Binding of serum albumin to the anthelmintic drugs albendazole, triclabendazole and their sulphoxides

Emma Chambers, Elizabeth M. Hoey, Alan Trudgett, Ian Fairweather, David J. Timson

    Research output: Contribution to journalArticlepeer-review

    Abstract

    The binding of drugs to plasma proteins - especially serum albumin - is an important factor in controlling the availability and distribution of these drugs. In this study we have investigated the binding of two drugs commonly used to treat liver fluke infections, albendazole (ABZ) and triclabendazole (TCBZ), and their sulphoxide metabolites to bovine serum albumin (BSA). Both ABZ and TCBZ caused shifts in the mobility of BSA in native gel electrophoresis. No such changes were observed with the sulphoxides under identical conditions. The drugs, and their sulphoxides, caused quenching of the intrinsic tryptophan fluorescence of BSA, indicating association between the drugs and this protein. Quantification of this quenching suggested a 5-10-fold reduction in affinity of the sulphoxides compared to the parent compounds. These results are discussed in respect to previous work on the pharmacodynamics of these fasciolicides and will inform the design of novel anthelmintics.

    Original languageEnglish
    Pages (from-to)172-175
    Number of pages4
    JournalVeterinary Parasitology
    Volume171
    Issue number1-2
    DOIs
    Publication statusPublished - 1 Jul 2010

    Keywords

    • ABZ
    • Bovine serum albumin
    • Drug binding
    • Fasciola hepatica.
    • Liver fluke
    • TCBZ

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