- MeSH
- COVID-19 prevence a kontrola MeSH
- epidemie prevence a kontrola MeSH
- koronavirové infekce prevence a kontrola MeSH
- ochranné prostředky zásobování a distribuce MeSH
- přenos infekční nemoci prevence a kontrola MeSH
- vláda MeSH
- Publikační typ
- populární práce MeSH
- Geografické názvy
- Česká republika MeSH
- Klíčová slova
- prezident,
- MeSH
- COVID-19 prevence a kontrola MeSH
- koronavirové infekce prevence a kontrola MeSH
- přenos infekční nemoci prevence a kontrola MeSH
- Publikační typ
- populární práce MeSH
- Geografické názvy
- Česká republika MeSH
- O autorovi
- Zeman, Miloš, 1944- Autorita
1. Giant liver fluke Fascioloides magna is a dangerous parasite, which infects herbivores. It was imported to Europe from North America and started to spread. Benzimidazoles like albendazole, mebendazole, triclabendazole and salicylanilides closantel and rafoxanide are the most used anthelmintics to control fascioloidosis. However their effect might be altered via drug-metabolizing enzymes of this parasite. 2. The aim of our study was to determine the activities of drug-metabolizing enzymes in F. magna and the metabolism of above mentioned anthelmintics. 3. Activities of several oxidative, reductive and conjugative enzymes towards various model xenobiotic substrates were found in F. magna subcellular fractions. 4. Subcellular fractions from F. magna oxidized albendazole to its sulphoxide metabolite and reduced mebendazole to hydroxyl-mebendazole. Under ex vivo conditions, only very-low concentrations of these compounds were detected using high-performance liquid chromatography/mass spectrometry. 5. The results indicate that the giant liver fluke possesses the active xenobiotic-metabolizing system. The overexpression of this system may play an important role in parasite resistance against these anthelmintics.
- MeSH
- albendazol metabolismus MeSH
- anthelmintika metabolismus MeSH
- benzimidazoly metabolismus MeSH
- Fasciola hepatica účinky léků enzymologie MeSH
- mebendazol metabolismus MeSH
- rafoxanid metabolismus MeSH
- salicylanilidy metabolismus MeSH
- sulfoxidy metabolismus MeSH
- vysokoúčinná kapalinová chromatografie MeSH
- xenobiotika metabolismus MeSH
- zvířata MeSH
- Check Tag
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
Albendazole (ABZ), widely used benzimidazole anthelmintic, administered to animals enters via excrements into environment and may impact non-target organisms. Moreover, exposure of lower development stages of helminths to anthelmintics may also encourage the development of drug-resistant strains of helminths. In present project, the kinetics of ABZ (10 mg kg(-1) p.o.) and its metabolite (ABZ.SO, ABZSO2) elimination in faeces from treated Texel lambs were studied using UHPLC/MS/MS with the aim to find out their concentrations achievable in the environment. Consequently, the effect of these compounds on lower development stages of Barber's pole worm (Haemonchus contortus) and on germination of white mustard (Sinapis alba) seeds was evaluated. The results showed that ABZ concentrations in faeces excreted in 4-60 h after treatment were above the concentrations lethal for H. contortus eggs. Moreover, pre-incubation with sub-lethal doses of ABZ and ABZ.SO did not increase the resistance of H. contortus eggs and larvae to anthelmintics. On the other hand, concentrations of ABZ and ABZ.SO in faeces are so high that might have negative influence on non-target soil invertebrates. As neither ABZ nor its metabolites affect the germination of mustard seeds, phytoremediation could be considered as potential tool for detoxification of ABZ in the environment.
- MeSH
- albendazol analýza farmakologie MeSH
- feces chemie MeSH
- Haemonchus účinky léků růst a vývoj MeSH
- hořčice rodu Sinapis účinky léků růst a vývoj MeSH
- klíčení účinky léků MeSH
- ovce MeSH
- semena rostlinná účinky léků MeSH
- tandemová hmotnostní spektrometrie MeSH
- vysokoúčinná kapalinová chromatografie MeSH
- zvířata MeSH
- Check Tag
- mužské pohlaví MeSH
- ženské pohlaví MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
The sheep tapeworm Moniezia expansa is very common parasite, which affects ruminants such as sheep, goats as well as other species. The benzimidazole anthelmintics albendazole (ABZ), flubendazole (FLU) and mebendazole (MBZ) are often used to treat the infection. The drug-metabolizing enzymes of helminths may alter the potency of anthelmintic treatment. The aim of our study was to assess the activity of the main drug-metabolizing enzymes and evaluate the metabolism of selected anthelmintics (ABZ, MBZ and FLU) in M. expansa. Activities of biotransformation enzymes were determined in subcellular fractions. Metabolites of the anthelmintics were detected and identified using high performance liquid chromatography/ultra-violet/VIS/fluorescence or ultra-high performance liquid chromatography/mass spectrometry. Reduction of MBZ, FLU and oxidation of ABZ were proved as well as activities of various metabolizing enzymes. Despite the fact that the conjugation enzymes glutathione S-transferase, UDP-glucuronosyl transferase and UDP-glucosyl transferase were active in vitro, no conjugated metabolites of anthelmintics were identified either ex vivo or in vitro. The obtained results indicate that sheep tapeworm is able to deactivate the administered anthelmintics, and thus protects itself against their action.
- MeSH
- albendazol farmakokinetika farmakologie MeSH
- alkoholoxidoreduktasy metabolismus MeSH
- anthelmintika farmakokinetika farmakologie MeSH
- biotransformace MeSH
- Cestoda účinky léků enzymologie ultrastruktura MeSH
- glukuronosyltransferasa metabolismus MeSH
- glutathiontransferasa metabolismus MeSH
- izoenzymy metabolismus MeSH
- katalasa metabolismus MeSH
- mebendazol analogy a deriváty farmakokinetika farmakologie MeSH
- monieziáza parazitologie MeSH
- multienzymové komplexy metabolismus MeSH
- NADH, NADPH oxidoreduktasy metabolismus MeSH
- nemoci ovcí parazitologie MeSH
- ovce MeSH
- oxidace-redukce MeSH
- oxygenasy se smíšenou funkcí metabolismus MeSH
- peroxidasa metabolismus MeSH
- superoxiddismutasa metabolismus MeSH
- systém (enzymů) cytochromů P-450 metabolismus MeSH
- tenké střevo parazitologie MeSH
- zvířata MeSH
- Check Tag
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
