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1.
Fitoterapia ; 158: 105172, 2022 Apr.
Article in English | MEDLINE | ID: mdl-35283240

ABSTRACT

Four undescribed secocycloartane monoglycosides (1-4) were isolated from an ethanolic extract of the dry flowers of Cordia lutea Lam. Their structural assignment is based on NMR and MS analysis. Their stereochemistry is confirmed by molecular modelling studies using DFT-NMR calculations done for compound 3. In vitro antibacterial activity of the four compounds was moderate on Helicobacter pylori (MIC = 15.6 µg/mL), and much weaker on Staphylococcus aureus, Pseudomonas aeruginosa or Escherichia coli (MIC >125 µg/mL). Toxicity evaluated against RAW 264.7 cells was weak (IC50 values ranging from 24 to 41 µM i.e. 15 to 24 µg/mL), but in the same range as anti-Helicobacter activity.


Subject(s)
Cordia , Anti-Bacterial Agents , Cordia/chemistry , Glycosides/pharmacology , Microbial Sensitivity Tests , Molecular Structure , Plant Extracts/chemistry
2.
Planta Med ; 87(3): 201-208, 2021 Mar.
Article in English | MEDLINE | ID: mdl-33231270

ABSTRACT

Four isocedrenes (1:  - 4: ), including one new compound (2: ), were isolated from an ethanolic extract of the aerial parts of Perezia multiflora by bioactivity-guided fractionation. For compounds 1: and 3: , a revised stereochemical assignment is proposed based on molecular modeling studies using DFT-NMR calculations. Antiparasitic activity of the four compounds was evaluated using an in vitro culture of Plasmodium falciparum and axenic amastigotes of Leishmania infantum. IC50 values ranged from 0.81 to 16.1 µM (P. falciparum) and 0.16 to 2.03 µM (L. infantum). Toxicity was evaluated against J774A.1 mouse macrophages or human macrophages generated from THP-1 monocytic cells (IC50 values ranging from 0.16 to 2.64 µM). Compound 4: exhibited weak selectivity against P. falciparum with a selectivity index (SI = CC50/IC50) of 3. No selectivity was observed for compounds 1:  - 3: against both parasites.


Subject(s)
Antiprotozoal Agents , Asteraceae , Leishmania infantum , Malaria, Falciparum , Humans , Plasmodium falciparum
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