Affiliation:
1. Department of Organic Chemistry, Faculty of Sciences, University
Autónoma of Madrid, Cantoblanco, Madrid, Spain
2. Department of Pharmacology, Pharmacognosy and Botany, Faculty of
Pharmacy, University Complutense of Madrid, Madrid, Spain
3. Dr. Goya Análisis, SL, Alcalá de Henares, Madrid,
Spain
Abstract
Abstract
Buddleja coriacea Remy is one of the plant species used by the Bolivian
population for the treatment of urinary infections. This study aimed to identify
the extract, fractions, and compounds responsible for the antibacterial and
anti-inflammatory activities of B. coriacea leaves. Bioguided isolation
of compounds with antibacterial and anti-inflammatory activities was carried out
by measuring the antibacterial effect against specific pathogenic microbial
strains, Klebsiella pneumoniae, Proteus mirabilis, Pseudomonas
aeruginosa, and Serratia marcescens, and the inhibition of
NF-κB in RM-2 and MM.14Ov cells. Bioassay-guided isolation
led to the isolation and characterisation of
(4aR,4bS,5 S,6aS,6bS,9aR,10aS,10bS)-6b-glycoloyl-5-hydroxy-4a,6a-dimethyl-8-propyl-4a,4b,5,6,6a,6b,9a,10,10a,10b,11,12-dodecahydro-2H-naphtho
[2',1':4,5] indeno [1,2-d][1,3] dioxol-2-one (1),
3-[3-(2-dimethylaminoethyl)-1H-indol-5-yl]-N-(4-methoxybenzyl)
acrylamide (2), and
(1β,11β,12α)-1,11,12-trihydroxy-11,20-epoxypicrasa-3,13(21)-diene-2,16-dione
(3) by nuclear magnetic resonance and mass spectroscopy. All
compounds showed antibacterial activity with minimum inhibitory concentration
values of 11.64–11.81, 0.17–0.19, and
0.34–0.36 µM, respectively, on the tested
strains, while the positive control, ofloxacin, had a minimum inhibitory
concentration of 27.66 µM. Finally, all the compounds
showed NF-κB inhibitory activity with IC50 values of
11.25–11.34, 0.15–0.16, and
0.33–0.36 µM, respectively, in all cell
lines, while the positive control, celastrol, had an IC50 of
7.96 µM. Thus, this study managed to isolate and
evaluate for the first time the pharmacological potential of three compounds
present in the leaves of B. coriacea with antibacterial and
anti-inflammatory activities.