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Open AccessArticle

Unveiling the Mechanism of Action of 7α-acetoxy-6β-hydroxyroyleanone on an MRSA/VISA Strain: Membrane and Cell Wall Interactions

1
Research Center for Biosciences and Health Technologies (CBIOS), Universidade Lusófona de Humanidades e Tecnologias, Campo Grande, 376, 1749-024 Lisboa, Portugal
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Department of Biomedical Sciences, Faculty of Pharmacy, University of Alcalá, Campus Universitario, 28871 Alcalá de Henares, Spain
3
Departamento de Ciências da Vida, [email protected], Faculdade de Ciências e Tecnologia, Universidade Nova de Lisboa, 2825-149 Caparica, Portugal
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Centro de Química Estrutural, Faculdade de Ciências, Universidade de Lisboa, 1749-016 Lisboa, Portugal
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Instituto de Investigação do Medicamento (iMed.ULisboa), Faculdade de Farmácia, Universidade de Lisboa, 1649-003 Lisboa, Portugal
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Institute of Biophysics and Biomedical Bioengeneering (IBEB), Faculdade de Ciências, Universidade de Lisboa, 1749-016 Lisboa, Portugal
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Centro de Estudos do Ambiente e do Mar (CESAM), Faculdade de Ciências, Universidade de Lisboa, 1749-016 Lisboa, Portugal
*
Authors to whom correspondence should be addressed.
Biomolecules 2020, 10(7), 983; https://doi.org/10.3390/biom10070983
Received: 7 April 2020 / Revised: 19 June 2020 / Accepted: 25 June 2020 / Published: 30 June 2020
(This article belongs to the Special Issue Selected Papers from Bio.Natural Meeting 2019)
The number of cases of failure in the treatment of infections associated with resistant bacteria is on the rise, due to the decreasing efficacy of current antibiotics. Notably, 7α-Acetoxy-6β-hydroxyroyleanone (AHR), a diterpene isolated from different Plectranthus species, showed antibacterial activity, namely against Methicillin-resistant Staphylococcus aureus (MRSA) strains. The high antibacterial activity and low cytotoxicity render this natural compound an interesting alternative against resistant bacteria. The aim of this study is to understand the mechanism of action of AHR on MRSA, using the MRSA/Vancomycin-intermediate S. aureus (VISA) strain CIP 106760, and to study the AHR effect on lipid bilayers and on the cell wall. Although AHR interacted with lipid bilayers, it did not have a significant effect on membrane passive permeability. Alternatively, bacteria treated with this royleanone displayed cell wall disruption, without revealing cell lysis. In conclusion, the results gathered so far point to a yet undescribed mode of action that needs further investigation. View Full-Text
Keywords: 7α-Acetoxy-6β-hydroxyroyleanone; MRSA; antibacterial activity; membrane interaction; cell wall 7α-Acetoxy-6β-hydroxyroyleanone; MRSA; antibacterial activity; membrane interaction; cell wall
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Pereira, F.; Figueiredo, T.; de Almeida, R.F.M.; Antunes, C.A.C.; Garcia, C.; Reis, C.P.; Ascensão, L.; Sobral, R.G.; Rijo, P. Unveiling the Mechanism of Action of 7α-acetoxy-6β-hydroxyroyleanone on an MRSA/VISA Strain: Membrane and Cell Wall Interactions. Biomolecules 2020, 10, 983.

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