Ex vivo anthelmintic activity of albendazole-sulphoxide enantiomers
F Bolás-Fernández1, S Rama-Iñiguez, J J Torrado
1Departamento de Parasitología, Facultad de Farmacia, Universidad Complutense, 28040 Madrid, Spain. francisb@farm.ucm.es
Abstract:
The antiparasitic activity of racemic albendazole-sulphoxide (Ricobendazole = racRBZ) and its (+) and (-) enantiomers was tested in an ex vivo murine model for Trichinella spiralis infection. Larvae were isolated from the muscle of infected mice and exposed to concentrations between 0.01 and 1 microg/ml of the racemic mixture or to each of its enantiomers. The activity of each compound was then assayed by measuring the ability of the treated larvae to infect naive mice (larval viability). At a concentration of 0.5 microg/ml, all 3 compounds were highly effective in reducing the viability of the larvae, achieving reductions of 91.26% (racRBZ), 96.7% (+), and 89.2% (-), when compared with untreated controls. At lower concentrations (0.1 microg/ml), only treatment with (+)RBZ rendered a significant reduction in larval viability in comparison with controls (84.3%; P < 0.01), whereas at 0.01 microg/ml, none of the compounds altered larval viability (P > 0.05).
Related Concept Videos
Anthelminthic Agents
Properties of Enantiomers and Optical Activity
Antiprotozoal Agents
¹H NMR Chemical Shift Equivalence: Enantiotopic and Diastereotopic Protons
In chiral compounds such as 2-butanol, replacing the methylene hydrogens at C3 produces a pair of...
Racemic Mixtures and the Resolution of Enantiomers
Direct-Acting Cholinergic Agonists: Pharmacokinetics

