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Antimicrob. Agents Chemother., Dec 1997, 2729-2732, Vol 41, No. 12
Copyright © 1997 by the American Society for Microbiology. All rights reserved.

In vitro susceptibilities of the AIDS-associated microsporidian Encephalitozoon intestinalis to albendazole, its sulfoxide metabolite, and 12 additional benzimidazole derivatives

SK Katiyar and TD Edlind
MCP-Hahnemann School of Medicine, Allegheny University of the Health Sciences, Philadelphia, Pennsylvania 19129, USA. katiyars@auhs.edu

Recent reports have described the successful treatment of Encephalitozoon intestinalis infection in AIDS patients with albendazole. However, this compound is rapidly metabolized in vivo to albendazole sulfoxide, and furthermore it is only 1 of about 15 commercially developed benzimidazole derivatives. To compare the activities of albendazole, albendazole sulfoxide, and other benzimidazoles, an in vitro system involving infection of green monkey kidney cell (E6) monolayers with E. intestinalis spores was developed. After 14 days, the effects of benzimidazoles on spore production were determined. Ten of fourteen derivatives tested, including albendazole, were inhibitory at concentrations of 1 to 10 ng/ml. Derivatives modified at the 1 or 2 position were less active. Albendazole sulfoxide was 1.7-fold more inhibitory than albendazole but significantly less toxic to E6 cells, a finding that explains the clinical efficacy of this compound. Potential alternatives to albendazole are discussed. No albendazole-resistant E. intestinalis mutants were obtained following in vitro selection.


This article has been cited by other articles:

  • Menotti, J., Santillana-Hayat, M., Cassinat, B., Sarfati, C., Derouin, F., Molina, J.-M. (2005). Inhibitory Activity of Human Immunodeficiency Virus Aspartyl Protease Inhibitors against Encephalitozoon intestinalis Evaluated by Cell Culture-Quantitative PCR Assay. Antimicrob. Agents Chemother. 49: 2362-2366 [Abstract] [Full Text]  
  • Ridoux, O., Drancourt, M. (1998). In Vitro Susceptibilities of the Microsporidia Encephalitozoon cuniculi, Encephalitozoon hellem, and Encephalitozoon intestinalis to Albendazole and Its Sulfoxide and Sulfone Metabolites. Antimicrob. Agents Chemother. 42: 3301-3303 [Abstract] [Full Text]  


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