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Molecules 2017, 22(4), 597; doi:10.3390/molecules22040597

Anti-Trypanosomatid Elemanolide Sesquiterpene Lactones from Vernonia lasiopus O. Hoffm

1
Institute of Pharmaceutical Biology and Phytochemistry (IPBP), University of Münster, PharmaCampus Corrensstraße 48, D-48149 Münster, Germany
2
Department of Chemistry, Egerton University, P.O. Box 536, Egerton, Nairobi 20115, Kenya
3
Swiss Tropical and Public Health Institute (Swiss TPH), Socinstr. 57, CH-4051 Basel, Switzerland
4
University of Basel, Petersplatz 1, CH-4003 Basel, Switzerland
This work is cordially dedicated to Prof. Dr. Nikolaus H. Fischer, Denton, TX, USA, a pioneer in sesquiterpene lactone research, on the occasion of his 80th birthday.
*
Author to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 29 March 2017 / Revised: 6 April 2017 / Accepted: 6 April 2017 / Published: 8 April 2017
View Full-Text   |   Download PDF [383 KB, uploaded 8 April 2017]   |  

Abstract

Sleeping sickness or human African trypanosomiasis (HAT) is a neglected tropical disease (NTD) threatening millions of peoples’ lives with thousands infected. The disease is endemic in poorly developed regions of sub-Saharan Africa and is caused by the kinetoplastid “protozoan” parasite Trypanosoma brucei. The parasites are transmitted to humans through bites of infected tsetse flies of the genus Glossina. The few available drugs for treatment of this disease are highly toxic, difficult to administer, costly and unavailable to poor rural communities bearing the major burden of this infection. Therefore, the search for new efficacious, safe and affordable drugs is of high importance. Vernonia lasiopus O. Hoffm., an indigenous African plant of the Asteraceae family, has been extensively reported to be used ethno-medicinally as a treatment for malaria. Its crude extracts obtained with solvents of different polarity were screened in vitro for anti-protozoal activity and the dichloromethane extract was found to be particularly active against Trypanosoma brucei rhodesiense (IC50 = 0.17 µg/mL). Bioassay-guided chromatographic fractionation of the dichloromethane extract led to the isolation and identification of six elemanolide type sesquiterpene lactones: 8-desacylvernolide, vernolepin, vernomenin, vernodalol, vernodalin and 11,13-dihydrovernodalin. All these elemanolide sesquiterpene lactones showed in vitro anti-trypanosomal activity. They were also tested for cytotoxicity against mammalian cells (L6 cell line). Vernolepin, the main component in the extract, was also the most potent with an IC50 value of 0.05 µg/mL against T.b. rhodesiense trypomastigotes. This compound showed a selectivity index of 14.5, which makes it an interesting candidate for in vivo tests and determination of its mechanism of action. View Full-Text
Keywords: Vernonia lasiopus; antiprotozoal activity; Trypanosoma brucei rhodesiense; Trypanosoma cruzi; Leishmania donovani; Plasmodium falciparum; elemanolide; sesquiterpene lactones Vernonia lasiopus; antiprotozoal activity; Trypanosoma brucei rhodesiense; Trypanosoma cruzi; Leishmania donovani; Plasmodium falciparum; elemanolide; sesquiterpene lactones
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Kimani, N.M.; Matasyoh, J.C.; Kaiser, M.; Brun, R.; Schmidt, T.J. Anti-Trypanosomatid Elemanolide Sesquiterpene Lactones from Vernonia lasiopus O. Hoffm. Molecules 2017, 22, 597.

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