Enantiospecific antitrypanosomal in vitro activity of eflornithine.
The polyamine synthesis inhibitor eflornithine is a recommended treatment for the neglected tropical disease Gambian human African trypanosomiasis in late stage. This parasitic disease, transmitted by the tsetse fly, is lethal unless treated. Eflornithine is administered by repeated intravenous infu...
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ftdoajarticles:oai:doaj.org/article:c09d0c37b3f74d8f93472961fd18e82d 2023-05-15T15:04:39+02:00 Enantiospecific antitrypanosomal in vitro activity of eflornithine. Mikael Boberg Monica Cal Marcel Kaiser Rasmus Jansson-Löfmark Pascal Mäser Michael Ashton 2021-07-01T00:00:00Z https://doi.org/10.1371/journal.pntd.0009583 https://doaj.org/article/c09d0c37b3f74d8f93472961fd18e82d EN eng Public Library of Science (PLoS) https://doi.org/10.1371/journal.pntd.0009583 https://doaj.org/toc/1935-2727 https://doaj.org/toc/1935-2735 1935-2727 1935-2735 doi:10.1371/journal.pntd.0009583 https://doaj.org/article/c09d0c37b3f74d8f93472961fd18e82d PLoS Neglected Tropical Diseases, Vol 15, Iss 7, p e0009583 (2021) Arctic medicine. Tropical medicine RC955-962 Public aspects of medicine RA1-1270 article 2021 ftdoajarticles https://doi.org/10.1371/journal.pntd.0009583 2022-12-31T11:17:59Z The polyamine synthesis inhibitor eflornithine is a recommended treatment for the neglected tropical disease Gambian human African trypanosomiasis in late stage. This parasitic disease, transmitted by the tsetse fly, is lethal unless treated. Eflornithine is administered by repeated intravenous infusions as a racemic mixture of L-eflornithine and D-eflornithine. The study compared the in vitro antitrypanosomal activity of the two enantiomers with the racemic mixture against three Trypanosoma brucei gambiense strains. Antitrypanosomal in vitro activity at varying drug concentrations was analysed by non-linear mixed effects modelling. For all three strains, L-eflornithine was more potent than D-eflornithine. Estimated 50% inhibitory concentrations of the three strains combined were 9.1 μM (95% confidence interval [8.1; 10]), 5.5 μM [4.5; 6.6], and 50 μM [42; 57] for racemic eflornithine, L-eflornithine and D-eflornithine, respectively. The higher in vitro potency of L-eflornithine warrants further studies to assess its potential for improving the treatment of late-stage Gambian human African trypanosomiasis. Article in Journal/Newspaper Arctic Directory of Open Access Journals: DOAJ Articles Arctic PLOS Neglected Tropical Diseases 15 7 e0009583 |
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Directory of Open Access Journals: DOAJ Articles |
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ftdoajarticles |
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English |
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Arctic medicine. Tropical medicine RC955-962 Public aspects of medicine RA1-1270 |
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Arctic medicine. Tropical medicine RC955-962 Public aspects of medicine RA1-1270 Mikael Boberg Monica Cal Marcel Kaiser Rasmus Jansson-Löfmark Pascal Mäser Michael Ashton Enantiospecific antitrypanosomal in vitro activity of eflornithine. |
topic_facet |
Arctic medicine. Tropical medicine RC955-962 Public aspects of medicine RA1-1270 |
description |
The polyamine synthesis inhibitor eflornithine is a recommended treatment for the neglected tropical disease Gambian human African trypanosomiasis in late stage. This parasitic disease, transmitted by the tsetse fly, is lethal unless treated. Eflornithine is administered by repeated intravenous infusions as a racemic mixture of L-eflornithine and D-eflornithine. The study compared the in vitro antitrypanosomal activity of the two enantiomers with the racemic mixture against three Trypanosoma brucei gambiense strains. Antitrypanosomal in vitro activity at varying drug concentrations was analysed by non-linear mixed effects modelling. For all three strains, L-eflornithine was more potent than D-eflornithine. Estimated 50% inhibitory concentrations of the three strains combined were 9.1 μM (95% confidence interval [8.1; 10]), 5.5 μM [4.5; 6.6], and 50 μM [42; 57] for racemic eflornithine, L-eflornithine and D-eflornithine, respectively. The higher in vitro potency of L-eflornithine warrants further studies to assess its potential for improving the treatment of late-stage Gambian human African trypanosomiasis. |
format |
Article in Journal/Newspaper |
author |
Mikael Boberg Monica Cal Marcel Kaiser Rasmus Jansson-Löfmark Pascal Mäser Michael Ashton |
author_facet |
Mikael Boberg Monica Cal Marcel Kaiser Rasmus Jansson-Löfmark Pascal Mäser Michael Ashton |
author_sort |
Mikael Boberg |
title |
Enantiospecific antitrypanosomal in vitro activity of eflornithine. |
title_short |
Enantiospecific antitrypanosomal in vitro activity of eflornithine. |
title_full |
Enantiospecific antitrypanosomal in vitro activity of eflornithine. |
title_fullStr |
Enantiospecific antitrypanosomal in vitro activity of eflornithine. |
title_full_unstemmed |
Enantiospecific antitrypanosomal in vitro activity of eflornithine. |
title_sort |
enantiospecific antitrypanosomal in vitro activity of eflornithine. |
publisher |
Public Library of Science (PLoS) |
publishDate |
2021 |
url |
https://doi.org/10.1371/journal.pntd.0009583 https://doaj.org/article/c09d0c37b3f74d8f93472961fd18e82d |
geographic |
Arctic |
geographic_facet |
Arctic |
genre |
Arctic |
genre_facet |
Arctic |
op_source |
PLoS Neglected Tropical Diseases, Vol 15, Iss 7, p e0009583 (2021) |
op_relation |
https://doi.org/10.1371/journal.pntd.0009583 https://doaj.org/toc/1935-2727 https://doaj.org/toc/1935-2735 1935-2727 1935-2735 doi:10.1371/journal.pntd.0009583 https://doaj.org/article/c09d0c37b3f74d8f93472961fd18e82d |
op_doi |
https://doi.org/10.1371/journal.pntd.0009583 |
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PLOS Neglected Tropical Diseases |
container_volume |
15 |
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7 |
container_start_page |
e0009583 |
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1766336382883594240 |