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Isolation of a Novel Flavanonol and an Alkylresorcinol with Highly Potent Anti-Trypanosomal Activity from Libyan Propolis

1
Strathclyde Institute of Pharmacy and Biomedical Science, University of Strathclyde, 161 Cathedral Street, Glasgow G4 0RE, UK
2
Institute of Infection, Immunity and Inflammation, College of Medical, Veterinary and Life Sciences, University of Glasgow, Glasgow G12 8TA, UK
3
Department of Chemistry, University of Agriculture, Makurdi PMB 2373, Nigeria
4
General Directorate of Medical Services, Ministry of Interior, Riyadh 13321, Saudi Arabia
5
BeeVital, Whitby, North Yorkshire YO22 5JR, UK
*
Authors to whom correspondence should be addressed.
Molecules 2019, 24(6), 1041; https://doi.org/10.3390/molecules24061041
Received: 28 February 2019 / Revised: 11 March 2019 / Accepted: 13 March 2019 / Published: 15 March 2019
(This article belongs to the Section Natural Products Chemistry)
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Abstract

Twelve propolis samples from different parts of Libya were investigated for their phytochemical constituents. Ethanol extracts of the samples and some purified compounds were tested against Trypanosoma brucei, Plasmodium falciparum and against two helminth species, Trichinella spiralis and Caenorhabditis elegans, showing various degrees of activity. Fourteen compounds were isolated from the propolis samples, including a novel compound Taxifolin-3-acetyl-4′-methyl ether (4), a flavanonol derivative. The crude extracts showed moderate activity against T. spiralis and C. elegans, while the purified compounds had low activity against P. falciparum. Anti-trypanosomal activity (EC50 = 0.7 µg/mL) was exhibited by a fraction containing a cardol identified as bilobol (10) and this fraction had no effect on Human Foreskin Fibroblasts (HFF), even at 2.0 mg/mL, thus demonstrating excellent selectivity. A metabolomics study was used to explore the mechanism of action of the fraction and it revealed significant disturbances in trypanosomal phospholipid metabolism, especially the formation of choline phospholipids. We conclude that a potent and highly selective new trypanocide may be present in the fraction. View Full-Text
Keywords: propolis; Trypanosoma brucei; anthelminthic activity; metabolomics; alkylresorcinol; bilobol propolis; Trypanosoma brucei; anthelminthic activity; metabolomics; alkylresorcinol; bilobol
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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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Siheri, W.; Ebiloma, G.U.; Igoli, J.O.; Gray, A.I.; Biddau, M.; Akrachalanont, P.; Alenezi, S.; Alwashih, M.A.; Edrada-Ebel, R.; Muller, S.; Lawrence, C.E.; Fearnley, J.; Watson, D.G.; De Koning, H.P. Isolation of a Novel Flavanonol and an Alkylresorcinol with Highly Potent Anti-Trypanosomal Activity from Libyan Propolis. Molecules 2019, 24, 1041.

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