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Home / Equine Research Bank / Vet Parasitol / In vitro efficacy of nitro- and halogeno-thiazolide/thiadiaz...
Veterinary parasitology2009; 162(3-4); 230-235; doi: 10.1016/j.vetpar.2009.03.022

In vitro efficacy of nitro- and halogeno-thiazolide/thiadiazolide derivatives against Sarcocystis neurona.

Abstract: Sarcocystis neurona is an obligate intracellular parasite that causes equine protozoal myeloencephalitis (EPM). The aim of this work was to document inhibitory activities of nitazoxanide (NTZ, [2-acetolyloxy-N-(5-nitro 2-thiazolyl) benzamide]) and new thiazolides/thiadiazolides on S. neurona in vitro development, and investigate their structure-activity relationships. S. neurona was grown in bovine turbinate cell cultures. At concentrations varying from 1.0 to 5.0mg/L, nitazoxanide and 21 of 32 second generation thiazolide/thiadiazolide agents exerted a > or =95% maximum inhibition on S. neurona development. Most active agents were either NO(2) or halogen substituted in position 5 of their thiazole moiety. In contrast, other 5-substitutions such as hydrogen, methyl, SO(2)CH(3), and CH(3) negatively impacted activity. Compared with derivatives with an acetylated benzene moiety, deacetylated compounds which most probably represent primary metabolites exhibited similar inhibitory activities. Present data provide the first evidence of in vitro inhibitory activities of nitazoxanide and new thiazolides/thiadiazolides on S. neurona development. Active halogeno-thiazolide/thiadiazolides may provide a valuable nitro-free alternative to nitazoxanide for EPM treatment depending on further evaluation of their in vivo activities.
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Publication Date: 2009-03-25 PubMed ID: 19369006DOI: 10.1016/j.vetpar.2009.03.022Google Scholar: Lookup
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  • Journal Article
  • Research Support
  • Non-U.S. Gov't

Summary

This research summary has been generated with artificial intelligence and may contain errors and omissions. Refer to the original study to confirm details provided. Submit correction.

The research article explores the potential impact of nitazoxanide and new thiazolides/thiadiazolides derivatives on the development of Sarcocystis neurona, a parasite that causes equine protozoal myeloencephalitis, in a laboratory setting. The study findings suggest that these compounds exert significant inhibitory effects on this parasite’s development and may serve as an effective alternative to current treatment options.

Objective and Methodology

  • The primary aim of the study was to investigate the influence of nitazoxanide and new thiazolides/thiadiazolides derivatives on the development of Sarcocystis neurona, a harmful parasite affecting horses.
  • The research employed an in vitro approach where the parasite was grown in a bovine turbinate cell culture.
  • The concentrations of nitazoxanide and the new thiazolide/thiadiazolide agents ranged from 1.0 to 5.0mg/L.

Results and Findings

  • It was observed that nitazoxanide and 21 of 32 second-generation thiazolide/thiadiazolide agents resulted in a 95% or higher maximum inhibition on S. neurona development.
  • The most effective agents were those that had been substituted with either NO(2) or halogen in position 5 of their thiazole moiety.
  • On the other hand, other 5-substitutions such as hydrogen, methyl, SO(2)CH(3), and CH(3) negatively affected the activity of these agents.
  • There was little to no difference in inhibitory activities between derivatives with an acetylated benzene moiety and deacetylated compounds, which likely represent primary metabolites.

Implications and Conclusion

  • The observed in vitro inhibitory activities of nitazoxanide and new thiazolides/thiadiazolides on S. neurona development provides novel insights into potential treatments for equine protozoal myeloencephalitis.
  • The halogeno-thiazolide/thiadiazolides, in particular, may offer a valuable nitro-free alternative to nitazoxanide for the treatment of this condition, subject to further investigation of their in vivo activities.

Cite This Article

APA
Gargala G, Le Goff L, Ballet JJ, Favennec L, Stachulski AV, Rossignol JF. (2009). In vitro efficacy of nitro- and halogeno-thiazolide/thiadiazolide derivatives against Sarcocystis neurona. Vet Parasitol, 162(3-4), 230-235. https://doi.org/10.1016/j.vetpar.2009.03.022

Publication

Veterinary parasitology
ISSN: 0304-4017
NlmUniqueID: 7602745
Country: Netherlands
Language: English
Volume: 162
Issue: 3-4
Pages: 230-235

Researcher Affiliations

Gargala, G
  • Parasitology Department, University of Rouen, France. gilles.gargala@univ-rouen.fr
Le Goff, L
    Ballet, J J
      Favennec, L
        Stachulski, A V
          Rossignol, J F

            MeSH Terms

            • Animals
            • Cattle
            • Cell Line
            • Coccidiostats / chemistry
            • Coccidiostats / pharmacology
            • Sarcocystis / drug effects
            • Structure-Activity Relationship
            • Thiadiazines / chemistry
            • Thiadiazines / pharmacology
            • Thiazoles / chemistry
            • Thiazoles / pharmacology

            Citations

            This article has been cited 6 times.
            1. Bowden GD, Land KM, O'Connor RM, Fritz HM. High-throughput screen of drug repurposing library identifies inhibitors of Sarcocystis neurona growth.. Int J Parasitol Drugs Drug Resist 2018 Apr;8(1):137-144.
              doi: 10.1016/j.ijpddr.2018.02.002pubmed: 29547840google scholar: lookup
            2. Dubey JP, Howe DK, Furr M, Saville WJ, Marsh AE, Reed SM, Grigg ME. An update on Sarcocystis neurona infections in animals and equine protozoal myeloencephalitis (EPM).. Vet Parasitol 2015 Apr 15;209(1-2):1-42.
              doi: 10.1016/j.vetpar.2015.01.026pubmed: 25737052google scholar: lookup
            3. Gargala G, François A, Favennec L, Rossignol JF. Activity of halogeno-thiazolides against Cryptosporidium parvum in experimentally infected immunosuppressed gerbils (Meriones unguiculatus).. Antimicrob Agents Chemother 2013 Jun;57(6):2821-3.
              doi: 10.1128/AAC.01538-12pubmed: 23478972google scholar: lookup
            4. Stachulski AV, Pidathala C, Row EC, Sharma R, Berry NG, Iqbal M, Bentley J, Allman SA, Edwards G, Helm A, Hellier J, Korba BE, Semple JE, Rossignol JF. Thiazolides as novel antiviral agents. 1. Inhibition of hepatitis B virus replication.. J Med Chem 2011 Jun 23;54(12):4119-32.
              doi: 10.1021/jm200153ppubmed: 21553812google scholar: lookup
            5. Ashton LV, Callan RL, Rao S, Landolt GA. In Vitro Susceptibility of Canine Influenza A (H3N8) Virus to Nitazoxanide and Tizoxanide.. Vet Med Int 2010 Aug 12;2010.
              doi: 10.4061/2010/891010pubmed: 20847948google scholar: lookup
            6. Gargala G, Le Goff L, Ballet JJ, Favennec L, Stachulski AV, Rossignol JF. Evaluation of new thiazolide/thiadiazolide derivatives reveals nitro group-independent efficacy against in vitro development of Cryptosporidium parvum.. Antimicrob Agents Chemother 2010 Mar;54(3):1315-8.
              doi: 10.1128/AAC.00614-09pubmed: 20047919google scholar: lookup
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