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Antimalarial Activity of Acetylenic Thiophenes from Echinops hoehnelii Schweinf

Malaria is one of the world’s most severe endemic diseases and due to the emergence of resistance to the currently available medicines, the need for new targets and relevant antimalarial drugs remains acute. The crude extract, four solvent fractions and two isolated compounds from the roots of Echin...

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Autores principales: Bitew, Helen, Mammo, Wendimagegn, Hymete, Ariaya, Yeshak, Mariamawit Yonathan
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2017
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6150322/
https://www.ncbi.nlm.nih.gov/pubmed/29160791
http://dx.doi.org/10.3390/molecules22111965
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author Bitew, Helen
Mammo, Wendimagegn
Hymete, Ariaya
Yeshak, Mariamawit Yonathan
author_facet Bitew, Helen
Mammo, Wendimagegn
Hymete, Ariaya
Yeshak, Mariamawit Yonathan
author_sort Bitew, Helen
collection PubMed
description Malaria is one of the world’s most severe endemic diseases and due to the emergence of resistance to the currently available medicines, the need for new targets and relevant antimalarial drugs remains acute. The crude extract, four solvent fractions and two isolated compounds from the roots of Echinops hoehnelii were tested for their antimalarial activity using the standard four-day suppressive method in Plasmodium berghei-infected mice. The 80% methanol extract exhibited suppression of 4.6%, 27.8%, 68.5% and 78.7% at dose of 50, 100, 200 and 400 mg/kg respectively. The dichloromethane fraction displayed chemosuppression of 24.9, 33.5 and 43.0% dose of 100, 200 and 400 mg/kg of body weight. Five acetylenicthiophenes were isolated from the dichloromethane fraction of which 5-(penta-1,3-diynyl)-2-(3,4-dihydroxybut-1-ynyl)-thiophene decreased the level of parasitaemia by 43.2% and 50.2% while 5-(penta-1,3-diynyl)-2-(3-chloro-4-acetoxy-but-1-yn)-thiophene suppressed by 18.8% and 32.7% at 50 and 100 mg/kg, respectively. The study confirmed the traditional claim of the plant to treat malaria and could be used as a new lead for the development of antimalarial drugs.
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spelling pubmed-61503222018-11-13 Antimalarial Activity of Acetylenic Thiophenes from Echinops hoehnelii Schweinf Bitew, Helen Mammo, Wendimagegn Hymete, Ariaya Yeshak, Mariamawit Yonathan Molecules Article Malaria is one of the world’s most severe endemic diseases and due to the emergence of resistance to the currently available medicines, the need for new targets and relevant antimalarial drugs remains acute. The crude extract, four solvent fractions and two isolated compounds from the roots of Echinops hoehnelii were tested for their antimalarial activity using the standard four-day suppressive method in Plasmodium berghei-infected mice. The 80% methanol extract exhibited suppression of 4.6%, 27.8%, 68.5% and 78.7% at dose of 50, 100, 200 and 400 mg/kg respectively. The dichloromethane fraction displayed chemosuppression of 24.9, 33.5 and 43.0% dose of 100, 200 and 400 mg/kg of body weight. Five acetylenicthiophenes were isolated from the dichloromethane fraction of which 5-(penta-1,3-diynyl)-2-(3,4-dihydroxybut-1-ynyl)-thiophene decreased the level of parasitaemia by 43.2% and 50.2% while 5-(penta-1,3-diynyl)-2-(3-chloro-4-acetoxy-but-1-yn)-thiophene suppressed by 18.8% and 32.7% at 50 and 100 mg/kg, respectively. The study confirmed the traditional claim of the plant to treat malaria and could be used as a new lead for the development of antimalarial drugs. MDPI 2017-11-21 /pmc/articles/PMC6150322/ /pubmed/29160791 http://dx.doi.org/10.3390/molecules22111965 Text en © 2017 by the authors. 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
Bitew, Helen
Mammo, Wendimagegn
Hymete, Ariaya
Yeshak, Mariamawit Yonathan
Antimalarial Activity of Acetylenic Thiophenes from Echinops hoehnelii Schweinf
title Antimalarial Activity of Acetylenic Thiophenes from Echinops hoehnelii Schweinf
title_full Antimalarial Activity of Acetylenic Thiophenes from Echinops hoehnelii Schweinf
title_fullStr Antimalarial Activity of Acetylenic Thiophenes from Echinops hoehnelii Schweinf
title_full_unstemmed Antimalarial Activity of Acetylenic Thiophenes from Echinops hoehnelii Schweinf
title_short Antimalarial Activity of Acetylenic Thiophenes from Echinops hoehnelii Schweinf
title_sort antimalarial activity of acetylenic thiophenes from echinops hoehnelii schweinf
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6150322/
https://www.ncbi.nlm.nih.gov/pubmed/29160791
http://dx.doi.org/10.3390/molecules22111965
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