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Novel Pharmacological Activity of Artesunate and Artemisinin: Their Potential as Anti-Tubercular Agents

Tuberculosis is a major infectious disease that globally causes the highest human mortality. From this aspect, this study was carried out to evaluate novel pharmacological activities/effects of artesunate and artemisinin causing anti-tubercular activity/effects against Mycobacterium tuberculosis (Mt...

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Autor principal: Choi, Won Hyung
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2017
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5372999/
https://www.ncbi.nlm.nih.gov/pubmed/28287416
http://dx.doi.org/10.3390/jcm6030030
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author Choi, Won Hyung
author_facet Choi, Won Hyung
author_sort Choi, Won Hyung
collection PubMed
description Tuberculosis is a major infectious disease that globally causes the highest human mortality. From this aspect, this study was carried out to evaluate novel pharmacological activities/effects of artesunate and artemisinin causing anti-tubercular activity/effects against Mycobacterium tuberculosis (Mtb). The anti-Mtb activities/effects of artesunate and artemisinin were evaluated using different anti-Mtb indicator assays, such as the resazurin microtiter assay, the Mycobacteria Growth Indicator Tube (MGIT) 960 system assay, and the Ogawa slant medium assay, as well as in vivo tests. Artesunate showed selective anti-Mtb effects by strongly inhibiting the growth of Mtb compared to artemisinin, and consistently induced anti-Mtb activity/effects by effectively inhibiting Mtb in the MGIT 960 system and in Ogawa slant medium for 21 days with a single dose; its minimum inhibitory concentration was 300 µg/mL in in vitro testing. Furthermore, artesunate demonstrated an anti-tubercular effect/action with a daily dose of 3.5 mg/kg in an in vivo test for four weeks, which did not indicate or induce toxicity and side effects. These results demonstrate that artesunate effectively inhibits the growth and/or proliferation of Mtb through novel pharmacological activities/actions, as well as induces anti-Mtb activity. This study shows its potential as a potent candidate agent for developing new anti-tuberculosis drugs of an effective/safe next generation, and suggests novel insights into its effective use by repurposing existing drugs through new pharmacological activity/effects as one of the substantive alternatives for inhibiting tuberculosis.
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spelling pubmed-53729992017-04-05 Novel Pharmacological Activity of Artesunate and Artemisinin: Their Potential as Anti-Tubercular Agents Choi, Won Hyung J Clin Med Article Tuberculosis is a major infectious disease that globally causes the highest human mortality. From this aspect, this study was carried out to evaluate novel pharmacological activities/effects of artesunate and artemisinin causing anti-tubercular activity/effects against Mycobacterium tuberculosis (Mtb). The anti-Mtb activities/effects of artesunate and artemisinin were evaluated using different anti-Mtb indicator assays, such as the resazurin microtiter assay, the Mycobacteria Growth Indicator Tube (MGIT) 960 system assay, and the Ogawa slant medium assay, as well as in vivo tests. Artesunate showed selective anti-Mtb effects by strongly inhibiting the growth of Mtb compared to artemisinin, and consistently induced anti-Mtb activity/effects by effectively inhibiting Mtb in the MGIT 960 system and in Ogawa slant medium for 21 days with a single dose; its minimum inhibitory concentration was 300 µg/mL in in vitro testing. Furthermore, artesunate demonstrated an anti-tubercular effect/action with a daily dose of 3.5 mg/kg in an in vivo test for four weeks, which did not indicate or induce toxicity and side effects. These results demonstrate that artesunate effectively inhibits the growth and/or proliferation of Mtb through novel pharmacological activities/actions, as well as induces anti-Mtb activity. This study shows its potential as a potent candidate agent for developing new anti-tuberculosis drugs of an effective/safe next generation, and suggests novel insights into its effective use by repurposing existing drugs through new pharmacological activity/effects as one of the substantive alternatives for inhibiting tuberculosis. MDPI 2017-03-10 /pmc/articles/PMC5372999/ /pubmed/28287416 http://dx.doi.org/10.3390/jcm6030030 Text en © 2017 by the author. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Choi, Won Hyung
Novel Pharmacological Activity of Artesunate and Artemisinin: Their Potential as Anti-Tubercular Agents
title Novel Pharmacological Activity of Artesunate and Artemisinin: Their Potential as Anti-Tubercular Agents
title_full Novel Pharmacological Activity of Artesunate and Artemisinin: Their Potential as Anti-Tubercular Agents
title_fullStr Novel Pharmacological Activity of Artesunate and Artemisinin: Their Potential as Anti-Tubercular Agents
title_full_unstemmed Novel Pharmacological Activity of Artesunate and Artemisinin: Their Potential as Anti-Tubercular Agents
title_short Novel Pharmacological Activity of Artesunate and Artemisinin: Their Potential as Anti-Tubercular Agents
title_sort novel pharmacological activity of artesunate and artemisinin: their potential as anti-tubercular agents
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5372999/
https://www.ncbi.nlm.nih.gov/pubmed/28287416
http://dx.doi.org/10.3390/jcm6030030
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