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Molecules 2017, 22(11), 1965; doi:10.3390/molecules22111965

Antimalarial Activity of Acetylenic Thiophenes from Echinops hoehnelii Schweinf

Department of Pharmaceutical Chemistry and Pharmacognosy, School of pharmacy, College of Health Sciences, Addis Ababa University, Addis Ababa P.O. Box 9086, Ethiopia
DDepartment of Pharmacognosy, School of Pharmacy, College of Health Sciences, Mekelle University, P.O.Box 1871, Ethiopia
Department of Chemistry, College of Natural and Computational Sciences, Addis Ababa University, Addis Ababa P.O. Box 1176, Ethiopia
Author to whom correspondence should be addressed.
Received: 6 October 2017 / Accepted: 11 November 2017 / Published: 21 November 2017
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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. View Full-Text
Keywords: Echinops hoehnelii Schweinf; acetylenicthiophenes; in vivo antimalarial; acute oral toxicity Echinops hoehnelii Schweinf; acetylenicthiophenes; in vivo antimalarial; acute oral toxicity

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Bitew, H.; Mammo, W.; Hymete, A.; Yeshak, M.Y. Antimalarial Activity of Acetylenic Thiophenes from Echinops hoehnelii Schweinf. Molecules 2017, 22, 1965.

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