Small intestinal sulphoxidation of Albendazole

Article abstract of DOI:10.3109/00498259509061863

The in vitro sulphoxidation of Albendazole (ABZ) by rat intestinal microsomes has been examined. The results revealed intestinal sulphoxidation of ABZ by intestinal microsomes in a NADPH-dependent enzymatic system. The kinetic constants for sulphoxidase activity were V(max) = 46 pmol/min/mg protein and Michaelis constant K(m) = 6.8 μM. The possible effect of inducers (Arochlor 1254 and ABZ pretreatment) and inhibitors (erythromycin, methimazole, carbon monoxide and fenbendazole), was also studied. In rat pretreated with Arochlor 1254, V(max) was 52 pmol/min/mg protein, whereas oral administration of ABZ increased the intestinal sulphoxidation of the drug, V(max) being 103 pmol/min/mg protein. Erythromycin did not change the enzymatic bioconversion of ABZ, but methimazole and carbon monoxide inhibited the enzyme activity by approximately 60 and 30% respectively. Fenbendazole (a structural analogue of ABZ) was a competitive inhibitor of the sulphoxidation process, characterized by a K(i) or 69 μM. These data demonstrate that the intestinal enzymes contributing to the initial sulphoxidation of ABZ may be similar to the hepatic enzymes involved in the biotransformation process by the P450 and FMO systems, a conclusion that needs to be further established.

Full text of DOI:10.3109/00498259509061863

Xenobiotica
the fate of foreign compounds in biological systems
ISSN: 0049-8254 (Print) 1366-5928 (Online) Journal homepage: http://www.tandfonline.com/loi/ixen20
Small intestinal sulphoxidation of Albendazole
C. Villaverde, A. I. Alvarez, P. Redondo, J. Voces, J. L. Del Estal & J. G. Prieto
To cite this article: C. Villaverde, A. I. Alvarez, P. Redondo, J. Voces, J. L. Del Estal & J. G. Prieto
(1995) Small intestinal sulphoxidation of Albendazole, Xenobiotica, 25:5, 433-441
To link to this article: http://dx.doi.org/10.3109/00498259509061863
Published online: 27 Aug 2009.
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Date: 06 November 2015, At: 14:46