Antibacterial Activity of THAM Trisphenylguanide against Methicillin-Resistant Staphylococcus aureus

Weaver, Alan J.; Shepard, Joyce B.; Wilkinson, Royce A.; Watkins, Robert L.; Walton, Sarah K.; Radke, Amanda R.; Wright, Thomas J.; Awel, Milat B.; Cooper, Cyrus; Erikson, Elizabeth; Labib, Mohamed E.; Voyich, Jovanka M.; Teintze, Martin

doi:10.1371/journal.pone.0097742

Cited by 14 publications

(18 citation statements)

References 27 publications

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“…This, along with the relatively short window of therapeutic application for antibiotics attributed to the rapid emergence of drug resistance, has, at least until recently, resulted in a waning interest in antibiotic discovery among pharmaceutical companies [ 10 ]. In this environment, “repurposing” (defined as investigating new uses for existing drugs) has gained renewed interest, as reflected by several recent studies [ 11 – 13 ].…”

Section: Introductionmentioning

confidence: 99%

Repurposing Salicylanilide Anthelmintic Drugs to Combat Drug Resistant Staphylococcus aureus

et al. 2015

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Staphylococcus aureus is a Gram-positive bacterium that has become the leading cause of hospital acquired infections in the US. Repurposing Food and Drug Administration (FDA) approved drugs for antimicrobial therapy involves lower risks and costs compared to de novo development of novel antimicrobial agents. In this study, we examined the antimicrobial properties of two commercially available anthelmintic drugs. The FDA approved drug niclosamide and the veterinary drug oxyclozanide displayed strong in vivo and in vitro activity against methicillin resistant S. aureus (minimum inhibitory concentration (MIC): 0.125 and 0.5 μg/ml respectively; minimum effective concentration: ≤ 0.78 μg/ml for both drugs). The two drugs were also effective against another Gram-positive bacteria Enterococcus faecium (MIC 0.25 and 2 μg/ml respectively), but not against the Gram-negative species Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa and Enterobacter aerogenes. The in vitro antimicrobial activity of niclosamide and oxyclozanide were determined against methicillin, vancomycin, linezolid or daptomycin resistant S. aureus clinical isolates, with MICs at 0.0625-0.5 and 0.125-2 μg/ml for niclosamide and oxyclozanide respectively. A time-kill study demonstrated that niclosamide is bacteriostatic, whereas oxyclozanide is bactericidal. Interestingly, oxyclozanide permeabilized the bacterial membrane but neither of the anthelmintic drugs exhibited demonstrable toxicity to sheep erythrocytes. Oxyclozanide was non-toxic to HepG2 human liver carcinoma cells within the range of its in vitro MICs but niclosamide displayed toxicity even at low concentrations. These data show that the salicylanilide anthelmintic drugs niclosamide and oxyclozanide are suitable candidates for mechanism of action studies and further clinical evaluation for treatment of staphylococcal infections.

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Section: Introductionmentioning

confidence: 99%

Repurposing Salicylanilide Anthelmintic Drugs to Combat Drug Resistant Staphylococcus aureus

et al. 2015

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“…oris, the CFU reduction did not achieve a 3 log10 units difference, which is considered a significant antimicrobial activity. 28,29 After 3 days of infection no strong invasion of bacteria to the root dentine walls can be expected. Concerning the five different used single strains (E. faecalis, F. nucleatum, A. oris, S. gordonii, and C. albicans) we consistently found a significant reduction of CFUs of 1-2 log10 units compared with the negative control, but there was in most cases no difference to manual dynamic irrigation with NaCl (Fig.…”

Section: Endodontic Disinfection With Er:yag Laser Discussionmentioning

confidence: 99%

In VitroEffect of Er:YAG Laser on Different Single and Mixed Microorganisms Being Associated with Endodontic Infections

Henninger

Berto

Eick

et al. 2019

Photobiomodulation, Photomedicine, and Laser Surgery

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Objective: The purpose of this in vitro study was to evaluate the antimicrobial effect of activated irrigation with different modes of erbium-doped yttrium aluminum garnet (Er:YAG) laser application on microorganisms related to secondary endodontic infection. Background: Er:YAG laser has been recommended as an adjuvant tool for root canal disinfection during endodontic treatment. Materials and methods: Laser-activated irrigation (LAI) with 300 or 600 lm tips were tested with or without intermittent irrigation with 0.9% sodium chloride (NaCl) solution against different microorganisms (five single strains and dual species (Streptococcus gordonii combined with Actinomyces oris or Fusobacterium nucleatum) in root canals after 3 days of incubation. In a 21-day infection model, LAI was used together with intermittent rinsing with sodium hypochlorite (NaOCl) against the dual-species mixtures; here the incidence of microbial regrowth after up to 7 days was monitored. Results: In the 3-day root infection model, LAI protocols did not show any significant reduction of the microbial load when compared with manual irrigation with saline solution. In the 21-day infection, S. gordonii combined with A. oris were not detectable anymore after applying the LAI protocol with a 600 lm tip (30 mJ/ 10 pps) up to 7 days after treatment. Conclusions: Application of LAI with a 600 lm tip by using an Er:YAG laser might be advantageous in treatment of endodontic infections.

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“…Since antibiotics were introduced into clinical practice, bacterial pathogens have developed resistance that might reduce their effectiveness. Moreover, with opportunistic pathogens innate resistance to antibiotics has become particularly problems arising in hospital environments [22] . Thus, the research of new molecules may provide an alternative for this scenario.…”

Section: Discussionmentioning

confidence: 99%

Antimicrobial activity of the toxin VdTX-I from the spider Vitalius dubius (Araneae, Theraphosidae)

Sutti

Rosa

Wunderlich

et al. 2015

Biochemistry and Biophysics Reports

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BackgroundCurrently there is an urgent need to develop new classes of antimicrobial agents with different mechanisms of action from conventionally antibiotics used for the control of pathogenic microorganisms. The acylpolyamine called VdTX-I was isolated from the venom of the tarantula Vitalius dubius, and first described with activity as an antagonist of nicotinic cholinergic receptors. The main objective of this study was to investigate the antimicrobial activity found in the venom of the spider, with emphasis on the toxin VdTX-I.MethodsAntimicrobial assays were performed in 96 well plates culture against 14 micro-organisms (fungi, yeasts and bacteria), which were tested concentrations from 0.19 to 100 μM of VdTX-I. After qualitative analysis, dose-response curve assays were performed in bacterial kill curve using MTT reagent and hemolytic assay.ResultsThe antimicrobial activity of the VdTX-I toxin was observed in 12 tested species of Candida, Trichosporiun, Staphylococcus and Micrococcus. The toxicity had a dose-response at 3.12 µM – 100 μM in Candida albicans, Candida guillermondii, Micrococcus luteus and Escherichia coli. VdTX-I took about 5 min to inhibit bacterial growth, which was faster than streptomycin. The toxin showed no hemolytic activity between 0.19 and 100 μM. At 2.5 µg/mL of toxin it was observed no growth inhibition against a mammalian cell lineage.ConclusionsThe VdTX-I toxin has a significant antimicrobial activity, with broad spectrum, and is experimentally inert to mammalian blood cells.General SignificanceThis paper explores the antimicrobial potential of the spider toxin VdTX-I, which can provide a new model to design new antimicrobial drugs.

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Antibacterial Activity of THAM Trisphenylguanide against Methicillin-Resistant Staphylococcus aureus

Cited by 14 publications

References 27 publications

Repurposing Salicylanilide Anthelmintic Drugs to Combat Drug Resistant Staphylococcus aureus

Repurposing Salicylanilide Anthelmintic Drugs to Combat Drug Resistant Staphylococcus aureus

In VitroEffect of Er:YAG Laser on Different Single and Mixed Microorganisms Being Associated with Endodontic Infections

Antimicrobial activity of the toxin VdTX-I from the spider Vitalius dubius (Araneae, Theraphosidae)

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