Biotransformation of anthelmintics and the activity of drug-metabolizing enzymes in the tapeworm Moniezia expansa
Jazyk angličtina Země Velká Británie, Anglie Médium print-electronic
Typ dokumentu časopisecké články
PubMed
25373326
DOI
10.1017/s0031182014001711
PII: S0031182014001711
Knihovny.cz E-zdroje
- Klíčová slova
- albendazole,
- 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
- Názvy látek
- albendazol MeSH
- alkoholoxidoreduktasy MeSH
- anthelmintika MeSH
- flubendazole MeSH Prohlížeč
- glukuronosyltransferasa MeSH
- glutathiontransferasa MeSH
- izoenzymy MeSH
- katalasa MeSH
- mebendazol MeSH
- multienzymové komplexy MeSH
- NADH, NADPH oxidoreduktasy MeSH
- oxygenasy se smíšenou funkcí MeSH
- peroxidasa MeSH
- superoxiddismutasa MeSH
- systém (enzymů) cytochromů P-450 MeSH
- thioredoxin glutathione reductase MeSH Prohlížeč
- UGT1A1 enzyme MeSH Prohlížeč
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.
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