Trypanocidal and cell swelling activity of 20-deoxysalinomycin

Steverding, Dietmar, Strand, Daniel and Huczyński, Adam (2022) Trypanocidal and cell swelling activity of 20-deoxysalinomycin. Experimental Parasitology, 243. ISSN 0014-4894

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The naturally occurring polyether ionophore salinomycin was previously found to display promising anti-proliferative activity against bloodstream forms of Trypanosoma brucei. Here, we report the evaluation of 20-deoxysalinomycin, a naturally occurring homolog to salinomycin, for trypanocidal and cell swelling activity. The concentration of 20-deoxysalinomycin required to reduce the growth rate of bloodstream-form trypanosomes by 50% was determined to be 0.12 μM and found to be 8 times more trypanocidal than that of salinomycin. Moreover, 20-deoxysalinomycin and salinomycin displayed similar cytotoxic activity against human HL-60 cells. Measured as the ratio of cytotoxic to trypanocidal activity, 20-deoxysalinomycin thus exhibits a four-fold higher selectivity compared to salinomycin. The stronger trypanocidal activity of 20-deoxysalinomycin is attributed to an enhanced ability to induce cell swelling in trypanosomes. The findings support 20-deoxysalinomycin as a useful lead in the rational development of new and improved anti-trypanosomal drugs.

Item Type: Article
Additional Information: Acknowledgements: Daniel Strand thanks The Swedish Cancer Foundation, Sweden (CAN 2013/864), The Crafoord Foundation, Sweden (2017/1300), and the Swedish Research Council, Sweden (2018-04113) for funding. Data availability: Data will be made available on request.
Uncontrolled Keywords: 20-deoxysalinomycin,african trypanosomiasis,polyether ionophores,trypanosoma brucei,parasitology,immunology,infectious diseases ,/dk/atira/pure/subjectarea/asjc/2400/2405
Faculty \ School: Faculty of Medicine and Health Sciences > Norwich Medical School
UEA Research Groups: Faculty of Medicine and Health Sciences > Research Groups > Gastroenterology and Gut Biology
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Depositing User: LivePure Connector
Date Deposited: 25 Oct 2022 11:30
Last Modified: 13 Jan 2023 09:30
DOI: 10.1016/j.exppara.2022.108414


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