PMID: 9420047Jan 7, 1998Paper

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

Antimicrobial Agents and Chemotherapy
S K Katiyar, T D Edlind

Abstract

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.

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Citations

Oct 20, 2018·Expert Opinion on Therapeutic Targets·Bing Han, Louis M Weiss
Mar 5, 2008·The Journal of Parasitology·Shajahan JohnyDouglas W Whitman
May 20, 2011·Journal of Clinical Microbiology·Oleg DitrichMartin Kvác
May 1, 2008·Expert Opinion on Drug Discovery·Bj FennellA Bell
Feb 16, 2007·The Journal of Eukaryotic Microbiology·Donna E AkiyoshiSaul Tzipori
Apr 25, 2013·Antimicrobial Agents and Chemotherapy·Maria Anete LalloJoão Manoel de Castro
Jul 5, 2021·The Korean Journal of Parasitology·Jong-Yil ChaiSung-Jong Hong
Jul 1, 2021·Clinical Microbiology Reviews·Bing HanLouis M Weiss

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