Selenocompounds as Novel Antibacterial Agents and Bacterial Efflux Pump Inhibitors

Autor: Carmen Sanmartín, Enrique Domínguez-Álvarez, Małgorzata Anna Marć, Andrea Csonka, Ádám Szabó Tönki, Karolina Witek, Gabriella Spengler, Jadwiga Handzlik, Katarzyna Kieć-Kononowicz, Tímea Mosolygó, Annamária Kincses
Přispěvatelé: Consejo Superior de Investigaciones Científicas (España), Hungarian Academy of Sciences, University of Szeged, Ministry of Human Capacities (Hungary)
Rok vydání: 2019
Předmět:
Chlamydia trachomatis D
Antibiotics
Staphylococcus aureus
Pharmaceutical Science
Chlamydia trachomatis
medicine.disease_cause
Escherichia coli K-12 AG100
Analytical Chemistry
Drug Resistance
Multiple
Bacterial
Drug Discovery
Enterococcus faecalis
Selenium Compounds
0303 health sciences
biology
Chemistry
Staphylococcal Infections
Antimicrobial
Anti-Bacterial Agents
Selenocompounds
Chemistry (miscellaneous)
Molecular Medicine
selenoesters
Efflux
Antibacterial activity
selenocompounds
Methicillin-Resistant Staphylococcus aureus
medicine.drug_class
Microbial Sensitivity Tests
Article
Selenoesters
Microbiology
lcsh:QD241-441
AcrAB-TolC efflux pump
03 medical and health sciences
Minimum inhibitory concentration
lcsh:Organic chemistry
Escherichia coli
medicine
Physical and Theoretical Chemistry
030304 developmental biology
030306 microbiology
Organic Chemistry
biochemical phenomena
metabolism
and nutrition
biology.organism_classification
Multiple drug resistance
Zdroj: Molecules
Volume 24
Issue 8
Dadun. Depósito Académico Digital de la Universidad de Navarra
instname
Digital.CSIC. Repositorio Institucional del CSIC
Molecules, Vol 24, Iss 8, p 1487 (2019)
ISSN: 1420-3049
2016-0003
Popis: 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 Staphylococcus aureus, methicillin resistant S. aureus (MRSA), Enterococcus faecalis, Escherichia coli, and Chlamydia trachomatis 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.
G.S. was supported by the János Bolyai Research Scholarship of the Hungarian Academy of Sciences, by the GINOP-2.3.2-15-2016-00038 project and by the University of Szeged, through the project SZTE ÁOK-KKA 2018/270-62-2. A.K. was supported by the ÚNKP-17-3 New National Excellence Program of the Ministry of Human Capacities of Hungary. E.D.A. was supported by the Spanish “Consejo Superior de Investigaciones Científicas” (CSIC, Spanish National Research Council), through Project 201780I027.
Databáze: OpenAIRE
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