ArticleAntimicrobial agents and chemotherapy2011
In vitro efficacy of dicationic compounds and mefloquine enantiomers against Echinococcus multilocularis metacestodes.
Article in Antimicrobial agents and chemotherapy, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers, 1 of them a synthesis that pooled it.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
19 citing papers in PubMed, 1 synthesis or guideline pooled it, 37 citations in OpenAlex.
- Novel amidines and analogues as promising agents against intracellular parasites: a systematic review.Parasitology · 2013Pooled it
- Chemotherapy for the treatment of alveolar echinococcosis: Where are we?Parasite (Paris, France) · 2024Review
- Effect of sunitinib against Echinococcus multilocularis through inhibition of VEGFA-induced angiogenesis.Parasites & vectors · 2023Article
- Laparoscopic hepatectomy for the treatment of hepatic alveolar echinococcosis.Parasite (Paris, France) · 2021Article
- Drug repurposing applied: Activity of the anti-malarial mefloquine against Echinococcus multilocularis.International journal for parasitology. Drugs and drug resistance · 2020Article
- The importance of being parasiticidal… an update on drug development for the treatment of alveolar echinococcosis.Food and waterborne parasitology · 2019Article
- Echinococcosis: Advances in the 21st Century.Clinical microbiology reviews · 2019Review
- Effect of anacardic acid against echinococcosis through inhibition of VEGF-induced angiogenesis.Veterinary research · 2019Article
- Repurposing of an old drug: In vitro and in vivo efficacies of buparvaquone against Echinococcus multilocularis.International journal for parasitology. Drugs and drug resistance · 2018Article
- Activity of mefloquine and mefloquine derivatives against Echinococcus multilocularis.International journal for parasitology. Drugs and drug resistance · 2018Article
- Progress in the pharmacological treatment of human cystic and alveolar echinococcosis: Compounds and therapeutic targets.PLoS neglected tropical diseases · 2018Article
- Screening of the Open Source Malaria Box Reveals an Early Lead Compound for the Treatment of Alveolar Echinococcosis.PLoS neglected tropical diseases · 2016Article
- In vivo and in vitro efficacies of mebendazole, mefloquine and nitazoxanide against cyst echinococcosis.Parasitology research · 2015Article
- Profound activity of the anti-cancer drug bortezomib against Echinococcus multilocularis metacestodes identifies the proteasome as a novel drug target for cestodes.PLoS neglected tropical diseases · 2014Article
- Treatment of echinococcosis: albendazole and mebendazole--what else?Parasite (Paris, France) · 2014Review
- Mefloquine, a new type of compound against schistosomes and other helminthes in experimental studies.Parasitology research · 2013Review
- In vitro and in vivo activities of dicationic diguanidino compounds against Echinococcus multilocularis metacestodes.Antimicrobial agents and chemotherapy · 2013Article
- In vitro efficacy of triclabendazole and clorsulon against the larval stage of Echinococcus multilocularis.Parasitology research · 2013Article
- Quantitative screening for anticestode drugs based on changes in baseline enzyme secretion by Taenia crassiceps.Antimicrobial agents and chemotherapy · 2013Article
Corrections and comments
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Authors and funding
9 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The current chemotherapy of alveolar echinococcosis (AE) is based on benzimidazoles such as albendazole and has been shown to be parasitostatic rather than parasiticidal, requiring lifelong duration. Thus, new and more efficient treatment options are urgently needed. By employing a recently validated assay based on the release of functional phosphoglucose isomerase (PGI) from dying parasites, the activities of 26 dicationic compounds and of the (+)- and (-)-erythro-enantiomers of mefloquine were investigated. Initial screening of compounds was performed at 40 μM, and those compounds exhibiting considerable antiparasitic activities were also assessed at lower concentrations. Of the dicationic drugs, DB1127 (a diguanidino compound) with activities comparable to nitazoxanide was further studied. The activity of DB1127 was dose dependent and led to severe structural alterations, as visualized by electron microscopy. The (+)- and (-)-erythro-enantiomers of mefloquine showed similar dose-dependent effects, although higher concentrations of these compounds than of DB1127 were required for metacestode damage. In conclusion, of the drugs investigated here, the diguanidino compound DB1127 represents the most promising compound for further study in appropriate in vivo models for Echinococcus multilocularis infection.
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