Characterization of the endogenous DAF-12 ligand and its use as an anthelmintic agent in Strongyloides stercoralis

Elife. 2021 Dec 7:10:e73535. doi: 10.7554/eLife.73535.

Abstract

A prevalent feature of Strongyloides stercoralis is a life-long and potentially lethal infection that is due to the nematode parasite's ability to autoinfect and, thereby, self-replicate within its host. Here, we investigated the role of the parasite's nuclear receptor, Ss-DAF-12, in governing infection. We identified Δ7-DA as the endogenous Ss-DAF-12 ligand and elucidated the hormone's biosynthetic pathway. Genetic loss of function of the ligand's rate-limiting enzyme demonstrated that Δ7-DA synthesis is necessary for parasite reproduction, whereas its absence is required for the development of infectious larvae. Availability of the ligand permits Ss-DAF-12 to function as an on/off switch governing autoinfection, making it vulnerable to therapeutic intervention. In a preclinical model of hyperinfection, pharmacologic activation of DAF-12 suppressed autoinfection and markedly reduced lethality. Moreover, when Δ7-DA was administered with ivermectin, the current but limited drug of choice for treating strongyloidiasis, the combinatorial effects of the two drugs resulted in a near cure of the disease.

Keywords: DAF-12; Strongyloides stercoralis; cytochrome P450; gerbil; infectious disease; ivermectin; microbiology; nematode parasitism; nuclear receptor.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anthelmintics / pharmacology*
  • Caenorhabditis elegans / metabolism
  • Caenorhabditis elegans Proteins / chemistry
  • Dogs
  • Gerbillinae
  • Ivermectin / pharmacokinetics*
  • Ligands
  • Male
  • Receptors, Cytoplasmic and Nuclear / agonists*
  • Strongyloides stercoralis / drug effects*
  • Strongyloidiasis / drug therapy
  • Strongyloidiasis / parasitology*

Substances

  • Anthelmintics
  • Caenorhabditis elegans Proteins
  • Ligands
  • Receptors, Cytoplasmic and Nuclear
  • Ivermectin