Selenocompounds as Novel Antibacterial Agents and Bacterial Efflux Pump Inhibitors

Bacterial multidrug resistance is becoming a growing problem for public health, due to the development and spreading of bacterial strains resistant to antimicrobials. In this study, the antibacterial and multidrug resistance reversing activity of a series of seleno-carbonyl compounds has been evalua...

Full description

Bibliographic Details
Main Authors: Tímea Mosolygó, Annamária Kincses, Andrea Csonka, Ádám Szabó Tönki, Karolina Witek, Carmen Sanmartín, Małgorzata Anna Marć, Jadwiga Handzlik, Katarzyna Kieć-Kononowicz, Enrique Domínguez-Álvarez, Gabriella Spengler
Format: Article
Language:English
Published: MDPI AG 2019-04-01
Series:Molecules
Subjects:
Online Access:https://www.mdpi.com/1420-3049/24/8/1487
Description
Summary:Bacterial multidrug resistance is becoming a growing problem for public health, due to the development and spreading of bacterial strains resistant to antimicrobials. In this study, the antibacterial and multidrug resistance reversing activity of a series of seleno-carbonyl compounds has been evaluated. The effects of eleven selenocompounds on bacterial growth were evaluated in <i>Staphylococcus aureus</i>, methicillin resistant <i>S. aureus</i> (MRSA), <i>Enterococcus faecalis, Escherichia coli</i>, and <i>Chlamydia trachomatis</i> D. The combination effect of compounds with antibiotics was examined by the minimum inhibitory concentration reduction assay. Their efflux pump (EP) inhibitory properties were assessed using real-time fluorimetry. Relative expressions of EP and quorum-sensing genes were studied by quantitative PCR. Results showed that a methylketone selenoester had remarkable antibacterial activity against Gram-positive bacteria and potentiated the activity of oxacillin in MRSA. Most of the selenocompounds showed significant anti-chlamydial effects. The selenoanhydride and the diselenodiester were active inhibitors of the AcrAB-TolC system. Based on these results it can be concluded that this group of selenocompounds can be attractive potential antibacterials and EP inhibitors. The discovery of new derivatives with a significant antibacterial activity as novel selenocompounds, is of high impact in the fight against resistant pathogens.
ISSN:1420-3049