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  • Title: Cryptosporidium parvum metalloaminopeptidase inhibitors prevent in vitro excystation.
    Author: Okhuysen PC, Chappell CL, Kettner C, Sterling CR.
    Journal: Antimicrob Agents Chemother; 1996 Dec; 40(12):2781-4. PubMed ID: 9124840.
    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 alpha-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 H-boronorleucine (pinacol) inhibited excystation by 84, 57, and 61%, respectively, compared with solvent-treated control oocysts. Sporozoites remained viable within the oocyst as determined by propidium iodide and fluorescein diacetate dye uptake, suggesting that alpha-aminoboronic acids were not directly lethal to the parasite.
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