Liver sulphoxidative metabolism of albendazole in rat: enantioselectivity and effect of methimazole.
The aim of the present work was to evaluate the effects of methimazole (MTZ) on the enantioselective sulphoxidation of albendazole (ABZ) by rat liver microsomes and tissue slices. Albendazole sulphoxide (ABZSO) was the metabolite recovered after the incubation with ABZ in both liver preparations. MTZ significantly reduced ABZSO production both in microsomes and slices. ABZSO production decreased as a function of MTZ concentration. The sulphoxidation reaction performed by rat liver explants in the presence of MTZ was 65% lower than that observed in controls. The reduction in the production of ABZSO in the presence of MTZ was mainly due to a lower production of (+) ABZSO. The results reported further contribute to the understanding of the enantioselective metabolism of ABZ. In addition, the work presented provides information on the comparison of two different liver tissue preparations for the evaluation of xenobiotic metabolism.
Solana
H D
HD
Laboratorio de Biología Celular, Facultad de Ciencias Veterinarios, Universidad Nacional del Centro de la Provincia de Buenos Aires, Tandil, Argentina. hsolana@vet.unicen.edu.ar
Sallovitz
J M
JM
Najle
R
R
Rodriguez
J A
JA
Lanusse
C E
CE
D015766:Albendazole / Q000378:metabolism*; D000818:Animals; D000871:Anthelmintics / Q000378:metabolism*; D013956:Antithyroid Agents / Q000494:pharmacology*; D008099:Liver / Q000378:metabolism*; D008713:Methimazole / Q000494:pharmacology*; D008862:Microsomes, Liver / Q000378:metabolism; D051381:Rats; D017208:Rats, Wistar; D013237:Stereoisomerism; D013454:Sulfoxides / Q000378:metabolism*
D000871:Anthelmintics; D013956:Antithyroid Agents; D013454:Sulfoxides; D008713:Methimazole; D015766:Albendazole