Toltrazuril is an antiprotozoal agent that acts upon Coccidia parasites in animals, fish, and man. Its primary metabolites include toltrazuril sulfoxide and toltrazuril sulfone. Toltrazuril can also be used as an analytical standard in food and environmental testing. The compound is soluble in DMSO.
| Application | Toltrazuril can be used as an analytical standard in food and environmental testing. |
| Mechanism of Action | Toltrazuril induces changes in the coccidia such that the intracellular stages (schizonts, gamonts) were destroyed. Anatomical changes include swelling of the endoplasmic reticulum and Golgi, and abnormalities in nuclear division leading to a reduction in respiratory enzymes. |
| Eukaryotic Cell Culture Applications | Toltrazuril was investigated in Neospora caninum using a molecular assay to distinguish between live and dead parasites. Infected cells were treated with 30 ug/ml toltrazuril for 2-20 days. NcGRA2-RT-real time PCR showed that a 10-day treatment was sufficient. This assay could be widely used to study the affect of novel compounds in the bovine host (Strohbusch et al, 2008). Cryptosporidium parvum is a protozoan parasite that is highly infectious in humans and animals, infecting the epithelial cells of the small intestine. Toltrazuril was used in vitro against oocysts to test for anticryptosporidial activity, and effectiveness was dose-dependent, with optimal being 100 ug/ml. A synergistic mixture of Toltrazuril with Monensin had the greatest efficacy (Fathi et al, 2011). |
| References | Fathi M, Sadraei J, and Ghaffarifar F (2011) Effects of two anticoccidial drugs, Monensin, Toltrazuril and the mixture of them on Cryptosporidium parvum in vitro. Jundishapur J. Microbiol. 4(2): 71-74 Martinez-Villalba A, Moyano E, Martins CPB and Galceran MT (2010) Fast liquid chromatography/tandem mass spectrometry (highly selective selected reaction monitoring) for the determination of toltrazuril and its metabolites in food. Anal. Bioanal. Chem. 397(7):2893-2901 Mehlhorn H, Schmahl G and HAberkorn A (1988) Toltrazuril effective against a broad spectrum of protozoan parasites. Parasitol. Res. 75(1):64-66 PMID 3144713 Strohbusch M, Muller N, Hemphill A, Greif G and Gottstein B (2008) NcGA2 as a molecular target to assess the parasiticidal activity of toltrazuril against Neospora caninum. Parasitol. 135(9):1065-1073 |
