Ivermectin (IVE), one of the most important anthelmintics, is often used in the treatment of haemonchosis in ruminants. The objective of our work was (1) to find and identify phase I and II metabolites of IVE formed by the Barber's pole worm (Haemonchus contortus), and (2) to compare IVE metabolites in helminths with IVE biotransformation in sheep (Ovis aries) as host species. Ultrahigh-performance liquid chromatography/tandem mass spectrometry (UHPLC/MS/MS) was used for this purpose. During in vitro incubations, microsomes (from adult worms or from ovine liver) and a primary culture of ovine hepatocytes were incubated with IVE. In the ex vivo study, living H. contortus adults were incubated in the presence of 1 μM IVE for 24 h. The results showed that the H. contortus enzymatic system is not able to metabolize IVE. On the other hand, 7 different phase I as well as 9 phase II IVE metabolites were detected in ovine samples using UHPLC/MS/MS analyses. Most of these metabolites have not been described before. Haemonchus contortus is not able to deactivate IVE through biotransformation; therefore, biotransformation does not contribute to the development of IVE-resistance in the Barber's pole worm.

• MeSH
• anthelmintika chemie   metabolismus   terapeutické užití   MeSH
• chromatografie kapalinová MeSH
• Haemonchus účinky léků   růst a vývoj   metabolismus   MeSH
• hemonchóza farmakoterapie   parazitologie   veterinární   MeSH
• hepatocyty metabolismus   MeSH
• hmotnostní spektrometrie MeSH
• ivermektin chemie   metabolismus   terapeutické užití   MeSH
• kultivované buňky MeSH
• mikrozomy metabolismus   MeSH
• nemoci ovcí farmakoterapie   parazitologie   MeSH
• ovce domácí metabolismus   MeSH
• ovce metabolismus   MeSH
• zvířata MeSH
• Check Tag
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• Názvy látek
• anthelmintika MeSH
• ivermektin MeSH

Monepantel (MOP) belongs to a new class of anthelmintic drugs known as aminoacetonitrile derivatives. It was approved for use in veterinary practice in Czech Republic in 2011. So far, biotransformation and transport of MOP in target animals have been studied insufficiently, although the study of metabolic pathways of anthelmintics is very important for the efficacy of safety of therapy and evaluation of the risk of drug-drug interactions. The aim of this study was to identify MOP metabolites and to suggest the metabolic pathways of MOP in sheep. For this purpose, primary culture of ovine hepatocytes was used as a model in vitro system. After incubation, medium samples and homogenates of hepatocytes were extracted separately using solid-phase extraction. Analysis was performed using a hybrid quadrupole-time-of-flight analyzer with respect to high mass accuracy measurements in full scan and tandem mass spectra for the confirmation of an elemental composition. The obtained results revealed S-oxidation to sulfoxide and sulfone and arene hydroxylation as MOP phase I biotransformations. From phase II metabolites, MOP glucuronides, sulfates, and acetylcysteine conjugates were found. Based on the obtained results, a scheme of the metabolic pathway of MOP in sheep has been proposed.

• MeSH
• aminoacetonitrily analogy a deriváty   metabolismus   MeSH
• anthelmintika metabolismus   MeSH
• extrakce na pevné fázi MeSH
• hepatocyty metabolismus   MeSH
• kultivované buňky MeSH
• metabolické sítě a dráhy MeSH
• ovce metabolismus   MeSH
• tandemová hmotnostní spektrometrie MeSH
• vysokoúčinná kapalinová chromatografie MeSH
• zvířata MeSH
• Check Tag
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• Názvy látek
• aminoacetonitrily MeSH
• anthelmintika MeSH
• monepantel MeSH Prohlížeč

Supplementation of the rumen ciliate Diploplastron affine growth medium with commercial chitin stimulated growth of ciliates and the density of their population was positively correlated with chitin doses (r = 0.95; p < 0.01). The cell-free extracts prepared from bacteria-free ciliates degraded chitin to N-acetyl-D: -glucosamine and chitobiose. Three exochitinases, two endochitinases and two beta-N-acetylglucosaminidases were identified in the cell-free extract of protozoa. The molar mass of exochitinases was 80, 65 and 30 kDa, and endochitinases 75 and 50 kDa; the molar mass of one of the identified beta-N-acetylglucosaminidases was 45 kDa.

• MeSH
• bachor metabolismus   parazitologie   MeSH
• chitin metabolismus   MeSH
• chitinasy chemie   klasifikace   metabolismus   MeSH
• Ciliophora enzymologie   růst a vývoj   MeSH
• kultivační média chemie   MeSH
• ovce metabolismus   parazitologie   MeSH
• protozoální proteiny klasifikace   metabolismus   MeSH
• zvířata MeSH
• Check Tag
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• Názvy látek
• chitin MeSH
• chitinasy MeSH
• kultivační média MeSH
• protozoální proteiny MeSH

Conjugal transfer between soil bacterial population and microorganisms isolated from the rumen of herbivores from mercury-polluted area was investigated. The transfer of merA encoding mercury-resistance plasmids from soil bacteria Enterobacter cloacae and Enterococcus durans into two ruminal isolates Citrobacter freundii and Bacillus subtilis was observed. Approximately the same frequency of mobilization in mating experiments was observed for both Gram-negative (approximately 2.5 x 10(-8), transconjugants-to-recipient ratio) and Gram-positive (approximately 1.3 x 10(-8)) bacteria.

• MeSH
• bachor mikrobiologie   MeSH
• Bacillus subtilis genetika   metabolismus   MeSH
• biodegradace MeSH
• Citrobacter freundii genetika   metabolismus   MeSH
• DNA fingerprinting MeSH
• konjugace genetická * MeSH
• látky znečišťující půdu metabolismus   MeSH
• ovce metabolismus   mikrobiologie   MeSH
• oxidoreduktasy genetika   metabolismus   MeSH
• přenos genů horizontální genetika   MeSH
• půdní mikrobiologie * MeSH
• rtuť metabolismus   MeSH
• zvířata MeSH
• Check Tag
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• Geografické názvy
• Slovenská republika MeSH
• Názvy látek
• látky znečišťující půdu MeSH
• mercuric reductase MeSH Prohlížeč
• oxidoreduktasy MeSH
• rtuť MeSH

Albendazole (ABZ) biotransformation was studied in vitro in liver microsomes of adult noncastrated male farm animals (ram, buck, bull and boar), castrated adult males (wether, billy and hog), and free living males (fallow buck, red deer stag, mouflon ram, roe buck and wild boar). Liver microsomal fractions were incubated with either ABZ or racemic albendazole sulphoxide (ABZSO). ABZ was extensively metabolized to the (+) and (-) enantiomers of ABZSO, whereas ABZSO underwent a slow oxidation to albendazole sulphone (ABZSO2) in all species. In all species both ABZSO enantiomers were detected. The chiral ratio, (+)-ABZSO/(-)-ABZSO, was greater than one in farm animals, mouflon and wild boar, and less than one in three species of deer. For total ABZ sulphoxidation, deer like species had lower values compared to the other species. Mouflon ram and ram had lower total sulphoxidation rates compared to wethers, as well as ABZ suphoxidation towards (+)-ABZSO. No significant difference occurred comparing ABZSO formation in mouflon ram and ram, but ABZSO2 formation rate in mouflon ram was higher than in rams and wethers. Roe deer stag, fallow buck and red deer stag did not differ in both total-ABZSO and (-)-ABZSO synthesis rates and roe deer stag and fallow buck did not differ in synthesis rates of (+)-ABZSO and ABZSO2. The bull differed from other species in all metabolites studied, except for red deer stag and boar in (-)-ABZSO synthesis rate. The extent of ABZSO sulphonation to ABZSO2 in bull microsomes was more than twice that of other species.

• MeSH
• albendazol analogy a deriváty   chemie   farmakokinetika   MeSH
• anthelmintika chemie   farmakokinetika   MeSH
• biotransformace MeSH
• divoká zvířata metabolismus   MeSH
• jaterní mikrozomy metabolismus   MeSH
• ovce metabolismus   MeSH
• oxidace-redukce MeSH
• prasata metabolismus   MeSH
• skot metabolismus   MeSH
• vysoká zvěř metabolismus   MeSH
• zvířata MeSH
• Check Tag
• mužské pohlaví MeSH
• skot metabolismus   MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• hodnotící studie MeSH
• práce podpořená grantem MeSH
• srovnávací studie MeSH
• Názvy látek
• albendazol MeSH
• albendazole sulfoxide MeSH Prohlížeč
• anthelmintika MeSH

The effect of nisin (in the form of Nisaplin) was determined using two species of rumen ciliate protozoa in vitro, on their co-culture bacterial population, and volatile fatty acid concentration. Nisaplin did not affect the in vitro growth of Entodinium caudatum at concentrations of 50-400 mg/L during short-term treatment (5 d). Long-term application (30 d) of Nisaplin (100 mg/L) significantly decreased growth of the Epidinium ecaudatum forma caudatum et ecaudatum but not growth of E. caudatum. Nisaplin moderately supported the growth of E. caudatum after omission of wheat gluten (source of amino acids for protozoan growth). An inhibition of Gram-positive facultative anaerobic bacterial population in the protozoan cultures (lactobacilli, enterococci, staphylococci and amylolytic streptococci) was observed during long-term Nisaplin treatment. The concentration of volatile fatty acids significantly increased during the long-term Nisaplin treatment of both cultures. The propionate concentration in the mixture of volatile fatty acids was nearly twice higher on the account of the decreased concentration (from 74 to 63%) of acetate.

• MeSH
• bachor metabolismus   MeSH
• bakteriociny farmakologie   MeSH
• Ciliophora účinky léků   růst a vývoj   metabolismus   MeSH
• gramnegativní fakultativně anaerobní tyčinky růst a vývoj   metabolismus   MeSH
• grampozitivní bakteriální infekce prevence a kontrola   MeSH
• kyseliny mastné těkavé metabolismus   MeSH
• nisin farmakologie   MeSH
• ovce metabolismus   MeSH
• počet mikrobiálních kolonií MeSH
• vysoká zvěř metabolismus   MeSH
• zvířata MeSH
• Check Tag
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• Názvy látek
• bakteriociny MeSH
• kyseliny mastné těkavé MeSH
• nisin MeSH

By the modification of the methods which are used for determination of amino acid uptake in the mammary gland and in the small intestine the uptake of 14C-lysine was measured in two parts of the sheep rumen epithelium in vitro. Three various lysine concentrations were used (0.95; 4.95 and 9.95 mM/l). Duration of the incubation was 15, 30 or 60 minutes. Comparison of the lysine distribution ratios as depending upon the duration of incubation period in the dorsal rumen sac at 9.95 mM/l concentration revealed significant differences between at the 15 min and 60 min incubation (0.952 +/- 0.089 vs 1.931 +/- 0.108; P < 0.05, respectively) and between 30 min and 60 min incubation (1.165 +/- 0.138 vs 1.931 +/- 0.108, P < 0.05, respectively)-Fig. 1. Comparison of the lysine distribution ratios as depending upon the duration of incubation period in the ventral rumen sac at 4.95 mM/l concentration revealed significant differences between the incubations of 15 and 30 min (1.182 +/- 0.131 vs 1.742 +/- 0.113; P < 0.05, respectively) and between the incubations of 15 and 60 min (1.182 +/- 0.131 vs 2.10 +/- 0.204; P < 0.05, respectively)-Fig. 2. Comparison of the lysine distribution ratios in both the dorsal and ventral sac as depending upon the duration of incubation period after 15 min incubation revealed a significant difference at the 4.95 mM/l concentration 1.619 +/- 0.078 vs 1.182 +/- 0.131; P < 0.05, respectively)-Fig. 3. Our results showed that the lysine uptake in the dorsal and ventral sheep rumen epithelium is dependent on the incubation duration only under certain concentrations of lysine. Differences in absorption of lysine between dorsal and ventral rumen epithelium are not mostly significant.

• MeSH
• bachor metabolismus   MeSH
• epitel metabolismus   MeSH
• lysin metabolismus   MeSH
• ovce metabolismus   MeSH
• zvířata MeSH
• Check Tag
• ženské pohlaví MeSH
• zvířata MeSH
• Publikační typ
• anglický abstrakt MeSH
• časopisecké články MeSH
• Názvy látek
• lysin MeSH

Clinical pattern and dynamics of some biochemical indicators were observed in six four-year lambing ewes of the Improved Wallachian breed in the course of 32-day administration of magnesite fly ash. A daily dose of the tested fly ash with the content of 305,000 mg/kg magnesium amounted to 500 mg/kg live weight of sheep. The intake of concentrate mixture with magnesium content in the test sheep decreased by a third between the 12th and 20th day, by another half between the 20th and 26th day and the intake was minimum to nil during the last seven days of the trial. The decrease in the intake of concentrate mixture was accompanied by increased water consumption and by gradual inappetence for hay. Shaped droppings started to change their consistency to slurry consistency from the 12th day of observation. Thinner to watery consistency of excrements appeared in all sheep between the 15th and 20th day and diarrheas persisted in all animals until the end of the trial. The indicators of hematological profile did not show an undoubted relationship to the administration of tested magnesium, and the variations in the particular indicators observed during the trial were within the physiological range. Serum enzymes showed a significant increase against the starting values only in the concentration of alanine aminotransferase on day 20 and day 26 (p < 0.05 and/or p < 0.001). An increase in the proteosynthetic activity of hepatocytes signalled a statistically significant increase in total proteins (p < 0.05), total immunoglobulins (p < 0.05) and an insignificant increase in albumin content. Out of the analyzed mineral elements, magnesium content showed the most significant relationship to administration of industrial pollutants as its significant increase in blood serum, urine and droppings was observable since day 20 (p < 0.05, p < 0.01 and p < 0.001, respectively). The dynamics of calcium, phosphorus, potassium, sodium, iron, copper, zinc, molybdenum, arsenic and cadmium concentrations showed different patterns in the blood serum, droppings and urine of sheep in the course of magnesite fly ash feeding, and the evaluation of interactions with magnesium requires further studies.

• MeSH
• hořčík toxicita   MeSH
• látky znečišťující životní prostředí toxicita   MeSH
• nemoci ovcí chemicky indukované   MeSH
• ovce metabolismus   MeSH
• průjem chemicky indukované   veterinární   MeSH
• zvířata MeSH
• Check Tag
• ženské pohlaví MeSH
• zvířata MeSH
• Publikační typ
• anglický abstrakt MeSH
• časopisecké články MeSH
• Názvy látek
• hořčík MeSH
• látky znečišťující životní prostředí MeSH
• magnesium carbonate MeSH Prohlížeč

The oxidative processes in the organism are activated by hormones of the thyroid gland. The pyruvate-lactate component catalyzed by lactate dehydrogenase presents one of the important oxidic-reductive systems in the animal organism of biochemical importance (EC. 1.1.1.27). In certain cases of the thyroid gland disturbances antithyroid drugs, such as derivatives of thiouracil, mercaptoimidazole and some others may be used for the treatment of men and animals (Marchant et al., 1979; Negwer, 1987). In the present study, the activity changes of lactate dehydrogenase isoenzymes in the blood plasma of young rams and ewe hoggets in experiments with carbimasole [carbimasolum(1-carbaethoxy-3-methyl-2-thioimidazolum) ] have been studied. The dose of carbimasole at the time of sampling (May, 1993) was 7O mg per animals and day. In May, no significant differences in T3 and T4 concentrations in the serum of experimental and control animals in males and females were found (Tab. 1). The T3 concentrations in the experimental group of young rams were 0.56 +/- 0.21 nmol/l (n = 3), in ewe hoggets 0.70 +/- 0.19 nmol/l (n = 6). The T4 concentrations in young rams were 39.15 +/- 24.15 nmol/l (n = 3), in ewe hoggets 48.6 +/- 15.3 nmol/l (n = 6). Out of lactate dehydrogenase isoenzymes, only LD4 exhibited significant differences (P < 0.02) in the blood plasma of ewe hoggets (Tab. I). In the course of these months, no clinical signs of hypothyrosis were observed in experimental animals.

• MeSH
• hormony štítné žlázy krev   MeSH
• izoenzymy MeSH
• karbimazol farmakologie   MeSH
• L-laktátdehydrogenasa krev   MeSH
• ovce metabolismus   MeSH
• thyreostatika farmakologie   MeSH
• zvířata MeSH
• Check Tag
• mužské pohlaví MeSH
• ženské pohlaví MeSH
• zvířata MeSH
• Publikační typ
• anglický abstrakt MeSH
• časopisecké články MeSH
• Názvy látek
• hormony štítné žlázy MeSH
• izoenzymy MeSH
• karbimazol MeSH
• L-laktátdehydrogenasa MeSH
• thyreostatika MeSH

The efficiency of the sorbent prepared by immobilization of [Iron(II)hexacyanoferrate(II)] on clinoptilolite--marked as ZEOFe--in reduction of the radiocaesium Cs-137 has been in vivo investigated in sheep. It was found that an application of this modified clinoptilolite affected both primary and secondary resorption of Cs-137 also by interrupting the enteral cycle of radiocaesium in sheep. It was proved that ZEOFe accelerated approx. twice the excretion of Cs-137 from sheep's body. The whole effect resulted in 15 to 50 times lowering of the equilibrium concentration of radiocaesium in the case of constant intake of the contaminated feed and simultaneous application of 50 grams of ZEOFe daily. The actual reduction depends mainly on the way of administration. The reduction of Cs-137 by non-modified clinoptilolite--ZEO--has been investigated, too. More than 10x lower sorption efficiency has been observed in comparison with ZEOFe.

• MeSH
• ovce metabolismus   MeSH
• radioizotopy cesia farmakokinetika   MeSH
• zeolity farmakologie   MeSH
• zvířata MeSH
• Check Tag
• zvířata MeSH
• Publikační typ
• anglický abstrakt MeSH
• časopisecké články MeSH
• práce podpořená grantem MeSH
• Názvy látek
• clinoptilolite MeSH Prohlížeč
• radioizotopy cesia MeSH
• zeolity MeSH