Phase I biotransformation of albendazole in lancet fluke (Dicrocoelium dendriticum)
Language English Country Great Britain, England Media print-electronic
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
18565554
DOI
10.1016/j.rvsc.2008.05.006
PII: S0034-5288(08)00110-0
Knihovny.cz E-resources
- MeSH
- Albendazole analogs & derivatives pharmacokinetics MeSH
- Anthelmintics pharmacokinetics MeSH
- Biotransformation MeSH
- Dicrocoelium metabolism MeSH
- Dicrocoeliasis parasitology veterinary MeSH
- Liver Diseases parasitology veterinary MeSH
- Sheep Diseases parasitology MeSH
- Sheep MeSH
- Reproducibility of Results MeSH
- Animals MeSH
- Check Tag
- Female MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- Albendazole MeSH
- albendazole sulfoxide MeSH Browser
- Anthelmintics MeSH
Dicroceliosis, a lancet fluke infection, is a frequent parasitosis of small ruminants and the anthelmintic drug albendazole (ABZ) is effective in control of this parasitosis. The aim of our project was to study the metabolism of ABZ and ABZ sulphoxide (ABZ.SO) in lancet fluke. Both invitro (subcellular fractions of fluke homogenates) and exvivo experiments (adult flukes cultivated in medium) were performed for this purpose. ABZ was metabolised invitro by lancet fluke NADPH-dependent enzymes by two oxidative steps (sulphoxidation and sulphonation). The apparent kinetic parameters of these reactions have been determined. In the exvivo experiments, only ABZ sulphoxidation was observed. The stereospecificity in ABZ sulphoxidation invitro was slight, with preferential formation of (+)-ABZ.SO enantiomer. In contrast (-)-ABZ.SO formation predominated in exvivo experiments. Sulphoreduction of ABZ.SO occurred neither invivo nor exvivo. The detection of ABZ oxidative metabolites indicates the presence of drug metabolising oxidases in lancet fluke.
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