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Biomedical subjects

M Semonský

Publications and source records attributed to M Semonský.

At least 19 recordsLinked to original sources

Effect of azathioprine on antibody formation in mice and its modification by delta-(2-amino-6-hydroxy-3,4-dihydro-4-oxo-5-pyrimidinyl)-valeric acid.

The effects of azathioprine, either alone or combined with delta-(2-amino-6-hydroxy-3,4-dihydro-4-oxo-5-pyrimidinyl)-valeric acid (VUFB-9777, Damvar) on serum antibody formation was studied in mice. The immunosuppressive effect of azathioprine depended on the regimen of administration. VUFB-9777 alone produced no immunosuppressive effect but markedly enhanced that of azathioprine.

Animals↗

Diminution of prostate by ergoline derivative VUFB--6638 (Dironyl) in rats.

Experiments in male rats showed that the administration of prolactin secretion inhibitor-N-(D-6-methyl-8-isoergolin-I-yl)-N', N'-diethylurea -- led to a decrease of prostate weight, while a simultaneous administration of prolactin prevented this effect. The histological examination showed that the quantity of secretions in the prostate glands are decreased.

Animals↗

Effect of chloro- and bromo-derivatives of isocrotonic acid of bioenergetic processes in Ehrlich ascites cells and isolated mitochondria.

The effect of nine chloro- and bromoderivatives of isocrotonic acid on some bioenergetic processes in both Ehrlich ascites cells and isolated rat liver mitochondria has been investigated. Substances studied in the concentration range 25--200 microM significantly inhibited incorporation of both 14C-adenine and 14C-valine into acid-insoluble material of Ehrlich ascites cells. The rate of 14C-precursors incorporation being directly related to the concentration of the inhibitor. Gamma,gamma-bis-4-ethylphenyl-alpha,beta-dichloroisocrotonic acid fully inhibits both aerobic glucose utilization and lactic acid formation at 200 microM concentration. At lower concentrations, however, glycolysis is stimulated. Maximal stimulation of rat liver mitochondrial respiration in state 4 with succinate as substrate was reached at concentrations as low as 10 microM. On the other hand, these substances were able to release by the oligomycin inhibited respiration of rat liver mitochondria. Our data suggest that cytotoxic and cancerostatic action of isocrotonic acid derivatives lies primarily in the exclusion of key processes in the energy metabolism of Ehrlich ascites cells and isolated mitochondria.

Animals↗

Biochemistry of drugs. XXIV. Substances with antineoplastic effect. LXII. Pharmacokinetics of gamma,gamma-bis-4-ethylphenyl-alpha,beta-dibromoisocrotonic acid-3H (Edikron-3H) in experimental animals.

After oral administration of Edikron-3H to mice with mammary gland adenocarcinoma HK, within 24 h after ingestion almost 50% of administered radioactivity was excreted (16% in urine, 33% in faeces), and within 4 day it was almost 80% (27% in urine, 50% in faeces). Like in mice, also in dogs the faecal excretion preponderated. In mice, the levels in most tissues and blood culminated at hour 6 after administration of the substance. Relatively high levels were found in the liver, the levels in other tissues and blood being substantially lower in comparison. The levels in the tumor were initially low, later on they rose, and culminated at hour 24. Besides, it was found that the transfer of radioactivity by milk into the sucklings' bodies was relatively low, and radioactivity penetration into fetuses was negligible. In urine, unchanged parent substance was present in very slight amounts only.

Adenocarcinoma↗

Biochemistry of drugs. XXV. Substances with antineoplastic effect. LXIII. Pharmacokinetics of delta-/2-amino-6-hydroxy-3,4-dihydro-4-oxo-5--pyrimidinyl/valeric acid-14C (Damvar-14C) in experimental animals.

In experiments on H mice and Wistar rats it was found that radioactivity was excreted after subcutaneous injection of Damvar-14C preponderantly in urine, and after oral administration, in faeces. After subcutaneous injection the urinary excretion set on very fast. After subcutaneous injection of Damvar-14C to H mice with Crocker's ascitic sarcoma S 180, peak radioactivity values were found in the majority of organs, blood, and ascitic fluid at hour 1 after injection; in the kidneys the peak value appeared as late as at hour 6. The renal levels were conspicuously higher than the other ones. Relatively high radioactivity levels were found in the ascitic fluid, skin, and blood. After oral administration the radioactivity levels in all organs, blood, and ascitic fluid culminated at hour 3 after ingestion. The highest levels after oral administration were likewise found in the kidneys and ascitic fluid. With the exception of the kidneys, blood, and skin, the peak values of specific radioactivity in organs were equally high or even higher after oral than after subcutaneous administration of the labeled substance. Furthermore, it was found that after administration of Damvar-14C to rat mothers the transfer of radioactivity into the milk and then into the sucklings was very slight, and so was the penetration of radioactivity into fetuses.

Administration, Oral↗

Biochemistry of drugs XXIII. Substance with antineoplastic acitivity LX. Pharmacokinetics of cis-beta-4-pentoxybenzoyl-beta-bromoacrylic acid (cis: Br, H)-3H (Penberol-3H).

After oral administration of Penberol-3H to mice with mammary gland adenocarcinoma HK, within 4 days 50% of the administered radioactivity was excreted in the urine, and 36% in the faeces. In dogs the excretion rates were slower. It was found that after oral administration of Penberol-3H to rats, radioactivity was excreted in the bile. After oral administration of Penberol-3H to mice with mammary gland adenocarcinoma, high specific radioactivities (per gram of tissue) were found in the liver, kidneys, lungs, and ovaries. Besides, it was found that after oral administration of Penberol-3H to nursing female rats the radioactivity was little eliminated in the milk, and in pregnant females its penetration into the fetuses was negligible.

Acrylates↗