An analog of the host-defense peptide hymenochirin-1B with potent broad-spectrum activity against multidrug-resistant bacteria and immunomodulatory properties

Peptides ◽  
2013 ◽  
Vol 50 ◽  
pp. 153-159 ◽  
Author(s):  
Milena Mechkarska ◽  
Manju Prajeep ◽  
Gordana D. Radosavljevic ◽  
Ivan P. Jovanovic ◽  
Amna Al Baloushi ◽  
...  
Keyword(s):  
Host Defense ◽  
Broad Spectrum ◽  
Multidrug Resistant ◽  
Resistant Bacteria ◽  
Multidrug Resistant Bacteria ◽  
Host Defense Peptide ◽  
Spectrum Activity ◽  
Immunomodulatory Properties ◽  
Broad Spectrum Activity

Alkoxyphenylthiazoles with broad-spectrum activity against multidrug-resistant gram-positive bacterial pathogens

2018 ◽  
Vol 152 ◽  
pp. 318-328 ◽  
Author(s):  
Moustafa ElAwamy ◽  
Haroon Mohammad ◽  
Abdelrahman Hussien ◽  
Nader S. Abutaleb ◽  
Mohamed Hagras ◽  
...  
Keyword(s):  
Broad Spectrum ◽  
Bacterial Pathogens ◽  
Multidrug Resistant ◽  
Gram Positive ◽  
Spectrum Activity ◽  
Broad Spectrum Activity

A Light-Activated Nanotherapeutic with Broad-Spectrum Bacterial Recognition to Eliminate Drug-Resistant Pathogens

2021 ◽  
Author(s):  
Xiaosong Wei ◽  
Yingchao Gao ◽  
Yuqing Hu ◽  
Yufei Zhang ◽  
Xinge Zhang
Keyword(s):  
Human Health ◽  
Broad Spectrum ◽  
Multidrug Resistant ◽  
Morbidity And Mortality ◽  
Resistant Bacteria ◽  
Drug Resistant ◽  
Multidrug Resistant Bacteria ◽  
Drug Resistant Bacteria

Obstinate infections caused by drug-resistant bacteria severely threaten human health. And the emergence of multidrug-resistant bacteria increases the morbidity and mortality of patients, innovative or alternative therapeutics thus necessitates the...

Broad-spectrum activity of a novel antibiotic peptide against multidrug-resistant veterinary isolates

2013 ◽  
Vol 198 (2) ◽  
pp. 534-537 ◽  
Author(s):  
Clotilde Silvia Cabassi ◽  
Simone Taddei ◽  
Sandro Cavirani ◽  
Maria Cristina Baroni ◽  
Paolo Sansoni ◽  
...  
Keyword(s):  
Broad Spectrum ◽  
Multidrug Resistant ◽  
Spectrum Activity ◽  
Antibiotic Peptide ◽  
Broad Spectrum Activity

scholarly journals 1370. Cefepime/VNRX-5133 Broad-Spectrum Activity Is Maintained Against Emerging KPC- and PDC-Variants in Multidrug-Resistant K. pneumoniae and P. aeruginosa

2018 ◽  
Vol 5 (suppl_1) ◽  
pp. S419-S420 ◽  
Author(s):  
Denis Daigle ◽  
Jodie Hamrick ◽  
Cassandra Chatwin ◽  
Natalia Kurepina ◽  
Barry N Kreiswirth ◽  
...  
Keyword(s):  
Broad Spectrum ◽  
Susceptibility Testing ◽  
Multidrug Resistant ◽  
Clinical Development ◽  
Clinical Isolates ◽  
Research Support ◽  
Class A ◽  
Highly Active ◽  
Spectrum Activity ◽  
Broad Spectrum Activity

Abstract Background VNRX-5133 is a cyclic boronate β-lactamase inhibitor (BLI) currently in clinical development with cefepime to treat multidrug-resistant (MDR) infections caused by ESBL- and carbapenemase-producing Enterobacteriaceae (ENT) and P. aeruginosa (PSA). VNRX-5133 has direct inhibitory activity against serine-active site β-lactamases (Ser-BL) and emerging VIM/NDM metallo-β-lactamases (MBL). We show herein that cefepime/VNRX-5133 is highly active against MDR-K. pneumoniae and P. aeruginosa clinical isolates producing BL-variants evolved during therapy that compromise activity of ceftazidime/avibactam and ceftolozane/tazobactam. Methods Susceptibility testing was performed according to CLSI methods with cefepime, ceftolozane, and ceftazidime alone or in combination with VNRX-5133, avibactam, or tazobactam, respectively, fixed at 4 mg/L. Five clinical isolates of K. pneumoniae producing KPC variants impacting ceftazidime/avibactam and five clinical isolates of P. aeruginosa producing Pseudomonas-derived cephalosporinase variants impacting ceftolozane/tazobactam activity were collected in 2016 and 2017, respectively, from United States and Spanish hospitals. All other clinical isolates of Enterobacteriaceae and P. aeruginosa (n = 40) were collected in 2016. Results Cefepime/VNRX-5133 was highly active against five ceftazidime/avibactam-resistant K. pneumoniae clinical isolates producing KPC variants with MIC ranging from 0.5 to 4 mg/L relative to ceftazidime/avibactam MIC range of 16 to >128 mg/L. Cefepime/VNRX-5133 was also active against all five clinical isolates of ceftolozane/tazobactam-resistant P. aeruginosa, where 4/5 isolates had MIC of 4–8 mg/L relative to ceftolozane/tazobactam MIC range of 32–128 mg/L. The elevated cefepime/VNRX-5133 MIC (16 mg/L) in the remaining P. aeruginosa isolate was not due to the PDC-221 variant, as an engineered strain of P. aeruginosa producing this enzyme had a cefepime/VNRX-5133 MIC of 1 mg/L. Conclusion VNRX-5133 is a potent BLI possessing a unique broad spectrum of activity, including Class A, C, and D Ser-BLs, clinically evolving variants of Ser-BLs (e.g., KPC, PDC) and emerging VIM/NDM-type MBLs. Cefepime/VNRX-5133 is highly active against emerging multidrug-resistant Enterobacteriaceae and P. aeruginosa. Disclosures D. Daigle, VenatoRx Pharmaceuticals Inc.: Employee and Shareholder, Salary. J. Hamrick, VenatoRx Pharmaceuticals Inc.: Employee, Salary. C. Chatwin, VenatoRx Pharmaceuticals Inc.: Employee, Salary. N. Kurepina, VenatoRx Pharmaceuticals Inc.: Research Contractor, Research support. B. N. Kreiswirth, VenatoRx Pharmaceuticals Inc.: Research Contractor, Research support. R. K. Shields, VenatoRx Pharmaceuticals Inc.: Research Contractor, Research support. A. Oliver, VenatoRx Pharmaceuticals Inc.: Research Contractor, Research support. C. J. Clancy, VenatoRx Pharmaceuticals Inc.: Research Contractor, Research support. M. H. Nguyen, VenatoRx Pharmaceuticals Inc.: Research Contractor, Research support. D. Pevear, VenatoRx Pharmaceuticals Inc.: Employee, Salary. L. Xerri, VenatoRx Pharmaceuticals Inc.: Employee and Shareholder, Salary.

scholarly journals Engineering of Antimicrobial Surfaces by Using Temporin Analogs to Tune the Biocidal/antiadhesive Effect

Molecules ◽  
2019 ◽  
Vol 24 (4) ◽  
pp. 814 ◽  
Author(s):  
Pierre-Carl Oger ◽  
Christophe Piesse ◽  
Ali Ladram ◽  
Vincent Humblot
Keyword(s):  
Broad Spectrum ◽  
Bacterial Resistance ◽  
Antibacterial Properties ◽  
Covalent Immobilization ◽  
Resistant Bacteria ◽  
Gold Surfaces ◽  
Cationic Antimicrobial Peptide ◽  
Bacterial Membranes ◽  
Spectrum Activity ◽  
Broad Spectrum Activity

Proliferation of resistant bacteria on biomaterials is a major problem leading to nosocomial infections. Due to their broad-spectrum activity and their ability to disrupt bacterial membranes through a rapid membranolytic mechanism, antimicrobial peptides (AMPs) are less susceptible to the development of bacterial resistance and therefore represent good candidates for surface coating strategies to prevent biofilm formation. In this study, we report on the covalent immobilization of temporin-SHa, a small hydrophobic and low cationic antimicrobial peptide exhibiting broad-spectrum activity, and (SHa) analogs on modified gold surfaces. Several analogs derived from SHa with either a carboxamidated ([K3]SHa, d-[K3]SHa) or a carboxylated C-terminus ([K3]SHa-COOH) were used to achieve peptide grafting on gold surfaces modified by a thiolated self-assembled monolayer (SAM). Surface functionalization was characterized by polarization modulation infrared reflection absorption spectroscopy (PM-RAIRS) and X-ray photoemission spectroscopy (XPS). The antibacterial properties of the temporin-functionalized surfaces were tested against the Gram-positive Listeria ivanovii. Direct visualization of the peptide effects on the bacterial membrane was investigated by scanning electron microscopy equipped with a field emission gun (SEM-FEG). All active temporin analogs were successfully grafted and display significant antibacterial activity (from 80 to 90% killing efficiency) in addition to a 2-fold decrease of bacterial adhesion when all d-SHa analogs were used.

scholarly journals Tigecycline: a review of the literature

2006 ◽  
Vol 7 (4) ◽  
pp. 211-222
Author(s):  
Mario Venditti ◽  
Maria Elena Pompeo ◽  
Flavia Fabi
Keyword(s):  
Antimicrobial Agent ◽  
Broad Spectrum ◽  
Bacterial Infections ◽  
Bacterial Resistance ◽  
Multidrug Resistant ◽  
Resistance Mechanisms ◽  
Resistant Bacteria ◽  
Antibiotic Administration ◽  
Spectrum Activity

Tigecycline is a new first-in-class glycylcycline antimicrobial agent with expanded broad-spectrum activity. It was developed to overcome the two key resistance mechanisms, efflux pumps and ribosomal protection, that limit the use of tetracycline. The spectrum of activity extends to clinically relevant susceptible and multidrug resistant bacteria, as methicillin resistant Staphylococcus aureus (MRSA), Streptococcus pneumoniae, vancomycin resistant Enterococci, Acinetobacter spp, Acinetobacter baumannii and Enterobacteriaceae, including extended-spectrum β-lactamase-producing strains (ESBLs). Tigecycline has been introduced into clinical practice as part of the effort to combat the growing problem of bacterial resistance to anti-infective therapy: tigecycline could replace some broad-spectrum agents for approved indications reducing the selective pressure provided by antibiotic administration. The expanded in vitro activity against a broad range of bacteria, including resistant pathogens, of tigecycline suggest that this novel antimicrobial agent should offer clinicians an option for the treatment of patients with serious bacterial infections.

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