Activity of compounds from temperate propolis against Trypanosoma brucei and Leishmania mexicana

Alotaibi, A. et al. (2021) Activity of compounds from temperate propolis against Trypanosoma brucei and Leishmania mexicana. Molecules, 26(13), 3912. (doi: 10.3390/molecules26133912) (PMID:34206940) (PMCID:PMC8272135)

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Ethanolic extracts of samples of temperate zone propolis, four from the UK and one from Poland, were tested against three Trypanosoma brucei strains and displayed EC50 values 20 µg/mL. The extracts were fractionated, from which 12 compounds and one two-component mixture were isolated, and characterized by NMR and high-resolution mass spectrometry, as 3-acetoxypinobanksin, tectochrysin, kaempferol, pinocembrin, 4′-methoxykaempferol, galangin, chrysin, apigenin, pinostrobin, cinnamic acid, coumaric acid, cinnamyl ester/coumaric acid benzyl ester (mixture), 4′,7-dimethoxykaempferol, and naringenin 4′,7-dimethyl ether. The isolated compounds were tested against drug-sensitive and drug-resistant strains of T. brucei and Leishmania mexicana, with the highest activities ≤ 15 µM. The most active compounds against T. brucei were naringenin 4′,7 dimethyl ether and 4′methoxy kaempferol with activity of 15–20 µM against the three T. brucei strains. The most active compounds against L. mexicana were 4′,7-dimethoxykaempferol and the coumaric acid ester mixture, with EC50 values of 12.9 ± 3.7 µM and 13.1 ± 1.0 µM. No loss of activity was found with the diamidine- and arsenical-resistant or phenanthridine-resistant T. brucei strains, or the miltefosine-resistant L. mexicana strain; no clear structure activity relationship was observed for the isolated compounds. Temperate propolis yields multiple compounds with anti-kinetoplastid activity.

Item Type:Articles
Keywords:Temperate propolis, flavonoids, isolated compounds, Trypanosoma brucei, Leishmania mexicana.
Glasgow Author(s) Enlighten ID:Alenezi, Mrs Sameah and Ebiloma, Mr Godwin and De Koning, Professor Harry and Natto, Dr Manal and ALFAYEZ, IBRAHIM ABDULLAH M and Igoli, Dr John
Creator Roles:
Ebiloma, G. U.Investigation
Alfayez, I. A.Investigation
Natto, M. J.Investigation
Alenezi, S.Methodology
Igoli, J. O.Formal analysis, Writing – review and editing, Supervision
De Koning, H. P.Conceptualization, Methodology, Formal analysis, Resources, Writing – review and editing, Supervision, Funding acquisition
Authors: Alotaibi, A., Ebiloma, G. U., Williams, R., Alfayez, I. A., Natto, M. J., Alenezi, S., Siheri, W., AlQarni, M., Igoli, J. O., Fearnley, J., De Koning, H. P., and Watson, D. G.
College/School:College of Medical Veterinary and Life Sciences > School of Infection & Immunity
Journal Name:Molecules
ISSN (Online):1420-3049
Published Online:26 June 2021
Copyright Holders:Copyright © 2021 The Authors
First Published:First published in Molecules 26(13): 3912
Publisher Policy:Reproduced under a Creative Commons License

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