scholarly journals Antimicrobial and Antifungal Activities of Terpene-Derived Palladium Complexes

Antibiotics ◽  
2020 ◽  
Vol 9 (5) ◽  
pp. 277 ◽  
Author(s):  
Olga Zalevskaya ◽  
Yana Gur’eva ◽  
Aleksandr Kutchin ◽  
Karl A. Hansford

In an era of multidrug-resistant bacterial infections overshadowed by a lack of innovation in the antimicrobial drug development pipeline, there has been a resurgence in multidisciplinary approaches aimed at tackling this global health problem. One such approach is to use metal complexes as a framework for new antimicrobials. Indeed, in this context, bismuth-, silver- and gold-derived compounds in particular have displayed demonstrable antimicrobial activity. In this work, we discuss the antimicrobial and antifungal activities of terpene-derived chiral palladium complexes against Staphylococcus aureus, Pseudomonas aeruginosa, Klebsiella pneumoniae, Acinetobacter baumannii, Escherichia coli, Candida albicans, and Cryptococcus neoformans. It was established that all studied coordination compounds of palladium were highly active antifungal drugs. In contrast, the subset of palladacycles possessing a palladium–carbon bond were only active against the Gram-positive bacterium Staphylococcus aureus. All compounds were inactive against the Gram-negative bacteria tested.

2011 ◽  
Vol 56 (3) ◽  
pp. 1584-1587 ◽  
Author(s):  
Johanne Blais ◽  
Stacey R. Lewis ◽  
Kevin M. Krause ◽  
Bret M. Benton

ABSTRACTTD-1792 is a new multivalent glycopeptide-cephalosporin antibiotic with potent activity against Gram-positive bacteria. Thein vitroactivity of TD-1792 was tested against 527Staphylococcus aureusisolates, including multidrug-resistant isolates. TD-1792 was highly active against methicillin-susceptibleS. aureus(MIC90, 0.015 μg/ml), methicillin-resistantS. aureus, and heterogeneous vancomycin-intermediateS. aureus(MIC90, 0.03 μg/ml). Time-kill studies demonstrated the potent bactericidal activity of TD-1792 at concentrations of ≤0.12 μg/ml. A postantibiotic effect of >2 h was observed after exposure to TD-1792.


Processes ◽  
2020 ◽  
Vol 8 (12) ◽  
pp. 1587
Author(s):  
Feng Wang ◽  
Xiaohang Liu ◽  
Zhengyu Deng ◽  
Yao Zhang ◽  
Xinyu Ji ◽  
...  

With the increasing spread of multidrug-resistant bacterial pathogens, it is of great importance to develop alternatives to conventional antibiotics. Here, we report the generation of a chimeric phage lysin, MLTphg, which was assembled by joining the lysins derived from Meiothermus bacteriophage MMP7 and Thermus bacteriophage TSP4 with a flexible linker via chimeolysin engineering. As a potential antimicrobial agent, MLTphg can be obtained by overproduction in Escherichia coli BL21(DE3) cells and the following Ni-affinity chromatography. Finally, we recovered about 40 ± 1.9 mg of MLTphg from 1 L of the host E. coli BL21(DE3) culture. The purified MLTphg showed peak activity against Staphylococcus aureus ATCC6538 between 35 and 40 °C, and maintained approximately 44.5 ± 2.1% activity at room temperature (25 °C). Moreover, as a produced chimera, it exhibited considerably improved bactericidal activity against Staphylococcus aureus (2.9 ± 0.1 log10 reduction was observed upon 40 nM MLTphg treatment at 37 °C for 30 min) and also a group of antibiotic-resistant bacteria compared to its parental lysins, TSPphg and MMPphg. In the current age of growing antibiotic resistance, our results provide an engineering basis for developing phage lysins as novel antimicrobial agents and shed light on bacteriophage-based strategies to tackle bacterial infections.


2019 ◽  
Vol 63 (4) ◽  
Author(s):  
Susanne Paukner ◽  
Steven P. Gelone ◽  
S. J. Ryan Arends ◽  
Robert K. Flamm ◽  
Helio S. Sader

ABSTRACTLefamulin, the first semisynthetic pleuromutilin antibacterial for intravenous and oral treatment of community-acquired bacterial pneumonia (CABP), and comparators were evaluated forin vitroactivity against a global collection of pathogens commonly causing CABP (n= 8595) from the 2015 and 2016 SENTRY Antimicrobial Surveillance Program. Lefamulin was highly active against the pathogensStreptococcus pneumoniae, including multidrug-resistant and extensively drug-resistant strains (MIC50/90for total and resistant subsets, 0.06/0.12 μg/ml; 100% inhibited at ≤1 μg/ml),Staphylococcus aureus, including methicillin-resistantStaphylococcus aureus(MRSA; both MIC50/90, 0.06/0.12 μg/ml; 99.8% and 99.6% inhibited at ≤1 μg/ml, respectively),Haemophilus influenzae(MIC50/90, 0.5/1 μg/ml; 93.8% inhibited at ≤1 μg/ml), andMoraxella catarrhalis(MIC50/90, 0.06/0.12 μg/ml; 100% inhibited at ≤0.25 μg/ml), and its activity was unaffected by resistance to other antibacterial classes.


2018 ◽  
Vol 69 (4) ◽  
pp. 915-920
Author(s):  
Petronela Cristina Chiriac ◽  
Vladimir Poroch ◽  
Alina Mihaela Pascu ◽  
Mircea Daniel Hogea ◽  
Ileana Antohe ◽  
...  

The antibiotic resistance of microorganisms involved in pediatric infections represents a significant cause of healthcare-associated infections (HAIs), and is also a matter of management, requiring specific intervention. The aim of the study was to evaluate the efficacy of some antibiotic molecules on pathogens isolated from patients admitted in a pediatric hospital. We carried out a descriptive study on a group of 411 patients admitted to the Sf. MariaClinical Emergency Hospital for Children Iasi, between January 1st and March 31st, 2016. Bacterial infections were most prevalent in the age group of 0-1 year (54.98% of the total isolates). Most affected by multidrug-resistant bacterial infections services were: general pediatrics (24.08% of the total isolates), then the intensive care unit (19.95%), surgical wards (14.84%), and acute therapy (11.43%). The germs were isolated from pathological samples: most often pus (23.85%), hypo-pharyngeal aspiration (21.65%), conjunctival secretion (12.42%), and ear secretion (9.48%). Penicillin G and oxacillin were inefficient in 30.26% of the Staphylococcus aureus strains, while erythromycin in 18.42%. Antibiotic resistance of Streptococcus pneumoniae was observed for penicillin G in 7.14% of the strains, while for erythromycin in 13.09%. Klebsiella pneumoniae strains were resistant to amoxicillin + clavulanic acid in 35.85% of the cases, and to cefuroxime, ceftazidime, ceftriaxone, cefepime in 33.96%. Our study highlighted that Staphylococcus aureus was resistant to penicillin G and oxacillin in more than one-third of the isolates, Streptococcus pneumoniae was resistant to penicillin G and erythromycin, and Klebsiella pneumoniae to amoxicillin + clavulanic acid and 1st, 2nd and 3rd generation cephalosporins. Continuing antibioresistance monitoring is crucial in order to promote appropriate guidelines in antibiotic prescription, which could result in decreasing HAIs� rates.


2015 ◽  
Vol 59 (7) ◽  
pp. 4308-4311 ◽  
Author(s):  
Frédéric Lamoth ◽  
Barbara D. Alexander

ABSTRACTThe limited armamentarium of active and oral antifungal drugs against emerging non-Aspergillusmolds is of particular concern. Current antifungal agents and the new orally available beta-1,3-d-glucan synthase inhibitor SCY-078 were testedin vitroagainst 135 clinical non-Aspergillusmold isolates. Akin to echinocandins, SCY-078 showed no or poor activity againstMucoromycotinaandFusariumspp. However, SCY-078 was highly active againstPaecilomyces variotiiand was the only compound displaying some activity against notoriously panresistantScedosporium prolificans.


2006 ◽  
Vol 61 (1-2) ◽  
pp. 31-34 ◽  
Author(s):  
Artur Smania ◽  
Elza F. A. Smania ◽  
Franco Delle Monache ◽  
Moacir G. Pizzolatti ◽  
Giuliano Delle Monache

Abstract Applanoxidic acids and sterols, isolated from Ganoderma spp., were acetylated and/or methylated. The antibacterial activity against Escherichia coli and Staphylococcus aureus and the antifungal activity against Candida albicans and Trichophyton mentagrophytes of the derivatives were investigated by a microdilution method, and compared with those of the natural products. Both natural and modified compounds exhibited comparable antibacterial and antifungal activities in a range of 1.0 to > 2.0 mg/ml minimal inhibitory concentration


2017 ◽  
Vol 12 (11) ◽  
pp. 1934578X1701201 ◽  
Author(s):  
Jung-Eun Kim ◽  
Goo Yoon ◽  
Jung-Hyun Shim ◽  
Seung-Sik Cho

The aim of this study was to evaluate the antibacterial activity of the licochalcones A (1) and E (2) against drug resistant strains of clinical origin. The results indicate that the licochalcones had a broad inhibitory activity against tested bacteria. Compared to vancomycin and teicoplanin, these compounds provided weaker activity against non-MDR Staphylococcus aureus and Enterococcus but broader activity against MRSA and VRE strains. The results provide promising baseline information for the potential use of 1 and 2 from Glycyrrhiza inflata in the treatment of drug resistant bacterial infections.


Antibiotics ◽  
2022 ◽  
Vol 11 (1) ◽  
pp. 65
Author(s):  
Hang Thi Nguyen ◽  
Henrietta Venter ◽  
Lucy Woolford ◽  
Kelly Young ◽  
Adam McCluskey ◽  
...  

In this study, we investigated the potential of an analogue of robenidine (NCL179) to expand its chemical diversity for the treatment of multidrug-resistant (MDR) bacterial infections. We show that NCL179 exhibits potent bactericidal activity, returning minimum inhibitory concentration/minimum bactericidal concentrations (MICs/MBCs) of 1–2 µg/mL against methicillin-resistant Staphylococcus aureus, MICs/MBCs of 1–2 µg/mL against methicillin-resistant S. pseudintermedius and MICs/MBCs of 2–4 µg/mL against vancomycin-resistant enterococci. NCL179 showed synergistic activity against clinical isolates and reference strains of Acinetobacter baumannii, Escherichia coli, Klebsiella pneumoniae and Pseudomonas aeruginosa in the presence of sub-inhibitory concentrations of colistin, whereas NCL179 alone had no activity. Mice given oral NCL179 at 10 mg/kg and 50 mg/kg (4 × doses, 4 h apart) showed no adverse clinical effects and no observable histological effects in any of the organs examined. In a bioluminescent S. aureus sepsis challenge model, mice that received four oral doses of NCL179 at 50 mg/kg at 4 h intervals exhibited significantly reduced bacterial loads, longer survival times and higher overall survival rates than the vehicle-only treated mice. These results support NCL179 as a valid candidate for further development to treat MDR bacterial infections as a stand-alone antibiotic or in combination with existing antibiotic classes.


Author(s):  
A. Yu. Borisenko ◽  
◽  
Yu. P. Dzhioev ◽  
L. A. Stepanenko ◽  
Yu. M. Zemlyanskaya ◽  
...  

In the modern world, infections caused by multidrug-resistant (MDR) bacteria have become carriers of global threats to human health. Today these pathogenic bacteria have come to be referred to as "superbugs" and their number and aggressiveness is growing. This group of "superbugs" also includes Staphylococcus aureus. It is capable of infecting almost any tissue in the human body. Therefore, it became necessary to find alternative antibiotic methods of treating bacterial infections. The use of bacteriophages is again among them. We propose a new approach in the search for strain-specific (target) phages through the structures of the CRISPR/Cas-systems of bacteria. As is known, CRISPR/Cas systems are the most ancient system of "adaptive immunity" in bacteria. This system makes bacteria resistant to phages and plasmids. This approach is based on the use of methods of structural genomics and software bioinformatics modeling. Using them, an algorithm was developed to search for the structures of CRISPR/Cas systems in bacterial genomes presented in the NCBI databases and screening through their CRISPR cassettes of phages with which a particular strain could meet. The design of the developed algorithm was tested on the genome of methicillin-resistant S. aureus strain (ST228-MRSA-I) from the GenBank database. The results of the search for loci and structures of the CRISPR/Cas system in the genome of this strain showed that the identified system belongs to type III-A. It was found that the cas genes and the CRISPR cassette are located at a distance from each other and between them are located several genes that perform other functions in the genome of the S. aureus strain. It was shown that the structures of spacers in the detected CRISPR cassette are identical to protospacers of phages, the hosts of which are bacteria of the following genera – Staphylococcus, Mycobacterium, Streptococcus, Bacillus, Gordonia, Arthrobacter, Streptomyces. Thus, it can be stated that the developed algorithm of software methods for searching for loci of CRISPR/Cas systems and screening for phages makes it possible to type both the system itself and through its spacers to detect and identify phage races with which a particular bacterial strain could meet. The degree of resistance of a particular bacterial strain to specific phages is also determined, which in the long term should ensure the effectiveness of targeted phage therapy for infections caused by pathogenic bacteria, including "superbugs".


Author(s):  
Logan Gildea ◽  
Joseph Ayariga ◽  
James Abugri ◽  
Robert Villafane

The emergence of multidrug-resistant bacterial strains, especially in the clinical setting, has renewed interest in alternative treatment methods. The utilization of prokaryotic viruses in phage therapy has demonstrated potential as a novel treatment method against multidrug-resistant bacterial infections. As the post-antibiotic era quickly approaches, the development and standardization of phage therapy is critically relevant to public health. This review serves to highlight the development of phage therapy against methicillin-resistant Staphylococcus aureus (MRSA), an antibiotic-resistant bacterial strain responsible for severe clinical infections.


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