Antibacterial and Antibiofilm Potency of Menadione Against Multidrug-Resistant S. aureus

Klebsiella pneumoniae is one of the members of the ESKAPE ( Enterococcus faecium , Staphylococcus aureus , Klebsiella pneumoniae , Acinetobacter baumannii , Pseudomonas aeruginosa , and Enterobacter species) group of pathogens and is responsible for nosocomial infections. The global increase of carbapenem-resistant K. pneumoniae has developed a substantial clinical threat because of the dearth of therapeutic choices available. K. pneumoniae is one of the commonly found bacteria responsible for biofilm-related infections.

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“…Untreated control samples were also run to obtain the bacterial count. Experiments were carried out in triplicates ( 41 , 51 ).…”

Section: Methodsmentioning

confidence: 99%

Characterization of Novel Klebsiella Phage PG14 and Its Antibiofilm Efficacy

2022

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“…Menadione, being a lipophilic substance, might attack the bacterial membrane thereby disrupting its integrity and enhancing membrane permeability. Mone et al [14] documented the antibacterial activity of menadione against ESKAPE and MDR pathogens and reported that S. aureus (64-256 μg/mL) was more susceptible to this compound than other Gramnegative MDR isolates. Lim et al [50] assessed the antibacterial activity of 1,4-NQ, 5-hydroxy-1,4-NQ and 5-hydroxy-2-methyl-1,4-NQ against Bifidobacterium bifidum, C. perfringens, E. coli and Lactobacillus casei.…”

Section: Methyl Group-containing 14-nqsmentioning

confidence: 99%

“…Among these different antimicrobial agents, naphthoquinones (NQs) and their derivatives have received the attention of researchers due to their exceptional structural diversity and varied biological and functional properties. [13,14,15] NQs are found as natural pigments in a variety of plants, fungi, and some animals. [16] NQs are bicyclic molecules comprising two carbonyl groups located either at the 1, 2 or 1, 4 positions.…”

Section: Introductionmentioning

confidence: 99%

“…[18] NQs are an emerging class of antibacterial agents that may be effective against priority pathogens in the ESKAPE and MDR categories. [13,14] The abbreviation ESKAPE is used to describe the bacterial pathogens Enterococcus faecium, Staphylococcus aur-eus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, and Enterobacter spp. [19] In 2017, WHO published a list of priority pathogens (critical, high, and medium) based on the severity of resistance towards antimicrobial agents and emphasized the need to develop new strategies to tackle the emergence of AMR.…”

Section: Introductionmentioning

confidence: 99%

“…[1] 1,4-NQs act against ESKAPE and MDR pathogens through diverse mechanisms of action such as curing of plasmids, [20] inhibition of efflux pumps, [21] generation of reactive oxygen species (ROS), [22] inhibition of DNA gyrases, [23] disruption of membrane potential [24] , and inhibition of biofilms. [14,16] NQs possess a variety of functional groups viz. hydroxyl (À OH), methyl (À CH 3 ), sulfur (À S), and non-metallic elements (halides (X = fluorine, F; chlorine, Cl; bromine, Br; iodine, I, and astatine, At) and metals (Zn, Ni, Mg, Mn, Pb, Co).…”

Section: Introductionmentioning

confidence: 99%

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How Structure–Function Relationships of 1,4‐Naphthoquinones Combat Antimicrobial Resistance in Multidrug‐Resistant (MDR) Pathogens

et al. 2022

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Antimicrobial resistance (AMR) is one of the top ten health‐related threats worldwide. Among several antimicrobial agents, naphthoquinones (NQs) of plant/chemical origin possess enormous structural and functional diversity and are effective against multidrug‐resistant (MDR) pathogens. 1,4‐NQs possess alkyl, hydroxyl, halide, and metal groups as side chains on their double‐ring structure, predominantly at the C‐2, C‐3, C‐5, and C‐8 positions. Among 1,4‐NQs, hydroxyl groups at either C‐2 or C‐5 exhibit significant antibacterial activity against Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, Enterobacter spp. (ESKAPE) and MDR categories. 1,4‐NQs exhibit antibacterial activities like plasmids curing, reactive oxygen species generation, efflux pumps inhibition, anti‐DNA gyrase activity, membrane permeabilization, and biofilm inhibition. This review emphasizes the structure‐function relationships of 1,4‐NQs against ESKAPE and MDR pathogens based on a literature review of studies published in the last 15 years. Overall, 1,4‐NQs have great potential for counteracting the antimicrobial resistance of MDR pathogens.

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Synergistic and Additive Effects of Menadione in Combination with Antibiotics on Multidrug‐Resistant Staphylococcus aureus: Insights from Structure‐Function Analysis of Naphthoquinones

Mone,

Syed,

Ravichandiran

et al. 2023

ChemMedChem

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Antimicrobial resistance (AMR) has interfered with effective treatment of microbial infection and increased the risk of microbial spread, illness, and deaths. The synergistic activities of combinations of antimicrobials offer satisfactory approaches to some extent. Structurally diverse naphthoquinones (NQs) including menadione (‐CH3 at C‐2) exhibit substantial antimicrobial activities against multidrug‐resistant (MDR) pathogens. We explored the combinations of menadione with antibiotic ciprofloxacin or ampicillin against Staphylococcus aureus and its biofilms. We found an additive (0.5 < FICI ≤ 1.0) and synergistic (FICI ≤ 0.5) effect of menadione with ciprofloxacin and ampicillin, respectively. High reactive oxygen species (ROS) activity and inhibition of biofilm formation (>90%) were also seen. However, preformed biofilms were not affected. Dent formation was also evident in S. aureus treated with the test compounds. The structure‐function relationship (SFR) of NQs was used to determine and predict their activity pattern against pathogens. Analysis of 10 structurally distinct NQs revealed that the compounds with ‐Cl, ‐Br, ‐CH3, or ‐OH groups displayed the lowest MICs (32–256 µg/mL). Furthermore, 1,4‐NQs possessing a halogen or ‐CH3 moiety showed elevated ROS activity, whereas molecules with an ‐OH group affected the cell integrity. Improved activity of antimicrobial combinations and SFR approaches are significant in antimicrobial therapies.

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Antibacterial and Antibiofilm Potency of Menadione Against Multidrug-Resistant S. aureus

Cited by 15 publications

References 42 publications

Characterization of Novel Klebsiella Phage PG14 and Its Antibiofilm Efficacy

Characterization of Novel Klebsiella Phage PG14 and Its Antibiofilm Efficacy

How Structure–Function Relationships of 1,4‐Naphthoquinones Combat Antimicrobial Resistance in Multidrug‐Resistant (MDR) Pathogens

Synergistic and Additive Effects of Menadione in Combination with Antibiotics on Multidrug‐Resistant Staphylococcus aureus: Insights from Structure‐Function Analysis of Naphthoquinones

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