The effect of triclabendazole (“Fasinex”) on protein synthesis by the liver fluke, Fasciola hepatica

• Published in: International journal for parasitology 1995-04, Vol.25 (4), p.421-429
• Main Authors: Stitt, A.W., Fairweather, I., Mackender, R.O.
• Format: Article
• Language: English
• Subjects: actinomycin D; Animals; Antibiotics. Antiinfectious agents. Antiparasitic agents; Antiparasitic agents; Benzimidazoles - pharmacology; Biological and medical sciences; cycloheximide; cytochalasin B; Cytochalasin B - pharmacology; Digenea; Dioxolanes - pharmacology; Fasciola hepatica; Fasciola hepatica - drug effects; Fasciola hepatica - metabolism; fluke; Leucine - pharmacokinetics; liquid scintillation counting; Male; Medical sciences; Pharmacology. Drug treatments; protein synthesis; Protein Synthesis Inhibitors - pharmacology; Rats; Rats, Wistar; sulphoxide metabolite of triclabendazole (TCBZ-SX); Trematoda; Triclabendazole; tubulozole-C
• ISSN: 0020-7519; 1879-0135
• DOI: 10.1016/0020-7519(94)00140-J

The effect of the active sulphoxide metabolite of the anthelmintic triclabendazole (TCBZ-SX, 15–50 μg ml −1) on the incorporation of radioactively labelled [ 14C] leucine by adult Fasciola hepatica tissue slices was measured by liquid scintillation counting. In addition, the ability of the microfilament-disrupting drug, cytochalasin B, and the microtubule-disrupting drug, tubulozole-C, to inhibit protein synthesis, was assessed by similar methods and compared with TCBZ-SX. The established protein synthesis inhibitors, cycloheximide and actinomycin D were used as positive controls. All the drugs showed a significant inhibition of protein synthesis, albeit to different extents; however, TCBZ-SX was the most potent, with no significant difference between its effect and that of cycloheximide or actinomycin D. Moreover, the concentration of TCBZ-SX, above 15 μg ml −1, had little further influence on incorporation of [ 14C] leucine. This investigation demonstrates the inhibitory effect of TCBZ-SX, cytochalasin B and tubulozole-C on protein synthesis in F. hepatica and confirms the qualitative observations made in several previous ultrastructural studies