Journal
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
Volume 24, Issue 2, Pages -Publisher
MDPI
DOI: 10.3390/ijms24021610
Keywords
organoselenium compounds; repurposing; antimicrobials; covalent drugs; bacterial proteins; cysteine modification; mechanisms of inhibition
Ask authors/readers for more resources
Ebselen is a compound with low-molecular-weight that has been extensively researched due to its antioxidant, anti-inflammatory, and cytoprotective properties. Its inhibition of various enzymes and proteins attributes to its antimicrobial potential, with the covalent modification of cysteine residues being a key mechanism. This article summarizes the current understanding of Ebselen's antibacterial activity, both alone and in combination with commercial pharmaceuticals, and explores its molecular mechanism. The specific inactivation of certain enzymes, bacterial toxins, and resistance factors shows potential therapeutic implications. The synergistic effect and sensitization to common antibiotics when using Ebselen are promising directions for treating persistent infections.
Ebselen is a low-molecular-weight organoselenium compound that has been broadly studied for its antioxidant, anti-inflammatory, and cytoprotective properties. These advantageous properties were initially associated with mimicking the activity of selenoprotein glutathione peroxidase, but the biomedical impact of this compound appear to be far more complex. Ebselen serves as a substrate or inhibitor with multiple protein/enzyme targets, whereas inhibition typically originates from the covalent modification of cysteine residues by opening the benzisoselenazolone ring and S-Se bond formation. The inhibition of enzymes of various classes and origins has been associated with substantial antimicrobial potential among other activities. In this contribution, we summarize the current state of the art regarding the antibacterial activity of ebselen. This activity, alone and in combination with commercial pharmaceuticals, against pathogens, including those resistant to drugs, is presented, together with the molecular mechanism behind the reactivity. The specific inactivation of thioredoxin reductase, bacterial toxins, and other resistance factors is considered to have certain therapeutic implications. Synergistic action and sensitization to common antibiotics assisted with the use of ebselen appear to be promising directions in the treatment of persistent infections.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available