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A New Discovery of Unique 13-(Benzimidazolylmethyl)berberines as Promising Broad-Spectrum Antibacterial Agents
- Source :
- Journal of Agricultural and Food Chemistry; 20220101, Issue: Preprints
- Publication Year :
- 2022
-
Abstract
- A new hybridization of berberine and benzimidazoles was performed to produce 13-(benzimidazolylmethyl)berberines (BMB) as potentially broad-spectrum antibacterial agents with the hope of confronting multidrug-resistant bacterial infections in the livestock industry. Some of the newly prepared hybrids showed obvious antibacterial effects against tested strains. Particularly, 13-((1-octyl-benzimidazolyl)methyl)berberine 6f(OBMB-6f) was found to be the most promising compound that not only exerted a strong activity (MIC = 0.25–2 μg/mL) and low cytotoxicity but also possessed a fast bactericidal capacity and low propensity to develop resistance toward Staphylococcus aureusand Escherichia colieven after 26 serial passages. Moreover, OBMB-6fdisplayed the ability to prevent bacterial biofilm formation at low and high temperatures. The mechanistic exploration revealed that OBMB-6fcould significantly disintegrate bacterial membranes, markedly facilitate intracellular ROS generation, and efficiently intercalate into DNA. These results provided a profound insight into BMB against multidrug-resistant bacterial infections in the livestock industry.
Details
- Language :
- English
- ISSN :
- 00218561 and 15205118
- Issue :
- Preprints
- Database :
- Supplemental Index
- Journal :
- Journal of Agricultural and Food Chemistry
- Publication Type :
- Periodical
- Accession number :
- ejs60857122
- Full Text :
- https://doi.org/10.1021/acs.jafc.2c03849