Naturally occurring cardenolides affecting Schistosoma mansoni

Keiser, Jennifer and Koch, Vanessa and Deckers, Anke and Cheung, H. T. Andrew and Jung, Nicole and Bräse, Stefan. (2020) Naturally occurring cardenolides affecting Schistosoma mansoni. ACS infectious diseases, 6 (7). pp. 1922-1927.

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Official URL: https://edoc.unibas.ch/77843/

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Schistosomiasis is a neglected tropical disease of considerable public health burden. We recently discovered a micromolar activity of several cardenolides against newly transformed schistosomula (NTS) of the parasitic flatworm; Schistosoma mansoni; in a small compound screen including different substance classes of both natural products as well as synthetic molecules. In further experiments, a focused library of naturally occurring and synthetic steroids was explored against NTS and adult; S. mansoni; , revealing seven cardenolides with comparable activities as known anthelminthics such as praziquantel. Of these, gomphoside monoacetate and uscharin showed suitable therapeutic indices. In a first; in vivo; study, at a dose of 10 mg/kg, only minor activity in mice harboring a chronic; S. mansoni; infection could be shown, which will be further investigated by structure-activity relationship studies as well as pharmacodynamic and pharmacokinetic approaches.
Faculties and Departments:09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH)
09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH) > Department of Medical Parasitology and Infection Biology (MPI) > Helminth Drug Development (Keiser)
UniBasel Contributors:Keiser, Jennifer
Item Type:Article, refereed
Article Subtype:Research Article
Publisher:ACS Publications
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:28 Jul 2020 07:52
Deposited On:28 Jul 2020 07:52

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