scholarly journals Indole-containing arene-ruthenium complexes with broad spectrum activity against antibiotic-resistant bacteria

2021 ◽  
pp. 100099
Author(s):  
Victoria C. Nolan ◽  
Laia Rafols ◽  
James Harrison ◽  
Joan J. Soldevila-Barreda ◽  
Marialuisa Crosatti ◽  
...  
Keyword(s):  
Broad Spectrum ◽  
Ruthenium Complexes ◽  
Resistant Bacteria ◽  
Antibiotic Resistant Bacteria ◽  
Antibiotic Resistant ◽  
Spectrum Activity ◽  
Broad Spectrum Activity

scholarly journals A Degradation Product from Hydrolysate of Imipenem with Imis Broad-Spectrum Inhibits Metallo-β-Lactamases

2020 ◽  
Vol 13 (10) ◽  
Author(s):  
Ying Ge ◽  
Li-Wei Xu ◽  
Jian-Bin Zhen ◽  
Cheng Chen ◽  
Miao Lv ◽  
...  
Keyword(s):  
Broad Spectrum ◽  
Degradation Product ◽  
Substrate Inhibition ◽  
Resistant Bacteria ◽  
Drug Resistant ◽  
Antibiotic Resistant Bacteria ◽  
Antibiotic Resistant ◽  
Leaving Group ◽  
Ic50 Values ◽  
Hydrolysis Of

Background: Infections caused by metallo-β-lactamases (MβLs)-producing antibiotic-resistant bacteria pose a severe threat to public health. The synergistic use of current antibiotics in combination with MβL inhibitors is a promising therapeutic mode against these antibiotic-resistant bacteria. Objectives: The study aimed to probe the inhibition of MβLs and obtain the active component, P1, in the degradation product after imipenem was hydrolyzed by ImiS. Methods: The hydrolysis of two carbapenems with MβL ImiS was monitored by UV-Vis in real-time, and the degradation product from the leaving group produced after imipenem was hydrolyzed (but not for faropenem) was purified by HPLC to give one component, P1. Results: Kinetic assays revealed that P1 exhibited a broad-spectrum inhibition against VIM-2, NDM-1, ImiS, and L1, from three sub-classes of MβLs, with IC50 values of 8 - 32, 13.8 - 29.3, and 14.2 - 19.2 µM, using imipenem, cefazolin, and nitrocefin as substrates, respectively. Also, P1 showed synergistic antibacterial efficacy against drug-resistant Escherichia coli producing VIM-2, NDM-1, ImiS, and L1, in combination with antibiotics, restoring 16 to 32-fold and 32 to 128-fold efficacies of imipenem and cefazolin, respectively. Spectroscopic and Ellman's reagent analyses suggested that P1, a mercaptoethyl-form imidamide, is a mechanism-based inhibitor, while faropenem has no substrate inhibition, due to the lack of a leaving group. Conclusions: This work reveals that the hydrolysate of imipenem, a carbapenem with a good leaving group, can be used in screening for broad-spectrum inhibitors of MβLs.

scholarly journals Bacteriocins as a new generation of antimicrobials: toxicity aspects and regulations

2020 ◽  
Author(s):  
Samira Soltani ◽  
Riadh Hammami ◽  
Paul D Cotter ◽  
Sylvie Rebuffat ◽  
Laila Ben Said ◽  
...  
Keyword(s):  
Regulatory Agencies ◽  
Resistant Bacteria ◽  
Antibiotic Resistant Bacteria ◽  
Food Preservatives ◽  
Food Preservative ◽  
Antibiotic Resistant ◽  
Spectrum Activity ◽  
Recent Trends ◽  
Global Threat ◽  
New Generation

ABSTRACT In recent decades, bacteriocins have received substantial attention as antimicrobial compounds. Although bacteriocins have been predominantly exploited as food preservatives, they are now receiving increased attention as potential clinical antimicrobials and as possible immune-modulating agents. Infections caused by antibiotic-resistant bacteria have been declared as a global threat to public health. Bacteriocins represent a potential solution to this worldwide threat due to their broad- or narrow-spectrum activity against antibiotic-resistant bacteria. Notably, despite their role in food safety as natural alternatives to chemical preservatives, nisin remains the only bacteriocin legally approved by regulatory agencies as a food preservative. Moreover, insufficient data on the safety and toxicity of bacteriocins represent a barrier against the more widespread use of bacteriocins by the food and medical industry. Here, we focus on the most recent trends relating to the application of bacteriocins, their toxicity and impacts.

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.

Ultrastable radical-doped coordination compounds with antimicrobial activity against antibiotic-resistant bacteria

2020 ◽  
Vol 56 (92) ◽  
pp. 14353-14356
Author(s):  
Hua Ke ◽  
Fen Hu ◽  
Lingyi Meng ◽  
Qi-Hua Chen ◽  
Qian-Sheng Lai ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Broad Spectrum ◽  
Coordination Compounds ◽  
Lone Pair ◽  
Resistant Bacteria ◽  
Drug Resistant ◽  
Antibiotic Resistant Bacteria ◽  
Antibiotic Resistant ◽  
Π Interactions ◽  
Drug Resistant Bacteria

Radical-doped coordination compounds—generated as a result of lone pair–π interactions and having a long-lived charge-separated state—display photochromism and broad-spectrum antimicrobial activity, even against multi-drug-resistant bacteria.

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