Phase I biotransformation of albendazole in lancet fluke (Dicrocoelium dendriticum)
Jazyk angličtina Země Velká Británie, Anglie Médium print-electronic
Typ dokumentu časopisecké články, práce podpořená grantem
PubMed
18565554
DOI
10.1016/j.rvsc.2008.05.006
PII: S0034-5288(08)00110-0
Knihovny.cz E-zdroje
- MeSH
- albendazol analogy a deriváty farmakokinetika MeSH
- anthelmintika farmakokinetika MeSH
- biotransformace MeSH
- Dicrocoelium metabolismus MeSH
- dikrocelióza parazitologie veterinární MeSH
- nemoci jater parazitologie veterinární MeSH
- nemoci ovcí parazitologie MeSH
- ovce MeSH
- reprodukovatelnost výsledků MeSH
- zvířata MeSH
- Check Tag
- ženské pohlaví MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- albendazol MeSH
- albendazole sulfoxide MeSH Prohlížeč
- anthelmintika 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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