Biotransformation of anthelmintics and the activity of drug-metabolizing enzymes in the tapeworm Moniezia expansa
Language English Country Great Britain, England Media print-electronic
Document type Journal Article
PubMed
25373326
DOI
10.1017/s0031182014001711
PII: S0031182014001711
Knihovny.cz E-resources
- Keywords
- albendazole,
- MeSH
- Albendazole pharmacokinetics pharmacology MeSH
- Alcohol Oxidoreductases metabolism MeSH
- Anthelmintics pharmacokinetics pharmacology MeSH
- Biotransformation MeSH
- Cestoda drug effects enzymology ultrastructure MeSH
- Glucuronosyltransferase metabolism MeSH
- Glutathione Transferase metabolism MeSH
- Isoenzymes metabolism MeSH
- Catalase metabolism MeSH
- Mebendazole analogs & derivatives pharmacokinetics pharmacology MeSH
- Monieziasis parasitology MeSH
- Multienzyme Complexes metabolism MeSH
- NADH, NADPH Oxidoreductases metabolism MeSH
- Sheep Diseases parasitology MeSH
- Sheep MeSH
- Oxidation-Reduction MeSH
- Mixed Function Oxygenases metabolism MeSH
- Peroxidase metabolism MeSH
- Superoxide Dismutase metabolism MeSH
- Cytochrome P-450 Enzyme System metabolism MeSH
- Intestine, Small parasitology MeSH
- Animals MeSH
- Check Tag
- Animals MeSH
- Publication type
- Journal Article MeSH
- Names of Substances
- Albendazole MeSH
- Alcohol Oxidoreductases MeSH
- Anthelmintics MeSH
- flubendazole MeSH Browser
- Glucuronosyltransferase MeSH
- Glutathione Transferase MeSH
- Isoenzymes MeSH
- Catalase MeSH
- Mebendazole MeSH
- Multienzyme Complexes MeSH
- NADH, NADPH Oxidoreductases MeSH
- Mixed Function Oxygenases MeSH
- Peroxidase MeSH
- Superoxide Dismutase MeSH
- Cytochrome P-450 Enzyme System MeSH
- thioredoxin glutathione reductase MeSH Browser
- UGT1A1 enzyme MeSH Browser
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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