TY - JOUR
T1 - Activity of compounds from temperate propolis against Trypanosoma brucei and Leishmania mexicana
AU - Alotaibi, Abdullah
AU - Ebiloma, Godwin U.
AU - Williams, Roderick
AU - Alfayez, Ibrahim A.
AU - Natto, Manal J.
AU - Alenezi, Sameah
AU - Siheri, Weam
AU - AlQarni, Malik
AU - Igoli, John O.
AU - Fearnley, James
AU - de Koning, Harry P.
AU - Watson, David G.
PY - 2021/6/26
Y1 - 2021/6/26
N2 - Ethanolic extracts of samples of temperate zone propolis, four from the UK and one from Poland, were tested against three strains and displayed EC 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 and , with the highest activities ≤ 15 µM. The most active compounds against were naringenin 4',7 dimethyl ether and 4'methoxy kaempferol with activity of 15-20 µM against the three strains. The most active compounds against were 4',7-dimethoxykaempferol and the coumaric acid ester mixture, with EC 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 strains, or the miltefosine-resistant strain; no clear structure activity relationship was observed for the isolated compounds. Temperate propolis yields multiple compounds with anti-kinetoplastid activity.
AB - Ethanolic extracts of samples of temperate zone propolis, four from the UK and one from Poland, were tested against three strains and displayed EC 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 and , with the highest activities ≤ 15 µM. The most active compounds against were naringenin 4',7 dimethyl ether and 4'methoxy kaempferol with activity of 15-20 µM against the three strains. The most active compounds against were 4',7-dimethoxykaempferol and the coumaric acid ester mixture, with EC 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 strains, or the miltefosine-resistant strain; no clear structure activity relationship was observed for the isolated compounds. Temperate propolis yields multiple compounds with anti-kinetoplastid activity.
KW - temperate propolis
KW - flavonoids
KW - isolated compounds
KW - Trypanosoma brucei
KW - Leishmania 40 mexicana
U2 - 10.3390/molecules26133912
DO - 10.3390/molecules26133912
M3 - Article
SN - 1420-3049
VL - 26
JO - Molecules
JF - Molecules
IS - 13
M1 - 3912
ER -