Antibiotic activity and target discovery of three-membered natural product-derived heterocycles in pathogenic bacteria

2012 ◽  
Vol 3 (6) ◽  
pp. 2035 ◽  
Author(s):  
Maximilian Pitscheider ◽  
Nina Mäusbacher ◽  
Stephan A. Sieber
Keyword(s):  
Natural Product ◽  
Pathogenic Bacteria ◽  
Antibiotic Activity ◽  
Target Discovery

scholarly journals ASSESSMENT ON ANTIMICROBIAL PROPERTIES OF SURFACTIN FROM BACILLUS SUBTILIS ON PROTOPLASTS AND SPHEROPLASTS OF PATHOGENIC BACTERIA

2016 ◽  
Vol 9 (1) ◽  
pp. 67
Author(s):  
B. Chitra ◽  
A. Benno Susai Vijayakumar
Keyword(s):  
Bacillus Subtilis ◽  
Pathogenic Bacteria ◽  
Inhibitory Concentration ◽  
Antimicrobial Properties ◽  
Polluted Soil ◽  
Antibiotic Activity ◽  
Lytic Activity ◽  
Haemolytic Activity ◽  
Pathogenic Microorganisms ◽  
Clear Zone

Objective: The aim of this paper is to assessment on antimicrobial properties of surfactin from Bacillus subtilis on protoplasts and spheroplasts of pathogenic bacteria.Methods: Bacillus sp were isolated from the polluted soil samples and these isolates were screened for biosurfactin activity using haemolytic activity. The biosurfactant was also studied for their antibiotic activity and the minimum inhibitory concentration was determined by testing the effect of surfactin on the pathogenic microorganisms. The lytic activity of surfactant was also tested on the protoplasts and spheroplasts of the pathogens.Results: The formation of a clear zone around the colonies and the lysis of erythrocytes shows the antimicrobial and lytic activity of biosurfactants.Conclusion: The results of the current study reveal that surfactin from B. subtilis possesses significant antimicrobial and lytic activity.

Phenolic Metabolites ofDaleaversicolorthat Enhance Antibiotic Activity against Model Pathogenic Bacteria

2004 ◽  
Vol 67 (3) ◽  
pp. 481-484 ◽  
Author(s):  
Gil Belofsky ◽  
Diamond Percivill ◽  
Kim Lewis ◽  
George P. Tegos ◽  
Julie Ekart
Keyword(s):  
Pathogenic Bacteria ◽  
Antibiotic Activity ◽  
Phenolic Metabolites

Direct antibacterial and antibiotic resistance modulatory activity of chalcones synthesized from the natural product 2-hydroxy-3,4,6-trimethoxyacetophenone

2020 ◽  
Vol 367 (15) ◽  
Author(s):  
Thiago Sampaio de Freitas ◽  
Jayze da Cunha Xavier ◽  
Raimundo L S Pereira ◽  
Janaina E Rocha ◽  
Dédora F Muniz ◽  
...  
Keyword(s):  
Natural Product ◽  
Bacterial Resistance ◽  
Inhibitory Concentration ◽  
Multidrug Resistant ◽  
Antibiotic Activity ◽  
Antibacterial Drug ◽  
Clinical Use ◽  
Synergistic Interactions ◽  
Resistance Reversal ◽  
Over Time

ABSTRACT Antibiotic for clinical use lose its effectiveness over time due to bacterial resistance. In this work, four chalcones with modifications in their ligands were synthesized from the natural product 2-hydroxy-3,4,6-trimethoxyacetophenone, characterized by nuclear magnetic resonance (NMR) and infrared spectroscopy, and tested in bacterial models to investigate the direct and modifiers effects of the antibiotic activity of these four novel chalcones. The tests followed the broth microdilution methodology to obtain the Minimum Inhibitory Concentration (MIC). The MIC/8 of the products were used in the resistance reversion test. The chalcone 2 showed the best result in terms of direct activity, with MIC 645 μg/mL for Staphylococcus aureus and 812 μg/mL for Escherichia coli. While, for the bacterial resistance reversal test, the chalcones presented several synergistic interactions, being that chalcone 4 had the best interaction with the tested antibiotics. It was found that the type of ligand, as well as its position in the ring, interferes in the modulation of the antibiotic activity. Our results show that chalcones are strong candidates to be used as antibacterial drug or in combination with antibiotics for the treatment of infections caused by multidrug-resistant (MDR) strains.

Screening of Soil Streptomycetes – Producers of Antibiotics against Phytopathogenic Bacteria

2020 ◽  
Vol 82 (5) ◽  
pp. 36-40
Author(s):  
B.P. Matselyukh ◽  
◽  
S.L. Golembiovska ◽  
O.I. Bambura ◽  
◽  
...  
Keyword(s):  
Pathogenic Bacteria ◽  
Fungal Growth ◽  
Antibiotic Activity ◽  
Soil Samples ◽  
Complete Medium ◽  
Agar Block ◽  
Genus Streptomyces ◽  
Phytopathogenic Bacteria ◽  
Petri Dishes ◽  
Aluminum Plates

Soil is an inexhaustible source of bacteria of the genus Streptomyces – the producers of the vast majority of known antibiotics that are successfully used in medicine, veterinary and agriculture. The emergence and spread of pathogenic bacteria resistance to antibiotics requires the search for new antibiotic compounds capable of overcoming this problem. Aim. The purpose of this work was to isolate streptomycetes from soil samples of Kyiv and the Kyiv region and study their antibiotic activity against four strains of the different species of phytopathogenic bacteria. Methods. A suspension of soil in distilled water was sown on solid Chapek or corn-soybean medium in Petri dishes, in which trimethoprim and nystatin were introduced to inhibit bacterial and fungal growth. The antibiotic activity of the streptomycetes was tested by setting their agar discs on lawns of phytopathogenic bacteria in Petri dishes. Antibiotics were extracted from the streptomycetes agar cultures with a mixture of chloroform and acetone (2:1), dried in a rotary vacuum evaporator, dissolved in ethanol, separated and purified by thin layer chromatography on aluminum plates (Silica gel 60 F254 from Merck KGaA). The UV/Vis absorption spectra of the antibiotics were measured with a Beckman DU 8 spectrophotometer. Results. 10 strains of streptomycetes were isolated from the soil samples of Kyiv and the Kyiv region, whose antibiotic activity was tested against four phytopathogenic bacteria using the agar block method. Three of the streptomycetes – B8, SK and KZ, formed growth inhibition zones of different phytopathogens on complete medium in Petri dishes, among which the strain SK was the most active. This strain showed antibiotic activity against all four phytopathogenic bacteria – P. syringae 8511, P. carotovorum 8982, C. michiganensis 10 and X. campestris 8003. Conclusions. The results obtained are of interest for the protection of sensitive plants by isolated antibiotics against phytopathogenic bacteria in hothouse conditions.

scholarly journals Antibiotics from Deep-Sea Microorganisms: Current Discoveries and Perspectives

Marine Drugs ◽  
2018 ◽  
Vol 16 (10) ◽  
pp. 355 ◽  
Author(s):  
Emiliana Tortorella ◽  
Pietro Tedesco ◽  
Fortunato Palma Esposito ◽  
Grant January ◽  
Renato Fani ◽  
...  
Keyword(s):  
Multidrug Resistance ◽  
Deep Sea ◽  
Pathogenic Bacteria ◽  
Biological Activities ◽  
Extreme Environment ◽  
Antibiotic Activity ◽  
Antimicrobial Drugs ◽  
Fermentation Products ◽  
Consequent Increase ◽  
Novel Antibiotics

The increasing emergence of new forms of multidrug resistance among human pathogenic bacteria, coupled with the consequent increase of infectious diseases, urgently requires the discovery and development of novel antimicrobial drugs with new modes of action. Most of the antibiotics currently available on the market were obtained from terrestrial organisms or derived semisynthetically from fermentation products. The isolation of microorganisms from previously unexplored habitats may lead to the discovery of lead structures with antibiotic activity. The deep-sea environment is a unique habitat, and deep-sea microorganisms, because of their adaptation to this extreme environment, have the potential to produce novel secondary metabolites with potent biological activities. This review covers novel antibiotics isolated from deep-sea microorganisms. The chemical classes of the compounds, their bioactivities, and the sources of organisms are outlined. Furthermore, the authors report recent advances in techniques and strategies for the exploitation of deep-sea microorganisms.

scholarly journals Optimization of cultivation medium for the production of antibacterial agents

2013 ◽  
pp. 217-227
Author(s):  
Jovana Grahovac ◽  
Bojana Bajic ◽  
Jelena Dodic ◽  
Zorana Roncevic ◽  
Aleksandar Jokic
Keyword(s):  
Soybean Meal ◽  
Pathogenic Bacteria ◽  
Antibacterial Agents ◽  
Desirability Function ◽  
Inhibition Zone ◽  
Antibiotic Activity ◽  
Cultivation Medium ◽  
Box Behnken Design ◽  
Residual Sugar ◽  
Streptomyces Spp

Optimization of the cultivation medium for production of antibiotic effective against pathogenic bacteria Staphylococcus aureus using strain of Streptomyces spp. isolated from the environment represents the aim of this study. After the biosynthesis, the medium was analyzed by determining residual sugar and nitrogen, and the antibiotic activity was determined using diffusion-disc method. Experiments were carried out in accordance with the Box-Behnken design, with three factors varied on three levels (glucose: 10.0, 30.0 and 50.0 g/L; soybean meal: 5.0, 15.0 and 25.0 g/L; phosphates: 0.5, 1.0 and 1.5 g/L) and for the optimization of selected parameters Response Surface Methodology was used. The obtained model with the desirability function of 0.985 estimates that the lowest amounts of residual sugar (0.89 g/L) and nitrogen (0.24 g/L) and the largest possible inhibition zone diameter (21.88 mm) that with its antibiotic activity against S. aureus creates the medium containing 10.0 g/L glucose, 5.0 g/L soybean meal and 1.04 g/L phosphates.

scholarly journals Natural Product Inhibition and Enzyme Kinetics Related to Phylogenetic Characterization for Bacterial Peptidyl-tRNA Hydrolase 1

Molecules ◽  
2021 ◽  
Vol 26 (8) ◽  
pp. 2281
Author(s):  
D. Scott Strange ◽  
Steven S. Gaffin ◽  
W. Blake Holloway ◽  
Meredyth D. Kinsella ◽  
Jacob N. Wisotsky ◽  
...  
Keyword(s):  
Enzyme Kinetics ◽  
Natural Product ◽  
Small Molecule ◽  
Broad Spectrum ◽  
Pathogenic Bacteria ◽  
Product Inhibition ◽  
Antibiotic Development ◽  
Small Molecule Inhibition ◽  
Loop Region

With the relentless development of drug resistance and re-emergence of many pathogenic bacteria, the need for new antibiotics and new antibiotic targets is urgent and growing. Bacterial peptidyl-tRNA hydrolase, Pth1, is emerging as a promising new target for antibiotic development. From the conserved core and high degree of structural similarity, broad-spectrum inhibition is postulated. However, Pth1 small-molecule inhibition is still in the earliest stages. Focusing on pathogenic bacteria, herein we report the phylogenetic classification of Pth1 and natural product inhibition spanning phylogenetic space. While broad-spectrum inhibition is found, narrow-spectrum and even potentially clade-specific inhibition is more frequently observed. Additionally reported are enzyme kinetics and general in vitro Pth1 solubility that follow phylogenetic boundaries along with identification of key residues in the gate loop region that appear to govern both. The studies presented here demonstrate the sizeable potential for small-molecule inhibition of Pth1, improve understanding of Pth enzymes, and advance Pth1 as a much-needed novel antibiotic target.

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