Antituberculosis Activities of Lapachol and β-Lapachone in Combination with Other Drugs in Acidic pH

Ieque, Andressa Lorena; Carvalho, Hayalla Corrêa de; Baldin, Vanessa Pietrowski; Santos, Nathally Claudiane de Souza; Costacurta, Giovana Ferreira; Sampiron, Eloísa G; Andrade, Carla Maria Mariano Fernandez de; Siqueira, Vera Lúcia Dias; Ferracioli, Katiany Rizzieri Caleffi; Cardoso, Rosilene Fressatti; Cortez, Diógenes Aparı́cio Garcia; Silva, Expedito Leite; Scodro, Regiane Bertin de Lima

doi:10.1089/mdr.2020.0164

Cited by 4 publications

(4 citation statements)

References 45 publications

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“…Several primary actives had low antibacterial MIC values and acted on H. pylori probably via metabolic inhibition. For further studies, we selected one small molecule, named Active1 (β-lapachone, a 2,4-naphthoquinone) long-known to have antibacterial effects on a variety of species ( 44 , 46 ), but not yet characterized to be active against H. pylori . β-lapachone derivatives, due to their cell-killing activity, are currently being further developed as anticancer agents ( 45 , 47 , 72 ) and were also strongly active against H. pylori in our hands.…”

Section: Discussionmentioning

confidence: 99%

Identification of Antimotilins, Novel Inhibitors of Helicobacter pylori Flagellar Motility That Inhibit Stomach Colonization in a Mouse Model

Suerbaum

Coombs

Patel

et al. 2022

mBio

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Section: Discussionmentioning

confidence: 99%

Identification of Antimotilins, Novel Inhibitors of Helicobacter pylori Flagellar Motility That Inhibit Stomach Colonization in a Mouse Model

Suerbaum

Coombs

Patel

et al. 2022

mBio

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“…β-Lap possesses antibacterial properties which act against a variety of bacteria species, including M. tuberculosis , its multidrug resistant (MDR) clinical isolates and methicillin resistant S. aureus (MRSA). β-Lap showed additive effect in combination with first line tuberculosis drugs and synergic effect with N-acetylcysteine against M. tuberculosis H37Rv [ 12 ]. In addition, it synergistically inhibited the growth of methicillin resistant S. aureus (MRSA) in combination with fluoroquinolones, carbapenems, and other beta-lactam antibiotic [ 13 ].…”

Section: Introductionmentioning

confidence: 99%

Antibacterial and Antibiofilm Activities of β-Lapachone by Modulating the Catalase Enzyme

et al. 2023

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Background: Bacterial infections constantly have a large impact on public health, because of increased rates of resistance and reduced frequency of development of novel antibiotics. The utility of conventional antibiotics for treating bacterial infections has become increasingly challenging. The aim of the study was to assess the antibacterial effect of β-Lapachone (β-Lap), a novel synthetic compound. Methods: The antibacterial activity of the β-Lap compound was examined against laboratory strains by agar well diffusion method and broth dilution assay. Growth kinetics in presence of β-Lap on Staphylococcus aureus, Staphylococcus epidermidis, and Pseudomonas aeruginosa (ATCC 27853) were assessed by microplate alamarBlue assay. Crystal violet blue assay was used for biofilm inhibition and biofilm eradication. P. aeruginosa catalase (KatA) complexed with β-Lap was modeled using molecular docking approach. Results: β-Lap exhibited potent antimicrobial activity against laboratory strains of bacteria with MIC of 0.2 mM for S. saprophyticus and Staphylococcus aureus, and 0.04 mM for Staphylococcus epidermidis and Pseudomonas aeruginosa ATCC 27853. The inhibition of catalase enzyme was found to be the cause for its antibacterial activity. Bioinformatics analysis suggests that β-Lap can inhibit KatA activity by interacting with catalase proximal active site and heme binding site. The activity of some commercial antibiotics was enhanced in association with β-Lap. In addition, β-Lap inhibited the biofilm formation and eradicated the already formed and ultra-mature biofilms of aforesaid bacterial strains. Conclusion: These observations indicated that β-Lap could be a promising antibacterial agent for the treatment and prevention of infectious diseases.

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“…β -Lap possesses antibacterial properties against a variety of bacteria species, including M. tuberculosis, its MDR clinical isolates, methicillin resistant S. aureus (MRSA). β -Lap showed additive effect in combination with first line TB drugs and synergic effect with Nacetylcysteine against M. tuberculosis H37Rv (10). In addition, it synergistically inhibited the growth of methicillin resistant S. aureus (MRSA) in combination with fluoroquinolones, carbapenems, and beta lactams (11).…”

Section: Introductionmentioning

confidence: 99%

Antibacterial and Antibiofilm Activities of Β –Lapachone by Modulating the Catalase Enzyme

Mir¹,

Altuhami²,

Mondal³

et al. 2023

Preprint

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Background: Bacterial infections constantly have a large impact on public health, because of increased rates of resistance and reduced frequency of development of novel antibiotics. The utility of conventional antibiotics for treating bacterial infections has become increasingly challenging. The aim of the study was to assess the antibacterial effect of β -Lapachone, a novel synthetic compound. Methods: The antibacterial activity of the β -Lapachone compound was examined against laboratory strains by agar well diffusion method, minimal inhibitory concentration (MICs), and minimal bactericidal concentration (MBCs). Growth kinetics inhibition in presence of β -Lapachone on Staphylococcus aureus, Staphylococcus epidermidis and Pseudomonas aeruginosa (ATCC 27853) was assessed by MABA. Crystal violet blue assay was used for biofilm inhibition assays, biofilm eradication assay and for molecular modeling PyMOL was used. Results: β -Lapachone exhibited potent antimicrobial activity against laboratory strains of bacteria with MIC of 0.2 mM for S. saprophyticus and Staphylococcus aureus, and 0.04 mM for Staphylococcus epidermidis and Pseudomonas aeruginosa ATCC 27853. The inhibition of catalase enzyme was found to be the cause for its antibacterial activity. Molecular modeling predicted the binding of β -Lap at active site and heme binding site of catalase, KatA. The activity of some commercial antibiotics was enhanced in association with β -Lap. In addition, β -Lap inhibited the biofilm formation and eradicated the already formed and ultra-mature biofilms of aforesaid bacterial strains.

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Antituberculosis Activities of Lapachol and β-Lapachone in Combination with Other Drugs in Acidic pH

Cited by 4 publications

References 45 publications

Identification of Antimotilins, Novel Inhibitors of Helicobacter pylori Flagellar Motility That Inhibit Stomach Colonization in a Mouse Model

Identification of Antimotilins, Novel Inhibitors of Helicobacter pylori Flagellar Motility That Inhibit Stomach Colonization in a Mouse Model

Antibacterial and Antibiofilm Activities of β-Lapachone by Modulating the Catalase Enzyme

Antibacterial and Antibiofilm Activities of Β –Lapachone by Modulating the Catalase Enzyme

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