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Adullah Alotaibi, Godwin U. Ebiloma, Roderick Williams, Ibrahim A. Alfayez, Manal J. Natto, Sameah Alenezi , Weam Siheri, Malik AlQarni , John O. Igoli, James Fearnley, Harry P. de Koning*, David G. Watson*
Research output: Contribution to journal › Article › peer-review
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 EC 50 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, pinos-trobin, 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 EC 50 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.
Original language | English |
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Article number | 3912 |
Number of pages | 16 |
Journal | Molecules |
Volume | 26 |
Issue number | 13 |
DOIs | |
Publication status | Published - 26 Jun 2021 |
Research output: Contribution to journal › Article › peer-review