ArticleAntimicrobial agents and chemotherapy2013
A reprofiled drug, auranofin, is effective against metronidazole-resistant Giardia lamblia.
Article in Antimicrobial agents and chemotherapy, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 78 papers.
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Who cites it
78 citing papers in PubMed, 142 citations in OpenAlex.
- Repurposing Auranofin for Oncology and Beyond: A Brief Overview of Clinical Trials as Mono- and Combination Therapy.Pharmaceuticals (Basel, Switzerland) · 2025Review
- Investigation of In Vitro and In Vivo Anti-leishmanial Activity of Auranofin on Leishmania Infantum.Acta parasitologica · 2025Article
- Searching for New Gold(I)-Based Complexes as Anticancer and/or Antiviral Agents.Molecules (Basel, Switzerland) · 2025Review
- Functional utility of gold complexes with phosphorus donor ligands in biological systems.Coordination chemistry reviews · 2025Article
- The Many Lives of Auranofin: How an Old Anti-Rheumatic Agent May Become a Promising Antimicrobial Drug.Antibiotics (Basel, Switzerland) · 2024Review
- Gold(I) ion and the phosphine ligand are necessary for the anti-Microbiology spectrum · 2024Article
- Nanoscale dihydroartemisinin@zeolitic imidazolate frameworks for enhanced antigiardial activity and mechanism analysis.Frontiers in veterinary science · 2024Article
- Repurposing Terfenadine as a Novel Antigiardial Compound.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Inhibition of selenoprotein synthesis is not the mechanism by which auranofin inhibits growth of Clostridioides difficile.Scientific reports · 2023Article
- Prdx5 in the Regulation of Tuberous Sclerosis Complex Mutation-Induced Signaling Mechanisms.Cells · 2023Article
- Structure ofInternational journal of molecular sciences · 2023Article
- The protein disulfide isomerase inhibitor 3-methyltoxoflavin inhibits Chikungunya virus.Bioorganic & medicinal chemistry · 2023Article
- Gold complex compounds that inhibit drug-resistantFrontiers in antibiotics · 2023Article
- A Subset Screen of the Compounds Australia Scaffold Library Identifies 7-Acylaminodibenzoxazepinones as Potent and Selective Hits for Anti-Biomedicines · 2022Article
- A Broad Spectrum Antiparasitic Activity of Organotin (IV) Derivatives and Its Untargeted Proteomic Profiling UsingPathogens (Basel, Switzerland) · 2022Article
- Application of Proteomics to the Study of the Therapeutics and Pathogenicity ofDiagnostics (Basel, Switzerland) · 2022Review
- Antigiardial Activity of Novel Guanidine Compounds.ChemMedChem · 2022Article
- Antibiofilm agents with therapeutic potential against enteroaggregative Escherichia coli.PLoS neglected tropical diseases · 2022Article
- Non-Antibiotic Drug Repositioning as an Alternative Antimicrobial Approach.Antibiotics (Basel, Switzerland) · 2022Review
- An Overview of Mucosa-Associated Protozoa: Challenges in Chemotherapy and Future Perspectives.Frontiers in cellular and infection microbiology · 2022Review
18 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
9 authors at 4 institutions in 2 countries.
Funding
Abstract
Giardiasis is one of the most common causes of diarrheal disease worldwide. Treatment is primarily with 5-nitro antimicrobials, particularly metronidazole. Resistance to metronidazole has been described, and treatment failures can occur in up to 20% of cases, making development of alternative antigiardials an important goal. To this end, we have screened a chemical library of 746 approved human drugs and 164 additional bioactive compounds for activity against Giardia lamblia. We identified 56 compounds that caused significant inhibition of G. lamblia growth and attachment. Of these, 15 were previously reported to have antigiardial activity, 20 were bioactive but not approved for human use, and 21 were drugs approved for human use for other indications. One notable compound of the last group was the antirheumatic drug auranofin. Further testing revealed that auranofin was active in the low (4 to 6)-micromolar range against a range of divergent G. lamblia isolates representing both human-pathogenic assemblages A and B. Most importantly, auranofin was active against multiple metronidazole-resistant strains. Mechanistically, auranofin blocked the activity of giardial thioredoxin oxidoreductase, a critical enzyme involved in maintaining normal protein function and combating oxidative damage, suggesting that this inhibition contributes to the antigiardial activity. Furthermore, auranofin was efficacious in vivo, as it eradicated infection with different G. lamblia isolates in different rodent models. These results indicate that the approved human drug auranofin could be developed as a novel agent in the armamentarium of antigiardial drugs, particularly against metronidazole-resistant strains.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.