Effect of 1,3-dithia-2-thioxo-cyclopent-4-ene and its derivatives on liver injury induced by carbon tetrachloride and orotic acid in rats.

  title={Effect of 1,3-dithia-2-thioxo-cyclopent-4-ene and its derivatives on liver injury induced by carbon tetrachloride and orotic acid in rats.},
  author={S Sadanobu and Makoto Takeuchi and Masakatsu Tezuka},
  journal={The Journal of toxicological sciences},
  volume={22 5},
The protective effect of 1,3-dithia-2-thioxo-cyclopent-4-ene (DT827A) and its two derivatives of 4-phenyl-1,3-dithia-2-thioxo-cyclopent-4-ene (DT827B) and 4-(4-fluorophenyl)-1,3-dithia-2-thioxo-cyclopent-4-ene (DT827C) on liver injury induced by carbon tetrachloride (CCl4) and orotic acid was studied using male rats. The approximate lethal doses were about 100 mg/kg for DT827A-treated animals and more than 800 mg/kg for the other two compounds-treated groups. Single oral administration of the… 
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Effect of 4-phenyl-1,3-dithia-2-thioxo-cyclopent-4-ene on liver injury induced by repeated exposure to galactosamine plus carbon tetrachloride in rats.
A hepatoprotective potential of DT827B was suggested under the conditions of these studies after a therapeutic effect against liver injury induced by D-GalN + CCl4 dose-dependently was suggested.
In vitro tests of 1,3-dithia-2-thioxo-cyclopent-4-ene to evaluate the mechanisms of its hepatoprotective action.
The protective effect of DT827A on a liver injury is due neither to its influence on liver GSH levels nor inhibition of the metabolic activation of CCl4, but a possible mechanism of action for theDT827 series of compounds to indicate an antioxidative effect would be brought about by the role of the compounds as a radical scavenger as well as its reductive effect.
Mutagenicity tests of 4-phenyl-1,3-dithia-2-thioxo-cyclopent-4-ene.
The mutagenicity of 4-phenyl-1,3-dithia-2-thioxo-cyclopent-4-ene was examined in reverse mutation tests, in the chromosomal aberration test with Chinese hamster ovary cells, and in the micronucleus test using mice bone-marrow, finding the increase in polyploidy probably is due to a toxic effect of the compound.


Effect of diisopropyl 1,3-dithiol-2-ylidenemalonate (NKK-105) on fatty liver induced by carbon tetrachloride.
The data suggest that NKK-105 exerts a curative effect on CCl4-induced fatty liver by improving the impaired protein synthesis and by promoting lipoprotein secretion.
[Effect of malotilate (diisopropyl 1, 3-dithiol-2-ylidenemalonate) on chronic liver injury caused by carbon tetrachloride].
  • M. Katoh, T. Sugimoto
  • Chemistry, Medicine
    Nihon yakurigaku zasshi. Folia pharmacologica Japonica
  • 1982
It is difficult to explain the protective effect of malotilate on the liver injury only by this phenomenon, as changes of biochemical parameters and histopathological findings caused by CCl4 were improved thereafter.
Prevention by cystamine of liver necrosis and early biochemical alterations induced by carbon tetrachloride.
Cystamine significantly prevented the necrosis and fatty infiltration, as well as the depression of glucose 6-phosphatase and ethylmorphine N -demethylase activities caused by oral CCl 4 administration, and significantly blocked the irreversible binding of 14 C from 14 C Cl 4 to liver microsomal lipids and the depression in spite of the fact that themicrosomal lipid peroxidation process was not inhibited.
Protection against paraquat-induced toxicity with sulfite or thiosulfate in mice.
The results suggest that the preventive effect against paraquat-induced toxicity with thiosulfate or sulfite may involve the glutathione-dependent detoxication in mice.
N-acetyl cysteine is an early but also a late preventive agent against carbon tetrachloride-induced liver necrosis.
N-Acetyl cysteine treatment 30 min before or 6 or 10 h after carbon tetrachloride administration significantly prevented the liver necrosis produced by the hepatotoxin at 24 h, and results suggest that early and late protective effects of NAC might be attributable to its prior conversion to Cysteine and glutathione.
Action of malotilate on reduced serum cholesterol level in rats with carbon tetrachloride-induced liver damage.
The results suggest that the mode of action by which serum cholesterol is normalized in rats with fatty liver is probably due to a stimulative effect of malotilate on hepatic cholesterol synthesis and cholesterol secretion from the liver.
Effect of cycloheximide and actinomycin D on carbon tetrachloride hepatotoxicity.
Observations support the concept that protein synthesis plays an active role in the production of cellular damage produced by CCl4.
Studies on fatty liver with isolated hepatocytes. I. The action of colchicine, phalloidin, cytochalasin B, and cyclohexamide on protein and triglyceride synthesis and secretion.
All four drugs reduce the secretion of proteins by hepatocytes, through different mechanisms, impair lipoprotein secretion and induce an accumulation of triglycerides within the liver cell.
Impaired glycosylation in liver microsomes of orotic-acid-fed rats.
In rats fed orotic acid, the incorporation in liver subcellular fractions of sugars injected intraperitonealy is altered only for mannose, but not for fucose or galactose, and Kinetic studies suggest that there is deficiency of both enzyme and endogenous dolichyl phosphate.
Estimation of Plasma Phosphatase by Determination of Hydrolysed Phenol with Amino-antipyrine
The conditions under which enzymic hydrolysis is carried out are the same as in the King-Armstrong method, as modified by King (1951), the amino-antipyrine reagent (A.A.P.) being used to estimate the phenol liberated.