ArticleBritish journal of pharmacology2019
Pterostilbene restores carbapenem susceptibility in New Delhi metallo-β-lactamase-producing isolates by inhibiting the activity of New Delhi metallo-β-lactamases.
Article in British journal of pharmacology, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
What it found
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Who cites it
25 citing papers in PubMed, 45 citations in OpenAlex.
- Herbal extracts as antibiotic adjuvants against ESKAPE pathogens: mechanisms and therapeutic potential.Engineering microbiology · 2026Review
- Targeting MCR-3 and membrane biosynthesis: mechanistic insights into pterostilbene-colistin synergy.Microbiology spectrum · 2026Article
- Pterostilbene Eliminates MRSA Independent of Metabolic State and Effectively Prevents Biofilm Formation in Milk Matrices.Foods (Basel, Switzerland) · 2025Article
- Highly Conserved Genetic Factors RegulatingJournal of microbiology and biotechnology · 2025Article
- Morin combined with meropenem is a potent inhibitor of NDM-1 against NDM-1-producing E. coli.Scientific reports · 2025Article
- An anti-virulence drug targeting the evolvability protein Mfd protects against infections with antimicrobial resistant ESKAPE pathogens.Nature communications · 2025Article
- Epicatechin gallate and its analogues interact with sortase A and β-lactamase to suppressFrontiers in cellular and infection microbiology · 2025Article
- New Delhi Metallo-Beta-Lactamase Inhibitors: A Systematic Scoping Review.Journal of clinical medicine · 2024Article
- Cinnamaldehyde targets SarA to enhance β-lactam antibiotic activity against methicillin-resistantmLife · 2024Article
- Progress of Antimicrobial Mechanisms of Stilbenoids.Pharmaceutics · 2024Review
- Hydroxyhexylitaconic acids as potent IMP-type metallo-β-lactamase inhibitors for controlling carbapenem resistance inMicrobiology spectrum · 2024Article
- Identification of a Potential Inhibitor (MCULE-8777613195-0-12) of New Delhi Metallo-β-Lactamase-1 (NDM-1) Using In Silico and In Vitro Approaches.Molecules (Basel, Switzerland) · 2022Article
- Risedronate and Methotrexate Are High-Affinity Inhibitors of New Delhi Metallo-β-Lactamase-1 (NDM-1): A Drug Repurposing Approach.Molecules (Basel, Switzerland) · 2022Article
- An Evaluation of the Antibacterial Activity ofEvidence-based complementary and alternative medicine : eCAM · 2022Article
- Towards combating antibiotic resistance by exploring the quantitative structure-activity relationship of NDM-1 inhibitors.EXCLI journal · 2022Article
- Enzyme Inhibitors: The Best Strategy to Tackle Superbug NDM-1 and Its Variants.International journal of molecular sciences · 2021Review
- Article
- Spectroscopic and biochemical characterization of metallo-β-lactamase IMP-1 with dicarboxylic, sulfonyl, and thiol inhibitors.Bioorganic & medicinal chemistry · 2021Article
- Activity of β-Lactam Antibiotics against Metallo-β-Lactamase-ProducingAntimicrobial agents and chemotherapy · 2021Review
- Drug repurposing for next-generation combination therapies against multidrug-resistant bacteria.Theranostics · 2021Review
Corrections and comments
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Authors and funding
9 authors at 2 institutions in 1 country.
Funding
Abstract
background and purposeBacteria producing New Delhi metallo-β-lactamase-1 (NDM-1) are an increasing clinical threat. NDM-1 can inactivate almost all β-lactams and is not sensitive to any existing β-lactamase inhibitors. To identify effective inhibitors of the NDM-1 enzyme and clarify the mechanism of action, a "lead compound" for developing more potent NDM-1 inhibitors needs to be provided. EXPERIMENTAL APPROACH: Natural compounds were tested by enzyme inhibition screening to find potential inhibitors. MIC assays, growth curve assays, and time-kill assays were conducted to evaluate the in vitro antibacterial activity of pterostilbene and the combination of pterostilbene and meropenem. A murine thigh model and a mouse pneumonia model were used to evaluate the in vivo efficacy of combined therapy. Molecular modelling and a mutational analysis were used to clarify the mechanism of action. KEY
resultsPterostilbene significantly inhibited NDM-1 hydrolysis activity in enzyme inhibition screening assays and effectively restored the effectiveness of meropenem in vitro with NDM-expressing isolates in antibacterial activity assays. In addition, the combined therapy effectively reduced the bacterial burden in a murine thigh model and protected mice from pneumonia caused by Klebsiella pneumoniae. By means of molecular dynamics simulation, we observed that pterostilbene localized to the catalytic pocket of NDM-1, hindering substrate binding to NDM-1 and reducing NDM-1 activity. CONCLUSIONS AND IMPLICATIONS: These findings indicated that pterostilbene combined with meropenem may offer a new safe and potential "lead compound" for the further development of NDM-1 inhibitors.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.