were injected with the derivatives at a dose equivalent to 5 mg/kg of alpha-chlorohydrin on a molar basis, the phosphorylated and amino acid derivatives produced complete infertility within 7 days; however, there were some signs of toxicity. Compound II also produced complete infertility and appeared less toxic. AY - 22,352, compounds III and IV and glycidol had no antifertility activity, although spermatozoan motility was reduced by injection of glycidol.

Adrenal Glands↗
PubMed1979

Effect of alpha-chlorohydrin on epididymal sperm and epididymal plasma in swine.

Investigation of the contraceptive mechanism of alpha-chlorohydrin was done by analyses of epididymal plasma and certain epididymal sperm characteristics after oral administration of 0, 5, 10 or 30 mg/kg, day of the drug to boars for 15 days. Water resorption in caput epididymidis was slightly decreased in all treatment groups. Sodium, potassium, chloride, glycerylphosphorylcholine levels, and seminal antigens in epididymal plasma were not altered significantly by 10 or 30 mg/kg of the drug. The boars on 5 mg/kg exhibited significantly elevated sodium, potassium, or chloride values in various segments. Motility was significantly lower on corpus and proximal cauda epididymal spermatozoa from alpha-chlorohydrin treated boars. Only boars receiving 30 mg/kg exhibited impaired sperm motility in the distal cauda. The movement of the cytoplasmic droplets to the distal position was retarded in boars on the two highest dose levels. The results suggest that the contraceptive effects of alpha-chlorohydrin in the boar is probably not mediated via an impaired epididymal function.

Animals↗
PubMedDate not supplied

Histochemical changes of the rat testis and epididymis after treatment of alpha-chlorohydrin-effects of a single low dose.

A histochemical study has been made of the localization and changes of lipids, carbohydrates, ATPase and 5'-nucleotidase in fresh and fixed frozen sections of testicular and epididymal components in the normal and alpha-chlorohydrin-treated rats. After treatment with a single low dose of alpha-chlorohydrin, the phospholipids are decreased with corresponding increase in triglycerides in both the testis and epididymis. Glycogen, ATPase and 5'-nucleotidase are also decreased after treatment with alpha-chlorohydrin. The physiological significance of these histochemical changes has been discussed.

Adenosine Triphosphatases↗
PubMed1979

Effect of sodium nitrite on the alpha-chlorohydrin-induced lesion of the testis--epididymis complexin the rat.

Administration of vasodilator, sodium nitrite (20 mg/kg body weight), 30 min before alpha-chlorohydrin treatment (90 mg/kg body weight) prevented the chlorohydrin-induced lesion in rat testis--epididymis complex. However, administration of vasodilator 90 min after alpha-chlorohydrin treatment did not prevent the chlorohydrin-induced lesion in the testis--epididymis complex. These observations suggest that the testicular vasculature is involved in drug action.

Animals↗
PubMed1978

Embryopathies due to spermatozoal impairment in Xenopus laevis.

An in vitro test system, involving gametes of Xenopus laevis has been used to study the effect of antifertility agents upon spermatozoa as manifest in developing embryos. Exposure to either the isomeric forms of dimethylmyleran, methyl methanesulphonate or gamma-radiation led to development of a range of embryopathies, whereas treatment with steroidal drugs or the rodent epididymal chemosterilants alpha-chlorohydrin and trimethylphosphate was compatible with production of apparently normal offspring.

Abnormalities, Drug-Induced↗
PubMed1979

Mutagenicity of halogenated and oxygenated three-carbon compounds.

Four structurally related three-carbon compounds, known for their antifertility activity in the male, and the brominated derivatives of two of these compounds were tested for mutagenic activity by the Salmonella typhimurium test of Ames et al. In the presence of strain TA-100, a base-pair substituion detector strain, 1,2-dibromo-3-chloropropane (DBCP), was the most active compound tested but required enzymatic conversion by 59 microsomal preparation to an active mutagen. Three of these compounds containing an epoxide group-epichlorohydrin, epibromohydrin, and glycidol-were highly active direct mutagens, not requiring 59 for activation, alpha-Chlorohydrin was the least active compound tested; alpha-bromohydrin was 40 times more active than its chlorinated analog. Epibromohydrin was only slightly more active than epichlorohydrin, but both were highly active. With both of the halogenated epoxides, 59 preparation caused a substantial decrease in mutagenic activity at every concentration tested. All six compounds showed dose-related responsiveness for the base-pair substitution detector strains used. However, they were relatively inactive against the frameshift detector strain of S. typhimurium, TA-98. Glycerol, propylene glycol, and n-propanol, which are also three-carbon compounds containing one or more hydroxy groups, were inactive when trested at high concentrations with strain TA-100.

Alcohols↗
PubMed1979

The metabolism of 3-amino-1-chloropropan-2-ol in relation to its antifertility activity in male rats.

1. The metabolism of 3-amino[36Cl]chloropropan-2-ol (III) was studied in male rats. Three urinary metabolites were isolated and identified as alpha-chlorohydrin (I), beta-chlorolactic acid (V) and oxalic acid (VI). Much of the administered aminochloropropanol was excreted unchanged in the urine; 63% within 72 h, 75% over 250 h. 2. Monoamine oxidase is capable of converting aminochloropropanol to beta-chlorolactaldehyde (IV) which, by processes of either reduction or oxidation, suggests that the metabolic pathway is IV leads to I and IV leads to V leads to VI. 3. As assessed by the diuretic activities of the isomers of aminochloropropanol, oxalate appears to be produced by the (+)-isomer but not by the (-)-isomer. A difference in metabolic rate or route of the isomers may account for their differing physiological activities. 4. (+)- and (-)-aminochloropropanol exhibited identical in vitro inhibitory activities on the glycolytic enzymes glyceraldehyde-3-phosphate dehydrogenase and triosephosphate isomerase, and were substrates for monoamine oxidase to equivalent extents.

Animals↗
PubMed1976

Purification and properties of arylsulphatase A from rabbit testis.

Rabbit testis arylsulphatase A was purified 140-fold with a recovery of 20% from detergent extracts of an acetone-dried powder by using DE-52 cellulose column chromatography, gel filtration on Sephadex G-200 and preparative isoelectric focusing. The purified enzyme showed one major band with one minor contaminant on electrophoresis in a 7.5% (w/v) polyacrylamide gel at pH8.3. On sodiumdodecyl sulphate/polyacrylamidegel electrophoresis, a single major band was observed with minor contaminants. The final preparation of enzyme was free from general proteolytic, esterase, hyaluronidase, beta-glucuronidase and beta-galactosidase activities. Rabbit testicular arylsulphatase A exists as a dimer of mol.wt. 110000 at pH7.1. At pH5.0 the enzyme is a tetramer of mol.wt. 220000. Arylsulphatase A appears to consist of two identical subunits of mol.wt. 55000 each. The highly purified enzyme has pI4.6. The enzyme hydrolyses p-nitrocatechol sulphate with Km and Vmax, of 4.1 mM and 80nmol/min respectively, but has no activity toward p-nitrophenyl sulphate. The pH optimum of the enzyme varies with the incubation time. By applying Sephacex G-200 chromatography and preparative isoelectric focusing, one form of enzyme was obtained. The enzyme has properites common to arylsulphatase A of other sources with respect to the anomalous time-activity relationship, pI, inhibition by PO42-, SO32- and Ag+ ions and substrate affinity to p-nitrocatechol sulphate. However, the enzyme shows the temperature optimum of arylsulphatase B of other species.

Animals↗