Activity of Compounds from Temperate Propolis against Trypanosoma brucei and Leishmania mexicana

  • Molecules. 2021 Jun 26;26(13):3912. doi: 10.3390/molecules26133912.
Adullah Alotaibi  1 ,  Godwin U Ebiloma  2  3 ,  Roderick Williams  4 ,  Ibrahim A Alfayez  2  5  6 ,  Manal J Natto  2 ,  Sameah Alenezi  1 ,  Weam Siheri  7 ,  Malik AlQarni  6 ,  John O Igoli  1  2  8 ,  James Fearnley  9 ,  Harry P De Koning  2 ,  David G Watson  1
Affiliations
  • 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. School of Health and Life Sciences, Teesside University, Middlesbrough TS1 3BX, UK.
  • 4. IBEHR, School of Health and Life Science, University of the West of Scotland, High Street, Paisley PA1 2BE, UK.
  • 5. Qassim Health Cluster, Ministry of Health, Buraydah 52367, Saudi Arabia.
  • 6. Department of Pharmaceutical Chemistry, College of Clinical Pharmacy, Imam Abdulrahman Bin Faisal University, Dammam 31441, Saudi Arabia.
  • 7. Department of Pharmacognosy and Natural Products, Faculty of Pharmacy, University of Tripoli, Tripoli 50676, Libya.
  • 8. Department of Chemistry, University of Agriculture, Makurdi PMB 2373, Nigeria.
  • 9. BeeVital, Whitby, North Yorkshire YO22 5JR, UK.
PMID: 34206940 DOI: 10.3390/molecules26133912
Abstract

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.

Keywords
Leishmania mexicana; Trypanosoma brucei; flavonoids; isolated compounds; temperate propolis.
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