Anti-hepatitis C virus drug simeprevir: a promising antimicrobial agent against MRSA

Li, Yimin; She, Pengfei; Xu, Lei; Liu, Yaqian; Li, Shasha; Li, Zehao; Yang, Yifan; Li, Linhui; Hussain, Zubair; Wu, Yong

doi:10.1007/s00253-022-11878-2

Cited by 8 publications

(8 citation statements)

References 52 publications

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“…In our study, by using the above fluorescent probes, S. aureus exhibited increased permeability and membrane hyperpolarization after being treated with TAF, indicating that the bacterial cell membrane was damaged. Similar to the report by Li et al ( 24 ), the membrane potential of TAF exhibited hyperpolarization, which was different from the positive control by melittin. Moreover, previous studies have reported that the antimicrobial agents of citral, basil, white sagebrush, and sweet acacia can also hyperpolarize the bacterial membranes ( 48 , 49 ).…”

Section: Discussionsupporting

confidence: 85%

“…OD 630 nm was measured and the colony-forming unit (CFU) was counted at the particular time points of 0, 2, 4, 8, 12, and 24 h, respectively. DMSO (1%, vol/vol) was used as a control ( 24 ).…”

Section: Methodsmentioning

confidence: 99%

“…The bacterial suspension in sub-MIC (1/2 × MIC) was 1,000-fold diluted with MH broth for the next day’s MIC determination. After 15 days of passages, the CIP- and RFP-induced resistant S. aureus strains of the last passage were used to detect the cross-resistance by TAF ( 24 ).…”

Section: Methodsmentioning

confidence: 99%

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Repurposing of the antimalarial agent tafenoquine to combat MRSA

She,

Yang,

et al. 2023

mSystems

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Staphylococcus aureus is an important human pathogen that often leads to hospital-acquired and community-acquired infections. The appearance of methicillin-resistant S. aureus (MRSA) has made the treatment extremely challenging. There is an urgent need to develop new antimicrobial agents to combat MRSA infections. In this study, through high-throughput screening, we found that tafenoquine (TAF), an antimalarial agent, exhibited antimicrobial efficacy against MRSA and its highly resistant phenotypes of biofilm and persister cells. No resistant mutation emerged by consecutive sub-minimal inhibitory concentration of TAF induction. Mechanistic studies by fluorescent probes of SYTOX Green/DiSC3(5), molecular dynamic simulations, electron microscopy, and proteomic analysis revealed that TAF exerts antimicrobial activity mainly through selective bacterial cell membrane disruption. In addition, TAF exhibited an effective antimicrobial effect in a subcutaneous abscess model in vivo with a good toxicity profile. In conclusion, TAF may have the potential to be developed as a new antimicrobial agent to treat refractory MRSA infections. IMPORTANCE This study represents the first investigation into the antimicrobial effect of TAF against S. aureus and its potential mechanisms. Our data highlighted the effects of TAF against MRSA planktonic cells, biofilms, and persister cells, which is conducive to broadening the application of TAF. Through mechanistic studies, we revealed that TAF targets bacterial cell membranes. In addition, the in vivo experiments in mice demonstrated the safety and antimicrobial efficacy of TAF, suggesting that TAF could be a potential antibacterial drug candidate for the treatment of infections caused by multiple drug-resistant S. aureus .

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Section: Discussionsupporting

confidence: 85%

Section: Methodsmentioning

confidence: 99%

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Repurposing of the antimalarial agent tafenoquine to combat MRSA

She,

Yang,

et al. 2023

mSystems

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“…The bacteria cultures in the log phase were adjusted to 3 × 10 8 CFU/mL in fresh BHI broth and then cultured with 10× MIC of LP or 0.1% DMSO for 1 h. The bacteria were then fixed with 1.5 mL of 2.5% glutaraldehyde at 4 °C for 48 h. Then, the samples were observed by SEM (HITACHI, Tokyo, Japan) and TEM (HITACHI, Tokyo, Japan), respectively. 53 Membrane Proton Motive Force (PMF) Determination by DiSC3(5). DiSC3( 5) is a membrane potential probe, which reflects disruption of PMF.…”

Section: ■ Conclusionmentioning

confidence: 99%

Lusutrombopag as a Repurposing Drug in Combination with Aminoglycosides against Vancomycin-Resistant Enterococcus

She,

Li,

Yang

et al. 2024

ACS Infect. Dis.

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Due to the widespread abuse of antibiotics, drug resistance in Enterococcus has been increasing. However, the speed of antibiotic discovery cannot keep pace with the acquisition of bacterial resistance. Thus, drug repurposing is a proposed strategy to solve the crises. Lusutrombopag (LP) has been approved as a thrombopoietin receptor agonist by the Food and Drug Administration. This study demonstrated that LP exhibited significant antimicrobial activities against vancomycin-resistant Enterococcus in vitro with rare resistance occurrence. Further, LP combined with tobramycin exhibited synergistic antimicrobial effects in vitro and in vivo against Enterococcus. No in vitro or in vivo detectable toxicity was observed when using LP. Mechanism studies indicated that the disrupted proton motive force may account for LP's antimicrobial activity. In summary, these results demonstrate that LP has the previously undocumented potential to serve as an antibacterial agent against refractory infections caused by Enterococcus.

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“…W wynikach serii doświadczeń wykazano, że działanie simepreviru może polegać na zakłócaniu błon komórkowych bakterii. W tym badaniu zauważono potencjał simeprewiru jako środka przeciwdrobnoustrojowego w leczeniu zakażeń MRSA [21].…”

Section: Zakażenie Mrsaunclassified

DAA - directly acting antivirals - as a new, more efficient solution of the chronic hepatitis C treatment and theirs various application.

ABRAM¹,

Patryk

ADAMUS³

et al. 2023

J Educ Health Sport

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Introduction Cirrhosis is a condition in which the liver becomes fibrotic following damage to the liver and transforms the architecture of the organ into regenerative nodules. The disease is caused 30% by HCV infection, resulting in a risk of severe complications and death. Since the use of direct-acting antivirals ( DAAs) for the treatment of chronic HCV, sustained virological response (SVR) rates have begun to increase, even in treatment-resistant cases. Studies have also shown that DAAs may have applications in other viral diseases and even In the treatment of breast cancer. Aim of the study The purpouse of our study was to review scientific articles to show the efficiency and potential use of DAAs in the treatment of chronic HCV, and to identify possible directions for further research. Methods and materials We reviewed the English literature in the PubMed, using the key words: "simeprevir" ; "sofosbuvir" ; "velpatasvir" ; "telaprevir" ; "chronic hepatitis C". Results Studies have shown that the therapeutic regimens currently being designed with (DAAs) offer the possibility of treating almost the entire population with hepatitis C, while reducing side effects of interferon therapy such as increased AST, ALT activities, diarrhoea, vomiting, nausea and depression. They remain effective and tolerable, regardless of the stage of cirrhosis and associated serious co-morbidities. Analysis of studiem shows, that DAAs also show efficacy against other disease such as breast cancer, MRSA infections, SARS-CoV-2 or flavivirus infection. Conclusion All (DAAs) are effective in the treatment of patients with HCV, including cirrhosis. They result in significant improvements in prognosis and clinical outcomes. Promising results have been obtained in published data on the effect of DAAs against disease entities other than HCV, suggesting the rationale for future clinical trials to further the hypothesis of the increased potential of these drugs.

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Anti-hepatitis C virus drug simeprevir: a promising antimicrobial agent against MRSA

Cited by 8 publications

References 52 publications

Repurposing of the antimalarial agent tafenoquine to combat MRSA

Repurposing of the antimalarial agent tafenoquine to combat MRSA

Lusutrombopag as a Repurposing Drug in Combination with Aminoglycosides against Vancomycin-Resistant Enterococcus

DAA - directly acting antivirals - as a new, more efficient solution of the chronic hepatitis C treatment and theirs various application.

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