We found a match
Your institution may have rights to this item. Sign in to continue.
- Title
Repurposing Auranofin and Evaluation of a New Gold(I) Compound for the Search of Treatment of Human and Cattle Parasitic Diseases: From Protozoa to Helminth Infections.
- Authors
Feng, Liwen; Pomel, Sébastien; Latre de Late, Perle; Taravaud, Alexandre; Loiseau, Philippe M.; Maes, Louis; Cho-Ngwa, Fidelis; Bulman, Christina A.; Fischer, Chelsea; Sakanari, Judy A.; Ziniel, Peter D.; Williams, David L.; Davioud-Charvet, Elisabeth; Schmidt, Thomas J.
- Abstract
Neglected parasitic diseases remain a major public health issue worldwide, especially in tropical and subtropical areas. Human parasite diversity is very large, ranging from protozoa to worms. In most cases, more effective and new drugs are urgently needed. Previous studies indicated that the gold(I) drug auranofin (Ridaura®) is effective against several parasites. Among new gold(I) complexes, the phosphole-containing gold(I) complex {1-phenyl-2,5-di(2-pyridyl)phosphole}AuCl (abbreviated as GoPI) is an irreversible inhibitor of both purified human glutathione and thioredoxin reductases. GoPI-sugar is a novel 1-thio-β-d-glucopyranose 2,3,4,6-tetraacetato-S-derivative that is a chimera of the structures of GoPI and auranofin, designed to improve stability and bioavailability of GoPI. These metal-ligand complexes are of particular interest because of their combined abilities to irreversibly target the essential dithiol/selenol catalytic pair of selenium-dependent thioredoxin reductase activity, and to kill cells from breast and brain tumors. In this work, screening of various parasites—protozoans, trematodes, and nematodes—was undertaken to determine the in vitro killing activity of GoPI-sugar compared to auranofin. GoPI-sugar was found to efficiently kill intramacrophagic Leishmania donovani amastigotes and adult filarial and trematode worms.
- Subjects
CATTLE diseases; PARASITIC diseases; HELMINTHS; HELMINTHIASIS; AURANOFIN; TREMATODA; PROTOZOA
- Publication
Molecules, 2020, Vol 25, Issue 21, p5075
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules25215075