2. Academic Validation
  3. The plant-derived chalcone Xanthoangelol targets the membrane of Gram-positive bacteria

The plant-derived chalcone Xanthoangelol targets the membrane of Gram-positive bacteria

  • Bioorg Med Chem. 2019 Dec 1;27(23):115151. doi: 10.1016/j.bmc.2019.115151.
Dieter Meier 1,  Melissa Vázquez Hernández 2,  Lasse van Geelen 1,  Rini Muharini 3,  Peter Proksch 1,  Julia E Bandow 2,  Rainer Kalscheuer 4
Affiliations

Affiliations

  • 1 Institute of Pharmaceutical Biology and Biotechnology, Heinrich Heine University Düsseldorf, Universitätsstrasse 1, 40225 Düsseldorf, Germany.
  • 2 Applied Microbiology, Faculty of Biology and Biotechnology, Ruhr University Bochum, Universitätsstrasse 150, 44780 Bochum, Germany.
  • 3 Institute of Pharmaceutical Biology and Biotechnology, Heinrich Heine University Düsseldorf, Universitätsstrasse 1, 40225 Düsseldorf, Germany; Department of Chemistry Education, Faculty of Education, Tanjungpura University, 78124 Pontianak, Indonesia.
  • 4 Institute of Pharmaceutical Biology and Biotechnology, Heinrich Heine University Düsseldorf, Universitätsstrasse 1, 40225 Düsseldorf, Germany. Electronic address: rainer.kalscheuer@hhu.de.
PMID: 31648878 DOI: 10.1016/j.bmc.2019.115151
Abstract

Xanthoangelol is a geranylated chalcone isolated from fruits of Amorpha fructicosa that exhibits Antibacterial effects at low micromolar concentration against Gram-positive Bacterial pathogens such as methicillin-resistant Staphylococcus aureus (MRSA), Enterococcus faecium and Enterococcus faecalis. We demonstrate that Xanthoangelol treatment of Gram-positive bacteria affects Bacterial membrane integrity and leads to a leakage of intracellular metabolites. This correlates with a rapid collapse of the membrane potential and results in a fast and strong bactericidal effect. Proteomic profiling of Xanthoangelol-treated cells revealed signatures of cell wall and/or membrane damage and oxidative stress. Xanthoangelol specifically disturbs the membrane of Gram-positive bacteria potentially by forming pores resulting in Cell Lysis. In contrast, Xanthoangelol treatment of human cells showed only mildly hemolytic and cytotoxic effects at higher concentrations. Therefore, geranylated Chalcones such as Xanthoangelol are promising lead structures for new antimicrobials against drug-resistant gram-positive pathogens.

Keywords

Amorpha fructicosa; Antibacterial activity; Chalcone; Cytotoxicity; Hemolysis; MRSA; Membrane; Phenolic metabolite; Xanthoangelol.

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