Design, synthesis and drug resistance reversal potential of novel curcumin mimics Van D

Dwivedi, Gaurav Raj; Khwaja, Sadiya; Negi, Arvind S.; Panda, Swati Sagarika; Sanket, A. Swaroop; Gupta, Akhilesh Kumar; Bawankule, Dnyaneshwar Umrao; Chanda, Debabrata; Kant, Rajni; Darokar, Mahendra P.

doi:10.1016/j.bioorg.2020.104454

Cited by 4 publications

(4 citation statements)

References 64 publications

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“…In this study, MSW and MPC determination were performed for all the 23 S. aureus isolates and for the reference strain S. aureus ATCC 29213, using 10 10 CFU/mL bacterial suspensions. Determinations were performed twice, as previously reported [ 32 , 33 , 34 ]. This concentration was selected based on the fact that the usual bacterial concentration found in infections, around 10 5 CFU/mL per gram of tissue, is five-fold lower than the concentration used in this protocol, which guarantees that the antimicrobial concentration obtained will be able to eliminate all the bacteria present in in vivo infections [ 8 ].…”

Section: Resultsmentioning

confidence: 99%

Nisin Mutant Prevention Concentration and the Role of Subinhibitory Concentrations on Resistance Development by Diabetic Foot Staphylococci

et al. 2022

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The most prevalent microorganism in diabetic foot infections (DFI) is Staphylococcus aureus, an important multidrug-resistant pathogen. The antimicrobial peptide nisin is a promising compound for DFI treatment, being effective against S. aureus. However, to avoid the selection of resistant mutants, correct drug therapeutic doses must be established, being also important to understand if nisin subinhibitory concentrations (subMIC) can potentiate resistant genes transfer between clinical isolates or mutations in genes associated with nisin resistance. The mutant selection window (MSW) of nisin was determined for 23 DFI S. aureus isolates; a protocol aiming to prompt vanA horizontal transfer between enterococci to clinical S. aureus was performed; and nisin subMIC effect on resistance evolution was assessed through whole-genome sequencing (WGS) applied to isolates subjected to a MEGA-plate assay. MSW ranged from 5–360 μg/mL for two isolates, from 5–540 μg/mL for three isolates, and from 5–720 μg/mL for one isolate. In the presence of nisin subMIC values, no transconjugants were obtained, indicating that nisin does not seem to promote vanA transfer. Finally, WGS analysis showed that incubation in the presence of nisin subMIC did not promote the occurrence of significant mutations in genes related to nisin resistance, supporting nisin application to DFI treatment.

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Section: Resultsmentioning

confidence: 99%

Nisin Mutant Prevention Concentration and the Role of Subinhibitory Concentrations on Resistance Development by Diabetic Foot Staphylococci

et al. 2022

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“…In the last two decades, combinatorial approach has yielded several potential derivatives of natural compounds [23,24] and these helped us to strive on combinatorial potential of natural compounds and their derivatives [25–37] . The present study depicts the enhancement of antibacterial potential of TET and ofloxacin (OFL) in combination with chalcones derived from a plant phenolic acid i. e. gallic acid.…”

Section: Introductionmentioning

confidence: 84%

“…[18,20,21,22] In the last two decades, combinatorial approach has yielded several potential derivatives of natural compounds [23,24] and these helped us to strive on combinatorial potential of natural compounds and their derivatives. [25][26][27][28][29][30][31][32][33][34][35][36][37] The present study depicts the enhancement of antibacterial potential of TET and ofloxacin (OFL) in combination with chalcones derived from a plant phenolic acid i. e. gallic acid. Chalcones with 3, 4, 5trimethoxyphenyl unit were reported as enhancer of the potency of drug (epirubicin) by inhibiting the efflux pump (human mdr1), as well as our previous work on bioenhancing potential of gallic acid derived compounds with 3, 4, 5trimethoxyphenyl unit against drug resistant E. coli.…”

Section: Introductionmentioning

confidence: 87%

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Synergistic Antibacterial Activity of Gallic Acid Based Chalcone Indl 2 by Inhibiting Efflux Pump Transporters

Dwivedi,

Pathak,

Tiwari

et al. 2024

Chemistry & Biodiversity

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As a part of novel discovery of drugs from natural resources, present study was undertaken to explore the antibacterial potential of chalcone Indl‐2 in combination with different group of antibiotics. MIC of antibiotics was reduced up to eight folds against the different cultures of E. coli by both chalcones. Among the two used compounds, the i.e. 1‐(3’, 4,’5’‐trimethoxyphenyl)‐3‐(3‐Indyl)‐prop‐2‐enone (6, Indl‐2), a chalcone derivative of gallic acid (Indl‐2) was best better along with tetracycline (TET) worked synergistically and was found to inhibit efflux transporters as obvious by ethidium bromide efflux confirmed by ATPase assays and docking studies. In combination, Indl‐2 kills the MDREC‐KG4 cells, post‐antibiotic effect (PAE) of TET was prolonged and mutant prevention concentration (MPC) of TET was also decreased. In‐vivo studies revealed that Indl‐2 reduces the concentration of TNF‐α. In acute oral toxicity study, Indl‐2 was non‐toxic and well tolerated up‐to dose of 2000 mg/kg. Perhaps, the study is going to report gallic acid derived chalcone as synergistic agent acting via inhibiting the primary efflux pumps.

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Nanoparticles: Warheads to Overcome the Resistance Mechanism of Bacterial Superbugs

Sahoo

Sanket

Kant

et al. 2022

Nanotechnology for Infectious Diseases

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Design, synthesis and drug resistance reversal potential of novel curcumin mimics Van D

Cited by 4 publications

References 64 publications

Nisin Mutant Prevention Concentration and the Role of Subinhibitory Concentrations on Resistance Development by Diabetic Foot Staphylococci

Nisin Mutant Prevention Concentration and the Role of Subinhibitory Concentrations on Resistance Development by Diabetic Foot Staphylococci

Synergistic Antibacterial Activity of Gallic Acid Based Chalcone Indl 2 by Inhibiting Efflux Pump Transporters

Nanoparticles: Warheads to Overcome the Resistance Mechanism of Bacterial Superbugs

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