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Pharmaceuticals
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Bioactive Compounds as Bacterial Efflux Pump Inhibitors
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Bioactive Compounds as Bacterial Efflux Pump Inhibitors

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Natural Products".

Deadline for manuscript submissions: closed (31 December 2023) | Viewed by 1290

Special Issue Editors

Prof. Dr. Jaime Ribeiro-Filho

E-Mail Website
Guest Editor
Oswaldo Cruz Foundation (FIOCRUZ), Eusébio, CE, Brazil
Interests: natural products; preclinical research; pharmacology; drug development; inflammatory diseases; antibiotic resistance; antifungals; ethnopharmacology; public health
Special Issues, Collections and Topics in MDPI journals
Dr. Irwin Rose Alencar Menezes

E-Mail Website
Guest Editor
Department of Biological Chemistry, Universidade Regional do Cariri, Crato, Brazil
Interests: natural product; bioctivity; inflammation; pain; antimicrobial activity; pharmacological activity
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Antibiotic resistance is responsible for approximately 700,000 yearly deaths worldwide. Therefore, managing infections caused by resistant bacteria and reducing the associated morbidity and mortality rates currently represent a significant challenge in public healthcare. Efflux pumps (EP) are cell membrane proteins that actively mediate the extrusion of dangerous compounds in various cells. In the context of antibiotic resistance, efflux pump expression stands out for the widespread occurrence among resistant bacterial strains, leading to the lack of effectiveness of a significant number of antibiotics. A large body of research has demonstrated that compounds of either synthetic or natural origin can potentiate the efficacy of conventional antibiotics against EP-overexpressing strains. Therefore, the discovery of bioactive compounds capable of acting as bacterial efflux pump inhibitors represents a promising strategy for combatting antibiotic resistance.

This Special Issue aims to gather manuscripts of all article types demonstrating the effectiveness of fully characterized bioactive compounds as efflux pump inhibitors and their impact on antibiotic resistance, through in vivo, ex vivo in vitro, and in silico testing.

Prof. Dr. Jaime Ribeiro-Filho
Dr. Irwin Rose Alencar Menezes
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceuticals is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • bioactive compounds
  • efflux pumps
  • bacterial strains
  • antibiotic resistance
  • drug development

Published Papers (1 paper)

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Research

18 pages, 2910 KiB  
Article
Antibacterial Potential of Symmetrical Twin-Drug 3,6-Diaminoxanthones
by Diana I. S. P. Resende, Fernando Durães, Sidika Zubarioglu, Joana Freitas-Silva, Nikoletta Szemerédi, Madalena Pinto, Eugénia Pinto, Paulo Martins da Costa, Gabriella Spengler and Emília Sousa
Pharmaceuticals 2024, 17(2), 209; https://doi.org/10.3390/ph17020209 - 6 Feb 2024
Viewed by 808
Abstract
Global health faces a significant issue with the rise of infectious diseases caused by bacteria, fungi, viruses, and parasites. The increasing number of multi-drug resistant microbial pathogens severely threatens public health worldwide. Antibiotic-resistant pathogenic bacteria, in particular, present a significant challenge. Therefore, there [...] Read more.
Global health faces a significant issue with the rise of infectious diseases caused by bacteria, fungi, viruses, and parasites. The increasing number of multi-drug resistant microbial pathogens severely threatens public health worldwide. Antibiotic-resistant pathogenic bacteria, in particular, present a significant challenge. Therefore, there is an urgent need to identify new potential antimicrobial targets and discover new chemical entities that can potentially reverse bacterial resistance. The main goal of this research work was to create and develop a library of 3,6-disubstituted xanthones based on twin drugs and molecular extension approaches to inhibit the activity of efflux pumps. The process involved synthesizing 3,6-diaminoxanthones through the reaction of 9-oxo-9H-xanthene-3,6-diyl bis(trifluoromethanesulfonate) with various primary and secondary amines. The resulting 3,6-disubstituted xanthone derivatives were then tested for their in vitro antimicrobial properties against a range of pathogenic strains and their efficacy in inhibiting the activity of efflux pumps, biofilm formation, and quorum-sensing. Several compounds have exhibited effective antibacterial properties against the Gram-positive bacterial species tested. Xanthone 16, in particular, has demonstrated exceptional efficacy with a remarkable MIC of 11 µM (4 µg/mL) against reference strains Staphylococcus aureus ATCC 25923 and Enterococcus faecalis ATCC 29212, and 25 µM (9 µg/mL) against methicillin-resistant S. aureus 272123. Furthermore, some derivatives have shown potential as antibiofilm agents in a crystal violet assay. The ethidium bromide accumulation assay pinpointed certain compounds inhibiting bacterial efflux pumps. The cytotoxic effect of the most promising compounds was examined in mouse fibroblast cell line NIH/3T3, and two monoamine substituted xanthone derivatives with a hydroxyl substituent did not exhibit any cytotoxicity. Overall, the nature of the substituent was critical in determining the antimicrobial spectra of aminated xanthones. Full article
(This article belongs to the Special Issue Bioactive Compounds as Bacterial Efflux Pump Inhibitors)
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