4 research outputs found
Antiviral, antimicrobial and antibiofilm activity of selenoesters and selenoanhydrides
Selenoesters and the selenium isostere of phthalic anhydride are bioactive selenium
compounds with a reported promising activity in cancer, both due to their cytotoxicity and capacity
to reverse multidrug resistance. Herein we evaluate the antiviral, the biofilm inhibitory, the
antibacterial and the antifungal activities of these compounds. The selenoanhydride and 7 out
of the 10 selenoesters were especially potent antiviral agents in Vero cells infected with herpes
simplex virus-2 (HSV-2). In addition, the tested selenium derivatives showed interesting antibiofilm
activity against Staphylococcus aureus and Salmonella enterica serovar Typhimurium, as well as a
moderate antifungal activity in resistant strains of Candida spp. They were inactive against anaerobes,
which may indicate that the mechanism of action of these derivatives depends on the presence of
oxygen. The capacity to inhibit the bacterial biofilm can be of particular interest in the treatment
of nosocomial infections and in the coating of surfaces of prostheses. Finally, the potent antiviral
activity observed converts these selenium derivatives into promising antiviral agents with potential
medical applications.
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 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 pathogen
Antiviral, antimicrobial and antibiofilm activity of selenoesters and selenoanhydrides
Selenoesters and the selenium isostere of phthalic anhydride are bioactive selenium
compounds with a reported promising activity in cancer, both due to their cytotoxicity and capacity
to reverse multidrug resistance. Herein we evaluate the antiviral, the biofilm inhibitory, the
antibacterial and the antifungal activities of these compounds. The selenoanhydride and 7 out
of the 10 selenoesters were especially potent antiviral agents in Vero cells infected with herpes
simplex virus-2 (HSV-2). In addition, the tested selenium derivatives showed interesting antibiofilm
activity against Staphylococcus aureus and Salmonella enterica serovar Typhimurium, as well as a
moderate antifungal activity in resistant strains of Candida spp. They were inactive against anaerobes,
which may indicate that the mechanism of action of these derivatives depends on the presence of
oxygen. The capacity to inhibit the bacterial biofilm can be of particular interest in the treatment
of nosocomial infections and in the coating of surfaces of prostheses. Finally, the potent antiviral
activity observed converts these selenium derivatives into promising antiviral agents with potential
medical applications.
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 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 pathogen