Cryptosporidium parvum metalloaminopeptidase inhibitors prevent in vitro excystation

Pablo C. Okhuysen, Cynthia L. Chappell, Charles Kettner, Charles R. Sterling

Research output: Contribution to journalArticlepeer-review

28 Scopus citations

Abstract

Cryptosporidium parvum arginine aminopeptidase (RAP) was studied during in vitro excystation. Specific RAP inhibitors were identified by using C. parvum extracts. Amastatin, a series of α-aminoboronic acids, and the chelating agents EDTA and 1.10-phenanthrolene, but not endoproteinase inhibitors, blocked enzymatic activity. RAP inhibitors found to be effective in soluble enzymatic assays were then studied for their effect on in vitro excystation. 1,10-Phenanthrolene, amastatin, and 11-boronorleucine (pinacol) inhibited excystation by 84, 57, and 61%, respectively, compared with solvent-treated control oocysts. Sporozoites remained viable within the oocyst an determined by propidium iodide and fluorescein diacetate dye uptake, suggesting that α-aminoboronic acids were not directly lethal to the parasite.

Original languageEnglish (US)
Pages (from-to)2781-2784
Number of pages4
JournalAntimicrobial Agents and Chemotherapy
Volume40
Issue number12
DOIs
StatePublished - Dec 1996

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)
  • Infectious Diseases

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