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Molecules 2019, 24(6), 1024; https://doi.org/10.3390/molecules24061024

Phenolic Compounds from Humulus lupulus as Natural Antimicrobial Products: New Weapons in the Fight against Methicillin Resistant Staphylococcus aureus, Leishmania mexicana and Trypanosoma brucei Strains

1
EA 7394—ICV, Charles Viollette Research Institute, SFR Condorcet FR CNRS 3417, Univ. Lille, INRA, ISA-Yncréa, Univ. Artois, University Littoral Côte d’Opale, 3 rue du Professeur Laguesse, 59000 Lille, France
2
Pharmacognosy Research group, Louvain Drug Research Institute, Université Catholique de Louvain, 1200 Brussels, Belgium
3
U995—LIRIC, Lille Inflammation Research International Center, University Lille, Inserm, CHU Lille, 59000 Lille, France
4
U1008—Controlled Drug Delivery Systems and Biomaterials, University Lille, Inserm, CHU Lille, 59000 Lille, France
*
Author to whom correspondence should be addressed.
Academic Editor: Pinarosa Avato
Received: 28 January 2019 / Revised: 9 March 2019 / Accepted: 10 March 2019 / Published: 14 March 2019
(This article belongs to the Special Issue Natural Products and Drug Discovery)
PDF [1109 KB, uploaded 14 March 2019]

Abstract

New anti-infective agents are urgently needed to fight microbial resistance. Methicillin-resistant Staphylococcus aureus (MRSA) strains are particularly responsible for complicated pathologies that are difficult to treat due to their virulence and the formation of persistent biofilms forming a complex protecting shell. Parasitic infections caused by Trypanosoma brucei and Leishmania mexicana are also of global concern, because of the mortality due to the low number of safe and effective treatments. Female inflorescences of hop produce specialized metabolites known for their antimicrobial effects but underexploited to fight against drug-resistant microorganisms. In this study, we assessed the antimicrobial potential of phenolic compounds against MRSA clinical isolates, T. brucei and L. mexicana. By fractionation process, we purified the major prenylated chalcones and acylphloroglucinols, which were quantified by UHPLC-UV in different plant parts, showing their higher content in the active flowers extract. Their potent antibacterial action (MIC < 1 µg/mL for the most active compound) was demonstrated against MRSA strains, through kill curves, post-antibiotic effects, anti-biofilm assays and synergy studies with antibiotics. An antiparasitic activity was also shown for some purified compounds, particularly on T. brucei (IC50 < 1 to 11 µg/mL). Their cytotoxic activity was assessed both on cancer and non-cancer human cell lines.
Keywords: Humulus lupulus; prenylated phenolic compounds; antimicrobial agents; methicillin-resistant Staphylococcus aureus; Leishmania mexicana mexicana; Trypanosoma brucei brucei Humulus lupulus; prenylated phenolic compounds; antimicrobial agents; methicillin-resistant Staphylococcus aureus; Leishmania mexicana mexicana; Trypanosoma brucei brucei
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).
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Bocquet, L.; Sahpaz, S.; Bonneau, N.; Beaufay, C.; Mahieux, S.; Samaillie, J.; Roumy, V.; Jacquin, J.; Bordage, S.; Hennebelle, T.; Chai, F.; Quetin-Leclercq, J.; Neut, C.; Rivière, C. Phenolic Compounds from Humulus lupulus as Natural Antimicrobial Products: New Weapons in the Fight against Methicillin Resistant Staphylococcus aureus, Leishmania mexicana and Trypanosoma brucei Strains. Molecules 2019, 24, 1024.

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