ArticleScientific reports2020
Retention of antibiotic activity against resistant bacteria harbouring aminoglycoside-N-acetyltransferase enzyme by adjuvants: a combination of in-silico and in-vitro study.
Article in Scientific reports, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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12 citing papers in PubMed, 26 citations in OpenAlex.
- Differential modulation of gentamicin antibacterial activity by vitamin B12 and vitamin D3 against Gram-positive and Gram-negative bacteria: anAnnals of medicine · 2026Article
- Antifungal resistance: from classical mechanisms to the expanding role of acetyltransferases.Journal of biomedical science · 2026Review
- Antimicrobial Peptides as Antibiotic Adjuvants: Overcoming Resistance through Multifaceted Mechanisms.Probiotics and antimicrobial proteins · 2026Article
- Enhanced nanoencapsulation of gentamicin, ciprofloxacin, and lysozyme in chitosan-MIL-53 metal-organic frameworks for a synergistic activity against drug-resistantRSC advances · 2026Article
- New Frontiers for Old Medications: Repurposing Approved Drugs Against Gram-Negative Bacterial Infections.Microorganisms · 2025Review
- Inhibiting Amikacin Resistance in Multidrug-Resistant Bacteria with Cadmium and Pyrithione.Current microbiology · 2025Review
- Targeting Aminoglycoside Acetyltransferase Activity of Mycobacterium tuberculosis (H37Rv) Derived Eis (Enhanced Intracellular Survival) Protein with Quercetin.The protein journal · 2024Article
- Restoring susceptibility to aminoglycosides: identifying small molecule inhibitors of enzymatic inactivation.RSC medicinal chemistry · 2023Review
- Decoding the Mechanism of Specific RNA Targeting by Ribosomal Methyltransferases.ACS chemical biology · 2022Article
- Amikacin potentiator activity of zinc complexed to a pyrithione derivative with enhanced solubility.Scientific reports · 2022Article
- Bacterial Antibiotic Resistance: The Most Critical Pathogens.Pathogens (Basel, Switzerland) · 2021Review
- Zinc: Multidimensional Effects on Living Organisms.Biomedicines · 2021Review
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Interference with antibiotic activity and its inactivation by bacterial modifying enzymes is a prevailing mode of bacterial resistance to antibiotics. Aminoglycoside antibiotics become inactivated by aminoglycoside-6'-N-acetyltransferase-Ib [AAC(6')-Ib] of gram-negative bacteria which transfers an acetyl group from acetyl-CoA to the antibiotic. The aim of the study was to disrupt the enzymatic activity of AAC(6')-Ib by adjuvants and restore aminoglycoside activity as a result. The binding affinities of several vitamins and chemical compounds with AAC(6')-Ib of Escherichia coli, Klebsiella pneumoniae, and Shigella sonnei were determined by molecular docking method to screen potential adjuvants. Adjuvants having higher binding affinity with target enzymes were further analyzed in-vitro to assess their impact on bacterial growth and bacterial modifying enzyme AAC(6')-Ib activity. Four compounds-zinc pyrithione (ZnPT), vitamin D, vitamin E and vitamin K-exhibited higher binding affinity to AAC(6')-Ib than the enzyme's natural substrate acetyl-CoA. Combination of each of these adjuvants with three aminoglycoside antibiotics-amikacin, gentamicin and kanamycin-were found to significantly increase the antibacterial activity against the selected bacterial species as well as hampering the activity of AAC(6')-Ib. The selection process of adjuvants and the use of those in combination with aminoglycoside antibiotics promises to be a novel area in overcoming bacterial resistance.
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