Cytotoxicity decreasing effect and antimycobacterial activity of chitosan conjugated with antituberculotic drugs

Eva Vavříková, Jana Mandíková, František Trejtnar, Kata Horváti, Szilvia Bösze, Jiřina Stolaříková, Jarmila Vinšová

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Abstract

Water-soluble chitosan conjugates were prepared by connection with isoniazid, pyrazinamide and ethionamide across the O-carboxymethyl and N-succinyl bridge followed by phosphorylation. Their structures were characterized by FTIR and 1H NMR spectroscopy. Degree of drug substitution and molecular weight of prepared compounds have been investigated. Antimycobacterial activity was determined against Mycobacterium tuberculosis and three non-tuberculosis strains. Chitosan derivatives showed significant MIC 125 μg/mL against all tested strains which can be explained by contribution of the presence of antituberculotic drugs and original structure of chitosan. Cytotoxicity of prepared compounds was evaluated in human liver cell line Hep G2 and human peripheral blood mononuclear cells (PBMC). Toxicity of antituberculotic drugs on Hep G2 cells were compensated by connection with chitosan and tested compounds have not exhibited significant cytotoxic effect on PBMC cells. Chitosan conjugates with antituberculotic drugs could be potentially effective in the non-toxic chemotherapy of tuberculosis.

Original languageEnglish
Pages (from-to)1901-1907
Number of pages7
JournalCarbohydrate Polymers
Volume83
Issue number4
DOIs
Publication statusPublished - Feb 1 2011

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Keywords

  • Chitosan
  • Cytotoxicity
  • Ethionamide
  • In vitro antimycobacterial activity
  • Isoniazid
  • Pyrazinamide

ASJC Scopus subject areas

  • Organic Chemistry
  • Polymers and Plastics
  • Materials Chemistry

Cite this

Vavříková, E., Mandíková, J., Trejtnar, F., Horváti, K., Bösze, S., Stolaříková, J., & Vinšová, J. (2011). Cytotoxicity decreasing effect and antimycobacterial activity of chitosan conjugated with antituberculotic drugs. Carbohydrate Polymers, 83(4), 1901-1907. https://doi.org/10.1016/j.carbpol.2010.10.053